Pub Date : 2025-01-31DOI: 10.2174/0122117385329819241212040246
Mahkesha Nisha, Mohammad Adnan, Kalyani Sakure, Ajazuddin, Parag Jain
This thorough analysis looks critically at how glycosaminoglycan (GAG) supports joint health. It emphasizes the importance of GAG in particular, clarifies the underlying processes linked to joint pain, and assesses the shortcomings of traditional therapy modalities. Additionally, the research delves into several traditional approaches, such as injectable GAG therapy and oral supplements, carefully evaluating the benefits and drawbacks of each. The study then explores novel GAG drug delivery technologies, acknowledging the urgent need for better treatment approaches. The article highlights the potential of hydrogel-based systems, liposomal/micellar carriers, and nanoparticles in addressing current challenges in GAG delivery. These challenges include achieving sustained release, improving bioavailability, facilitating targeted delivery, and reducing safety concerns related to biocompatibility. Examining these elements closely and critically, the review seeks to provide a thorough grasp of the developments, difficulties, and possible breakthroughs in GAG delivery systems. In the end, this thorough investigation will greatly aid in the improvement of joint pain therapies. The results imply that by shielding articular joints from erosive effects, early use of GAG therapy-particularly hyaluronic acid-can reduce joint deterioration associated with arthritis. Even though GAG-based therapies have shown promise in lowering inflammation and increasing joint flexibility, further study is required to improve their effectiveness in treating joint pain, particularly in diseases like osteoarthritis.
{"title":"Innovations in Glycosaminoglycan Delivery: Transforming Joint Health Therapies.","authors":"Mahkesha Nisha, Mohammad Adnan, Kalyani Sakure, Ajazuddin, Parag Jain","doi":"10.2174/0122117385329819241212040246","DOIUrl":"https://doi.org/10.2174/0122117385329819241212040246","url":null,"abstract":"<p><p>This thorough analysis looks critically at how glycosaminoglycan (GAG) supports joint health. It emphasizes the importance of GAG in particular, clarifies the underlying processes linked to joint pain, and assesses the shortcomings of traditional therapy modalities. Additionally, the research delves into several traditional approaches, such as injectable GAG therapy and oral supplements, carefully evaluating the benefits and drawbacks of each. The study then explores novel GAG drug delivery technologies, acknowledging the urgent need for better treatment approaches. The article highlights the potential of hydrogel-based systems, liposomal/micellar carriers, and nanoparticles in addressing current challenges in GAG delivery. These challenges include achieving sustained release, improving bioavailability, facilitating targeted delivery, and reducing safety concerns related to biocompatibility. Examining these elements closely and critically, the review seeks to provide a thorough grasp of the developments, difficulties, and possible breakthroughs in GAG delivery systems. In the end, this thorough investigation will greatly aid in the improvement of joint pain therapies. The results imply that by shielding articular joints from erosive effects, early use of GAG therapy-particularly hyaluronic acid-can reduce joint deterioration associated with arthritis. Even though GAG-based therapies have shown promise in lowering inflammation and increasing joint flexibility, further study is required to improve their effectiveness in treating joint pain, particularly in diseases like osteoarthritis.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143123361","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-01-30DOI: 10.2174/0122117385323941241211084423
Zahra Khaksari, Freshteh Mehri, Mohadeseh Haji Abdolvahab, Mohammad Amin Manavi, Mohammad Hosein Fathian Nasab, Ashkan Karbasi, Maryam Baeeri, Akram Ranjbar
<p><strong>Introduction: </strong>Crocin, a natural compound found in saffron, has shown promising potential as an anti-inflammatory and antioxidant agent. Paraquat is a widely used herbicide known to cause severe oxidative stress and inflammation in the liver, leading to significant tissue damage. This study explores the potential of crocin and its nanoformulation for mitigating paraquat-induced liver damage associated with inflammation and oxidative stress.</p><p><strong>Materials and methods: </strong>The experimental design included 30 male Wistar rats divided into a control group, a paraquat group (5 mg/kg/day for 1 week, i.p.), and four treatment groups: crocin (20 mg/kg/day for 1 week, i.p.), nano-crocin (20 mg/kg/day for 1 week, i.p.), crocin+paraquat, and nano-crocin+paraquat. The levels of TNF-α, IL-1β, and NF-κB mRNA, reactive oxygen species (ROS), lipid peroxidation (LPO) generation, thiol level, and superoxide dismutase (SOD) activity were assessed.</p><p><strong>Results: </strong>According to the results, the TNF-α, IL-1β, and NF-κB mRNA levels, as well as LPO and ROS generation increased following paraquat administration. Furthermore, both treatment groups showed significantly lower levels compared to the paraquat group (p<0.0001), with the nano-crocin group showing the most significant reduction (p<0.0001). On the other hand, reduced thiol level and SOD activity in the paraquat group were significantly attenuated by crocin and nano-crocin administration (p<0.0001). Notably, nano-crocin exhibited superior protective effects, with a greater reduction in inflammatory markers and oxidative stress indicators compared to crocin (p<0.01).</p><p><strong>Discussion: </strong>This study provides strong evidence that nano-crocin offers superior hepatoprotective effects over crocin in mitigating paraquat-induced liver injury by reducing oxidative stress and inflammation. The results suggest that nano-crocin could be a promising candidate for the development of novel antioxidant therapies targeting liver diseases characterized by oxidative stress. The study further elucidates the underlying mechanisms of action, highlighting the role of nano-crocin in modulating inflammatory pathways and enhancing antioxidant defenses, which may be attributed to its improved bioavailability and targeted delivery. Future studies should focus on the long-term safety and efficacy of nano-crocin, as well as exploring its potential applications in other models of liver injury and systemic oxidative stress-related diseases.</p><p><strong>Conclusion: </strong>In conclusion, nano-crocin treatment exerted more protective effects than crocin on the liver against inflammation and oxidative stress induced by paraquat. These findings suggest that nano-crocin could serve as a promising therapeutic candidate for the management of liver diseases characterized by oxidative stress and inflammation. Future studies should focus on exploring the long-term safety and efficacy of na
{"title":"Crocin and Nano-Crocin Mitigate Paraquat Hepatotoxicity by Modulating Expression of Genes Involved in Oxidative Stress and Inflammation.","authors":"Zahra Khaksari, Freshteh Mehri, Mohadeseh Haji Abdolvahab, Mohammad Amin Manavi, Mohammad Hosein Fathian Nasab, Ashkan Karbasi, Maryam Baeeri, Akram Ranjbar","doi":"10.2174/0122117385323941241211084423","DOIUrl":"https://doi.org/10.2174/0122117385323941241211084423","url":null,"abstract":"<p><strong>Introduction: </strong>Crocin, a natural compound found in saffron, has shown promising potential as an anti-inflammatory and antioxidant agent. Paraquat is a widely used herbicide known to cause severe oxidative stress and inflammation in the liver, leading to significant tissue damage. This study explores the potential of crocin and its nanoformulation for mitigating paraquat-induced liver damage associated with inflammation and oxidative stress.</p><p><strong>Materials and methods: </strong>The experimental design included 30 male Wistar rats divided into a control group, a paraquat group (5 mg/kg/day for 1 week, i.p.), and four treatment groups: crocin (20 mg/kg/day for 1 week, i.p.), nano-crocin (20 mg/kg/day for 1 week, i.p.), crocin+paraquat, and nano-crocin+paraquat. The levels of TNF-α, IL-1β, and NF-κB mRNA, reactive oxygen species (ROS), lipid peroxidation (LPO) generation, thiol level, and superoxide dismutase (SOD) activity were assessed.</p><p><strong>Results: </strong>According to the results, the TNF-α, IL-1β, and NF-κB mRNA levels, as well as LPO and ROS generation increased following paraquat administration. Furthermore, both treatment groups showed significantly lower levels compared to the paraquat group (p<0.0001), with the nano-crocin group showing the most significant reduction (p<0.0001). On the other hand, reduced thiol level and SOD activity in the paraquat group were significantly attenuated by crocin and nano-crocin administration (p<0.0001). Notably, nano-crocin exhibited superior protective effects, with a greater reduction in inflammatory markers and oxidative stress indicators compared to crocin (p<0.01).</p><p><strong>Discussion: </strong>This study provides strong evidence that nano-crocin offers superior hepatoprotective effects over crocin in mitigating paraquat-induced liver injury by reducing oxidative stress and inflammation. The results suggest that nano-crocin could be a promising candidate for the development of novel antioxidant therapies targeting liver diseases characterized by oxidative stress. The study further elucidates the underlying mechanisms of action, highlighting the role of nano-crocin in modulating inflammatory pathways and enhancing antioxidant defenses, which may be attributed to its improved bioavailability and targeted delivery. Future studies should focus on the long-term safety and efficacy of nano-crocin, as well as exploring its potential applications in other models of liver injury and systemic oxidative stress-related diseases.</p><p><strong>Conclusion: </strong>In conclusion, nano-crocin treatment exerted more protective effects than crocin on the liver against inflammation and oxidative stress induced by paraquat. These findings suggest that nano-crocin could serve as a promising therapeutic candidate for the management of liver diseases characterized by oxidative stress and inflammation. Future studies should focus on exploring the long-term safety and efficacy of na","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143123359","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-01-27DOI: 10.2174/0122117385358312250108180301
Pooja V Nagime, Nishat M Shaikh, Sudarshan Singh, Vaishali S Chandak, Vijay R Chidrawar, Eloise Parry Nweye
Metallic nanostructures play a vital role in technological advancement, providing exceptional performance and improved adaptability in comparison to their bulk equivalents. Conventional synthesis techniques frequently depend on dangerous reducing agents to transform metal ions into Nanoparticles (NPs), which presents considerable environmental and health issues. In contrast, the approach of green synthesis, which emphasizes the use of non-toxic reagents, has garnered significant interest as a sustainable method for the fabrication of Metallic Nanoparticles (MNPs). This sustainable approach utilizes biological sources, like actinomycetes, algae, fungi, polymers, crops, waste biomass, and yeast, recognized for their excellent biocompatibility, availability, affordability, and efficiency. Biological extracts act as reducing and stabilizing agents, with the metabolites and enzymes present in these extracts aiding in the conversion of metal ions into nanoparticles. This review offers an in-depth examination of different MNPs, such as copper, gold, platinum, silver, and zinc, emphasizing their distinct characteristics and a variety of synthesis methods. The review further explores the diverse applications of MNPs in biomimetics, agriculture, and various industrial sectors, including energy, catalysis, and wastewater treatment, along with optical enhancement. This review explores stability and toxicity profiles, filling a significant gap in the existing knowledge base and providing valuable insights into the broad applicability of MNPs.
{"title":"Metallic Nanostructures: An Updated Review on Synthesis, Stability, Safety, and Applications with Tremendous Multifunctional Opportunities.","authors":"Pooja V Nagime, Nishat M Shaikh, Sudarshan Singh, Vaishali S Chandak, Vijay R Chidrawar, Eloise Parry Nweye","doi":"10.2174/0122117385358312250108180301","DOIUrl":"https://doi.org/10.2174/0122117385358312250108180301","url":null,"abstract":"<p><p>Metallic nanostructures play a vital role in technological advancement, providing exceptional performance and improved adaptability in comparison to their bulk equivalents. Conventional synthesis techniques frequently depend on dangerous reducing agents to transform metal ions into Nanoparticles (NPs), which presents considerable environmental and health issues. In contrast, the approach of green synthesis, which emphasizes the use of non-toxic reagents, has garnered significant interest as a sustainable method for the fabrication of Metallic Nanoparticles (MNPs). This sustainable approach utilizes biological sources, like actinomycetes, algae, fungi, polymers, crops, waste biomass, and yeast, recognized for their excellent biocompatibility, availability, affordability, and efficiency. Biological extracts act as reducing and stabilizing agents, with the metabolites and enzymes present in these extracts aiding in the conversion of metal ions into nanoparticles. This review offers an in-depth examination of different MNPs, such as copper, gold, platinum, silver, and zinc, emphasizing their distinct characteristics and a variety of synthesis methods. The review further explores the diverse applications of MNPs in biomimetics, agriculture, and various industrial sectors, including energy, catalysis, and wastewater treatment, along with optical enhancement. This review explores stability and toxicity profiles, filling a significant gap in the existing knowledge base and providing valuable insights into the broad applicability of MNPs.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143053129","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-01-27DOI: 10.2174/0122117385346215250109142123
Gopinath Subramaniyan, Rubina Shaik, Bachu Venkata Ramana, Meriton Stanley A, Devasena Srinivasan
Aim: This study aimed to develop and evaluate lornoxicam (LXM) and thiocolchicoside (TCS) transferosomal transdermal patches.
Background: Oral administration of LXM and TCS can lead to gastric irritation, necessitating alternative delivery methods for pain and inflammation relief. Incorporating LXM & TCS into transferosomes within a transdermal patch offers a potential solution.
Objective: The objective of this study is to develop and evaluate transferosomal transdermal patches containing LXM and TCS, incorporating Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers. The aim is to enhance the skin permeation of these drugs while mitigating gastric irritation associated with their oral administration.
Method: Transferosomes were made by the thin film hydration tactic, with nine formulations based on three independent variables: phosphatidylcholine, span 80, and sonication time. Entrapment efficiency and drug release at 6th h were assessed as dependent variables. The optimized combination was then formulated into transdermal patches via central composite design, evaluating the impact of AVLM and LO on lornoxicam discharge and other physicochemical properties.
Results: The average weight and thickness of the patches ranged from 7.52±0.75 to 8.07±0.11g and from 1.69±0.01 to 1.82±0.02mm, respectively, representing minimal variance. The LXM/TCS content homogeneity ranged from 92.84±3.55 to 94.07±4.61% for LXM and from 90.17±1.98 to 93.18±2.98% for TCS, demonstrating robust uniformity. Higher proportions of phosphatidylcholine and span 80, along with lesser sonication time, led to improved entrapment of lornoxicam. In vitro, discharge studies demonstrated optimal discharge with a higher proportion of phosphatidylcholine, a medium proportion of span 80, and a longer sonication time. The transferosomal patches exhibited zero-order discharge kinetics, with LXM & TCS discharge % at 24, 48, and 72 h.
Conclusion: The study concludes that formulation TDP-8, which incorporates 3g of Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers, demonstrated favorable discharge characteristics. This indicates its potential as an effective transdermal delivery system for LXM and TCS, offering a promising substitute for pain and inflammation relief while minimizing gastric irritation. The study succeeded in developing and evaluating transferosomal transdermal patches for LXM and TCS, providing an alternative delivery method that minimizes gastric irritation.
{"title":"Revolutionizing Drug Delivery: A Design Professional's Approach to Drug-loaded Transferosomal Vesicles for Transdermal Use.","authors":"Gopinath Subramaniyan, Rubina Shaik, Bachu Venkata Ramana, Meriton Stanley A, Devasena Srinivasan","doi":"10.2174/0122117385346215250109142123","DOIUrl":"https://doi.org/10.2174/0122117385346215250109142123","url":null,"abstract":"<p><strong>Aim: </strong>This study aimed to develop and evaluate lornoxicam (LXM) and thiocolchicoside (TCS) transferosomal transdermal patches.</p><p><strong>Background: </strong>Oral administration of LXM and TCS can lead to gastric irritation, necessitating alternative delivery methods for pain and inflammation relief. Incorporating LXM & TCS into transferosomes within a transdermal patch offers a potential solution.</p><p><strong>Objective: </strong>The objective of this study is to develop and evaluate transferosomal transdermal patches containing LXM and TCS, incorporating Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers. The aim is to enhance the skin permeation of these drugs while mitigating gastric irritation associated with their oral administration.</p><p><strong>Method: </strong>Transferosomes were made by the thin film hydration tactic, with nine formulations based on three independent variables: phosphatidylcholine, span 80, and sonication time. Entrapment efficiency and drug release at 6th h were assessed as dependent variables. The optimized combination was then formulated into transdermal patches via central composite design, evaluating the impact of AVLM and LO on lornoxicam discharge and other physicochemical properties.</p><p><strong>Results: </strong>The average weight and thickness of the patches ranged from 7.52±0.75 to 8.07±0.11g and from 1.69±0.01 to 1.82±0.02mm, respectively, representing minimal variance. The LXM/TCS content homogeneity ranged from 92.84±3.55 to 94.07±4.61% for LXM and from 90.17±1.98 to 93.18±2.98% for TCS, demonstrating robust uniformity. Higher proportions of phosphatidylcholine and span 80, along with lesser sonication time, led to improved entrapment of lornoxicam. In vitro, discharge studies demonstrated optimal discharge with a higher proportion of phosphatidylcholine, a medium proportion of span 80, and a longer sonication time. The transferosomal patches exhibited zero-order discharge kinetics, with LXM & TCS discharge % at 24, 48, and 72 h.</p><p><strong>Conclusion: </strong>The study concludes that formulation TDP-8, which incorporates 3g of Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers, demonstrated favorable discharge characteristics. This indicates its potential as an effective transdermal delivery system for LXM and TCS, offering a promising substitute for pain and inflammation relief while minimizing gastric irritation. The study succeeded in developing and evaluating transferosomal transdermal patches for LXM and TCS, providing an alternative delivery method that minimizes gastric irritation.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143053130","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-01-24DOI: 10.2174/0122117385331332241226101149
Dyandevi Mathure, Sejal Bhandare, Dipanjan Karati, Mohammad Adnan, Dileep Kumar
Even with recent advancements in surgery and multimodal adjuvant therapy, brain cancer treatment is still difficult. The blood-brain barrier and the potentially deadly medications' nonspecificity have made pharmacological treatment for brain cancer particularly ineffective. The nanoparticle has surfaced as a viable brain delivery vector that can solve the issues with existing approaches. Furthermore, it is possible to integrate many functions into a single nanoplatform to enable tumor-specific diagnosis, therapy, and follow-up observation. Conventional technology does not allow for such multitasking. Recent developments in brain cancer treatment and detection using nanoparticles are discussed in this study. The benefits of delivery via nanoparticles are discussed, along with the kinds of nanoparticle systems being studied and their potential uses.
{"title":"Unraveling the Mysteries of Brain Cancer from Diagnosis to Treatment.","authors":"Dyandevi Mathure, Sejal Bhandare, Dipanjan Karati, Mohammad Adnan, Dileep Kumar","doi":"10.2174/0122117385331332241226101149","DOIUrl":"https://doi.org/10.2174/0122117385331332241226101149","url":null,"abstract":"<p><p>Even with recent advancements in surgery and multimodal adjuvant therapy, brain cancer treatment is still difficult. The blood-brain barrier and the potentially deadly medications' nonspecificity have made pharmacological treatment for brain cancer particularly ineffective. The nanoparticle has surfaced as a viable brain delivery vector that can solve the issues with existing approaches. Furthermore, it is possible to integrate many functions into a single nanoplatform to enable tumor-specific diagnosis, therapy, and follow-up observation. Conventional technology does not allow for such multitasking. Recent developments in brain cancer treatment and detection using nanoparticles are discussed in this study. The benefits of delivery via nanoparticles are discussed, along with the kinds of nanoparticle systems being studied and their potential uses.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143047373","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-01-21DOI: 10.2174/0122117385341583250119054309
Irfan A Mohammed, Sriramakamal Jonnalagadda
Background: Itraconazole (ICZ) has been approved by the FDA to treat many fungal infections including, blastomycosis, histoplasmosis, and aspergillosis. ICZ can be also used as prophylaxis in the population who are at high risk for developing systemic fungal infections, such as HIV patients, and chemotherapy patients.
Aim: However, since ICZ is a BCS Class II drug that has low solubility and high permeability, leads to low oral bioavailability. In addition, the absorption of ICZ from commercial oral dosage forms is highly affected by food intake and pH.
Objective: The current study aimed to develop, optimize, and characterize ICZ-loaded solid lipid nanoparticles (ICZ-SLNs) using a Central Composite Design for improved solubility and extendedrelease profile.
Methods: ICZ-SLNs were optimized based on physicochemical characteristics. ICZ-SLNs were also evaluated for differential scanning calorimetry (DSC), in-vitro release, lyophilization, transmission electron microscopy (TEM), and physicochemical stability at refrigerated and room temperatures for three months.
Results: The optimized ICZ-SLNs formulation showed particle size, polydispersity index, zeta potential, drug content, and entrapment efficiency of 335.6±8.0 nm, 0.25±0.02, -23.8±0.5 mV, 98.3±2.5%, and 99.5±1.5%, respectively. ICZ-SLN dispersions showed extended-release profiles for ICZ compared to the control solution over 24 h. The absence of the endothermic melting drug peak of the lyophilized formulation indicated that the drug was converted to its amorphous form inside the solid matrix. In addition, TEM studies showed spherical shape nanoparticles. Moreover, the optimized ICZ-SLN formulation was stable at both tested storage conditions.
Conclusion: The current ICZ formulation could exhibit improved oral bioavailability with better therapeutic outcomes during the treatment of systemic fungal infections.
{"title":"Enhancing Solubility of a BCS Class II Drug- Itraconazole by Developing and Optimizing Solid Lipid Nanoparticles using a Central Composite Design.","authors":"Irfan A Mohammed, Sriramakamal Jonnalagadda","doi":"10.2174/0122117385341583250119054309","DOIUrl":"https://doi.org/10.2174/0122117385341583250119054309","url":null,"abstract":"<p><strong>Background: </strong>Itraconazole (ICZ) has been approved by the FDA to treat many fungal infections including, blastomycosis, histoplasmosis, and aspergillosis. ICZ can be also used as prophylaxis in the population who are at high risk for developing systemic fungal infections, such as HIV patients, and chemotherapy patients.</p><p><strong>Aim: </strong>However, since ICZ is a BCS Class II drug that has low solubility and high permeability, leads to low oral bioavailability. In addition, the absorption of ICZ from commercial oral dosage forms is highly affected by food intake and pH.</p><p><strong>Objective: </strong>The current study aimed to develop, optimize, and characterize ICZ-loaded solid lipid nanoparticles (ICZ-SLNs) using a Central Composite Design for improved solubility and extendedrelease profile.</p><p><strong>Methods: </strong>ICZ-SLNs were optimized based on physicochemical characteristics. ICZ-SLNs were also evaluated for differential scanning calorimetry (DSC), in-vitro release, lyophilization, transmission electron microscopy (TEM), and physicochemical stability at refrigerated and room temperatures for three months.</p><p><strong>Results: </strong>The optimized ICZ-SLNs formulation showed particle size, polydispersity index, zeta potential, drug content, and entrapment efficiency of 335.6±8.0 nm, 0.25±0.02, -23.8±0.5 mV, 98.3±2.5%, and 99.5±1.5%, respectively. ICZ-SLN dispersions showed extended-release profiles for ICZ compared to the control solution over 24 h. The absence of the endothermic melting drug peak of the lyophilized formulation indicated that the drug was converted to its amorphous form inside the solid matrix. In addition, TEM studies showed spherical shape nanoparticles. Moreover, the optimized ICZ-SLN formulation was stable at both tested storage conditions.</p><p><strong>Conclusion: </strong>The current ICZ formulation could exhibit improved oral bioavailability with better therapeutic outcomes during the treatment of systemic fungal infections.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143024283","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-01-17DOI: 10.2174/0122117385353188241218153916
Devesh U Kapoor, Mansi Gaur, Hetal Hingalajia, Sudarshan Singh, Bhupendra G Prajapati
Polymeric nano-discs offer a promising and adaptable nanocarrier platform for topical applications involving the targeted administration of drugs. These biocompatible polymer-based, disc-shaped, nanoscale structures have drawn interest due to their exceptional capacity to encapsulate a diverse range of theranostics. Theranostics, the concept of combining treatments and diagnostics into a single system, is the core of attraction. Precision and fewer adverse effects are provided by the regulated and prolonged release of these drugs made possible by polymeric nano-discs. They also offer the perfect foundation for keeping track of the effectiveness of treatments. The selection of polymeric materials that provide biocompatibility and customized release mechanisms is critical to effectively implementing polymeric nano-discs. Recent pre-clinical and clinical research has demonstrated efficacy in targeted therapeutic interventions. Nevertheless, there are obstacles and restrictions in real-world implementation, and more study is necessary to fully realize their potential. Hence polymeric nano-discs offer controlled drug release and simultaneous diagnostic capabilities, making them a flexible and viable path forward for topical theranostics. Their advancement has opportunities for improved treatment results; however, more study is needed to properly resolve obstacles and realize their therapeutic potential.
{"title":"Polymeric Nano-discs: A Versatile Nanocarrier Platform for Delivering Topical Theranostics.","authors":"Devesh U Kapoor, Mansi Gaur, Hetal Hingalajia, Sudarshan Singh, Bhupendra G Prajapati","doi":"10.2174/0122117385353188241218153916","DOIUrl":"https://doi.org/10.2174/0122117385353188241218153916","url":null,"abstract":"<p><p>Polymeric nano-discs offer a promising and adaptable nanocarrier platform for topical applications involving the targeted administration of drugs. These biocompatible polymer-based, disc-shaped, nanoscale structures have drawn interest due to their exceptional capacity to encapsulate a diverse range of theranostics. Theranostics, the concept of combining treatments and diagnostics into a single system, is the core of attraction. Precision and fewer adverse effects are provided by the regulated and prolonged release of these drugs made possible by polymeric nano-discs. They also offer the perfect foundation for keeping track of the effectiveness of treatments. The selection of polymeric materials that provide biocompatibility and customized release mechanisms is critical to effectively implementing polymeric nano-discs. Recent pre-clinical and clinical research has demonstrated efficacy in targeted therapeutic interventions. Nevertheless, there are obstacles and restrictions in real-world implementation, and more study is necessary to fully realize their potential. Hence polymeric nano-discs offer controlled drug release and simultaneous diagnostic capabilities, making them a flexible and viable path forward for topical theranostics. Their advancement has opportunities for improved treatment results; however, more study is needed to properly resolve obstacles and realize their therapeutic potential.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143009443","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Background: Malaria remains a formidable public health obstacle across Africa, Southeast Asia, and portions of South America, exacerbated by resistance to antimalarial medications, such as artemisinin-based combinations. The combination of curcumin and artemisinin shows promise due to its potential for dose reduction, reduced toxicity, synergistic effects, and suitability for drug delivery improvement.
Objectives: This research aims to enhance the solubility and dissolution rates of curcumin and artemisinin by employing Solid Lipid Nanoparticles (SLNs). Oral delivery of both drugs faces challenges due to their poor water solubility, inefficient absorption, and rapid metabolism and elimination.
Methods: The study focuses on formulating and optimizing Solid Lipid Nanoparticles (SLNs) encapsulating artemisinin (ART) and curcumin (CUR). SLNs were developed using the hot homogenization method, incorporating ultrasonication. Drug-excipient compatibility was evaluated using Differential Scanning Calorimetry (DSC). Lipid and surfactant screening was performed to select suitable components. A 3² full factorial design was utilized to investigate the influence of lipid and surfactant concentrations on key parameters, such as entrapment efficiency (%EE) and cumulative drug release (%CDR). Additionally, evaluations of %EE, drug loading, particle size, zeta potential, and in-vitro drug release were conducted.
Results: Successful development of artemisinin and curcumin SLNs was achieved using a full factorial design, demonstrating controlled drug release and high entrapment efficiency. The optimized nanoparticles exhibited a size of 114.7nm, uniformity (PDI: 0.261), and a zeta potential of -9.24 mV. Artemisinin and curcumin showed %EE values of 79.1% and 74.5%, respectively, with cumulative drug release of 85.1% and 80.9%, respectively. The full factorial design indicated that increased lipid concentration improved %EE, while higher surfactant concentration enhanced drug release and %EE. Stability studies of the optimized batch revealed no alterations in physical or chemical characteristics.
Conclusion: The study successfully developed Solid Lipid Nanoparticles (SLNs) for artemisinin and curcumin, achieving controlled drug release, high entrapment efficiency, and desired particle size and uniformity. This advancement holds promise for enhancing drug delivery of herbal formulations.
{"title":"Preparation and <i>In-Vitro</i> Characterization of Solid Lipid Nanoparticles Containing Artemisinin and Curcumin.","authors":"Bhagyashri Khatri, Vaishali Thakkar, Saloni Dalwadi, Avani Shah, Hardik Rana, Purvi Shah, Tejal Gandhi, Bhupendra Prajapati","doi":"10.2174/0122117385296893240626061552","DOIUrl":"10.2174/0122117385296893240626061552","url":null,"abstract":"<p><strong>Background: </strong>Malaria remains a formidable public health obstacle across Africa, Southeast Asia, and portions of South America, exacerbated by resistance to antimalarial medications, such as artemisinin-based combinations. The combination of curcumin and artemisinin shows promise due to its potential for dose reduction, reduced toxicity, synergistic effects, and suitability for drug delivery improvement.</p><p><strong>Objectives: </strong>This research aims to enhance the solubility and dissolution rates of curcumin and artemisinin by employing Solid Lipid Nanoparticles (SLNs). Oral delivery of both drugs faces challenges due to their poor water solubility, inefficient absorption, and rapid metabolism and elimination.</p><p><strong>Methods: </strong>The study focuses on formulating and optimizing Solid Lipid Nanoparticles (SLNs) encapsulating artemisinin (ART) and curcumin (CUR). SLNs were developed using the hot homogenization method, incorporating ultrasonication. Drug-excipient compatibility was evaluated using Differential Scanning Calorimetry (DSC). Lipid and surfactant screening was performed to select suitable components. A 3² full factorial design was utilized to investigate the influence of lipid and surfactant concentrations on key parameters, such as entrapment efficiency (%EE) and cumulative drug release (%CDR). Additionally, evaluations of %EE, drug loading, particle size, zeta potential, and <i>in-vitro</i> drug release were conducted.</p><p><strong>Results: </strong>Successful development of artemisinin and curcumin SLNs was achieved using a full factorial design, demonstrating controlled drug release and high entrapment efficiency. The optimized nanoparticles exhibited a size of 114.7nm, uniformity (PDI: 0.261), and a zeta potential of -9.24 mV. Artemisinin and curcumin showed %EE values of 79.1% and 74.5%, respectively, with cumulative drug release of 85.1% and 80.9%, respectively. The full factorial design indicated that increased lipid concentration improved %EE, while higher surfactant concentration enhanced drug release and %EE. Stability studies of the optimized batch revealed no alterations in physical or chemical characteristics.</p><p><strong>Conclusion: </strong>The study successfully developed Solid Lipid Nanoparticles (SLNs) for artemisinin and curcumin, achieving controlled drug release, high entrapment efficiency, and desired particle size and uniformity. This advancement holds promise for enhancing drug delivery of herbal formulations.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"199-211"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141748762","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-01-01DOI: 10.2174/0122117385306495240529052911
Swarupananda Mukherjee, Ayon Dutta, Dipanjana Ash, Dipanjan Karati
Cubosomes, a novel drug delivery system, have gained significant attention in recent years due to their unique self-assembled structures and enhanced drug encapsulation capabilities. They are administered by oral, ophthalmic, transdermal, and chemotherapeutic routes, to name a few. Due to their many potential benefits-which include high drug dispersal due to the cubic structure, a large surface area, a relatively simple manufacturing process, biodegradability, the capacity to encapsulate hydrophobic, hydrophilic, and amphiphilic compounds, targeted and controlled release of bioactive agents, and the biodegradability of lipids-cubosomes show enormous promise in drug nanoformulations for cancer therapeutics. The most common preparation method involves emulsifying a monoglyceride with a polymer, homogenizing, and then sonicating the mixture. Two distinct approaches to preparing are top-down and bottom-up. This evaluation will examine the materials, methods of preparation, cubosome-related drug encapsulating techniques, drug loading, release mechanism, and their uses. The following databases were used for literature searches: PubMed, Frontiers, Science Direct, Springer, Wiley, and MDPI. For the purpose of finding pertinent articles and contents (2015-2024), the keywords "cubosome; drug delivery systems, nano-carrier, theranostic, drug release mechanism" and others of a similar nature were utilized. This review will conduct a comprehensive analysis of the cubosome-related composition, production methods, drug encapsulating strategies, drug release mechanisms, and applications. Moreover, the difficulties encountered in fine-tuning different parameters to improve loading capabilities and prospects are also discussed. Innovation in pharmaceutical research and development can be stimulated by the knowledge gathered about cubosomal drug delivery methods. Through the clarification of the mechanisms involved in drug release from cubosomes and the investigation of innovative fabrication procedures, scientists can enhance the cubosomal formulation design for targeted therapeutic uses.
立方体是一种新型给药系统,近年来因其独特的自组装结构和更强的药物封装能力而备受关注。它们可通过口服、眼科、透皮和化疗等途径给药。由于它们具有许多潜在的优点--包括立方结构带来的高药物分散性、大表面积、相对简单的制造工艺、生物可降解性、封装疏水性、亲水性和两性化合物的能力、生物活性剂的定向和控制释放以及脂质的生物可降解性--在癌症治疗药物纳米制剂方面显示出巨大的前景。最常见的制备方法是将单甘酯与聚合物乳化、均质,然后对混合物进行超声处理。自上而下和自下而上是两种不同的制备方法。本评估将研究材料、制备方法、立方体相关的药物封装技术、药物负载、释放机制及其用途。文献检索使用了以下数据库:PubMed、Frontiers、Science Direct、Springer、Wiley 和 MDPI。为了查找相关文章和内容(2015-2024 年),使用了关键词 "cubosome; drug delivery systems, nano-carrier, theranostic, drug release mechanism "及其他类似性质的关键词。本综述将全面分析立方体的相关组成、生产方法、药物封装策略、药物释放机制和应用。此外,还将讨论在微调不同参数以提高装载能力方面遇到的困难和前景。有关立方体给药方法的知识可以促进药物研发的创新。通过阐明立方体释放药物的机制和研究创新的制造程序,科学家们可以提高立方体配方设计的针对性治疗用途。.
{"title":"An Insight into Cubosomal Drug Delivery Approaches: An Explicative Review.","authors":"Swarupananda Mukherjee, Ayon Dutta, Dipanjana Ash, Dipanjan Karati","doi":"10.2174/0122117385306495240529052911","DOIUrl":"10.2174/0122117385306495240529052911","url":null,"abstract":"<p><p>Cubosomes, a novel drug delivery system, have gained significant attention in recent years due to their unique self-assembled structures and enhanced drug encapsulation capabilities. They are administered by oral, ophthalmic, transdermal, and chemotherapeutic routes, to name a few. Due to their many potential benefits-which include high drug dispersal due to the cubic structure, a large surface area, a relatively simple manufacturing process, biodegradability, the capacity to encapsulate hydrophobic, hydrophilic, and amphiphilic compounds, targeted and controlled release of bioactive agents, and the biodegradability of lipids-cubosomes show enormous promise in drug nanoformulations for cancer therapeutics. The most common preparation method involves emulsifying a monoglyceride with a polymer, homogenizing, and then sonicating the mixture. Two distinct approaches to preparing are top-down and bottom-up. This evaluation will examine the materials, methods of preparation, cubosome-related drug encapsulating techniques, drug loading, release mechanism, and their uses. The following databases were used for literature searches: PubMed, Frontiers, Science Direct, Springer, Wiley, and MDPI. For the purpose of finding pertinent articles and contents (2015-2024), the keywords \"cubosome; drug delivery systems, nano-carrier, theranostic, drug release mechanism\" and others of a similar nature were utilized. This review will conduct a comprehensive analysis of the cubosome-related composition, production methods, drug encapsulating strategies, drug release mechanisms, and applications. Moreover, the difficulties encountered in fine-tuning different parameters to improve loading capabilities and prospects are also discussed. Innovation in pharmaceutical research and development can be stimulated by the knowledge gathered about cubosomal drug delivery methods. Through the clarification of the mechanisms involved in drug release from cubosomes and the investigation of innovative fabrication procedures, scientists can enhance the cubosomal formulation design for targeted therapeutic uses.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"794-803"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141443170","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Background: HER2-positive breast cancer is an aggressive subtype characterized by the overexpression of the HER2 receptor, a transmembrane glycoprotein critical for tumor progression. Current therapies often face challenges like drug resistance and systemic toxicity, necessitating the development of advanced drug delivery systems.
Objective: This study aimed to fabricate and determine the cytotoxicity of pH-sensitive PLA nanoparticles dual-loaded with docetaxel and each of the small molecule tyrosine kinase inhibitors (STKIs) (tucatinib, neratinib, lapatinib) in HER2-positive breast cancer cells.
Method: Nanoparticles were synthesized by a dispersion polymerization method using an acidlabile crosslinking agent, PEG and lactide macromonomers. They were characterized for structure (TEM), surface morphology (SEM), particle size, polydispersity index, zeta potential, and drug loading capacity. Cytotoxicity was assessed in vitro on SKBR3 and MCF7 breast cancer cell lines, with IC50 values compared across formulations.
Results: The nanoparticles were spherical with nanoscale sizes and negative zeta potential values. In vitro studies demonstrated enhanced antiproliferative effects of the drug-loaded nanoparticles, with synergistic activity observed between docetaxel and the STKIs. The drug concentrations were halved in combination formulations and resulted in better cytotoxicity compared to single-drug treatments, particularly against SKBR3 cells. The IC50 values were lower in SKBR3 cells than in MCF7 cells, highlighting the role of HER2 expression in the activity of TKIs.
Conclusion: The pH-sensitive PLA nanoparticles effectively co-delivered docetaxel and STKIs and demonstrated enhanced efficacy and reduced drug dosages in HER2-positive breast cancer models. This study provides a foundation for further exploration of nanoparticle-based combination therapies with potential applications in treating other aggressive cancer types.
{"title":"Nanotechnology Platform for the Delivery of Docetaxel and Tyrosine Kinase Inhibitors for HER2-Positive Breast Cancer Therapy.","authors":"Bharathi Mandala, Yvonne Berko, Gantumur Battogtokh, Funmilola Fisusi, Haijun Gao, Emmanuel O Akala","doi":"10.2174/0122117385373466250219070753","DOIUrl":"10.2174/0122117385373466250219070753","url":null,"abstract":"<p><strong>Background: </strong>HER2-positive breast cancer is an aggressive subtype characterized by the overexpression of the HER2 receptor, a transmembrane glycoprotein critical for tumor progression. Current therapies often face challenges like drug resistance and systemic toxicity, necessitating the development of advanced drug delivery systems.</p><p><strong>Objective: </strong>This study aimed to fabricate and determine the cytotoxicity of pH-sensitive PLA nanoparticles dual-loaded with docetaxel and each of the small molecule tyrosine kinase inhibitors (STKIs) (tucatinib, neratinib, lapatinib) in HER2-positive breast cancer cells.</p><p><strong>Method: </strong>Nanoparticles were synthesized by a dispersion polymerization method using an acidlabile crosslinking agent, PEG and lactide macromonomers. They were characterized for structure (TEM), surface morphology (SEM), particle size, polydispersity index, zeta potential, and drug loading capacity. Cytotoxicity was assessed in vitro on SKBR3 and MCF7 breast cancer cell lines, with IC<sub>50</sub> values compared across formulations.</p><p><strong>Results: </strong>The nanoparticles were spherical with nanoscale sizes and negative zeta potential values. In vitro studies demonstrated enhanced antiproliferative effects of the drug-loaded nanoparticles, with synergistic activity observed between docetaxel and the STKIs. The drug concentrations were halved in combination formulations and resulted in better cytotoxicity compared to single-drug treatments, particularly against SKBR3 cells. The IC50 values were lower in SKBR3 cells than in MCF7 cells, highlighting the role of HER2 expression in the activity of TKIs.</p><p><strong>Conclusion: </strong>The pH-sensitive PLA nanoparticles effectively co-delivered docetaxel and STKIs and demonstrated enhanced efficacy and reduced drug dosages in HER2-positive breast cancer models. This study provides a foundation for further exploration of nanoparticle-based combination therapies with potential applications in treating other aggressive cancer types.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"1017-1043"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143493205","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}