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Cancer Therapy with Polymeric Nanocarriers and the Transition to Targeted Cancer Therapy: Advances and Future Directions.
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-02-04 DOI: 10.2174/0122117385350610250112112855
Panagiotis Theodosis-Nobelos, Elina N Kitiri, Melina Christou, Maria Pantelidou, Maria Rikkou-Kalourkoti

The development of targeted cancer therapies has become crucial in addressing the limitations of conventional chemotherapy, particularly its lack of specificity and severe side effects. Polymeric nanocarriers have emerged as a transformative solution, providing enhanced drug solubility, selective targeting, and controlled release of therapeutics. This review discusses recent advances in polymeric nanocarriers, emphasizing their capacity to incorporate multiple drugs and optimize delivery through both active and passive targeting strategies, and especially the transition to targeted cancer therapy through the various applied methods in the field. Mechanisms such as the enhanced permeability and retention (EPR) effect for passive targeting, and the use of ligands, peptides, and proteins for active targeting, are explored in depth. Furthermore, the potential of these nanocarriers to improve therapeutic outcomes through targeting specific cellular and subcellular sites, including the nucleus, mitochondria, and endoplasmic reticulum, is examined. These innovations pave the way for the development of safer and more effective cancer treatments with the potential to enhance clinical outcomes.

{"title":"Cancer Therapy with Polymeric Nanocarriers and the Transition to Targeted Cancer Therapy: Advances and Future Directions.","authors":"Panagiotis Theodosis-Nobelos, Elina N Kitiri, Melina Christou, Maria Pantelidou, Maria Rikkou-Kalourkoti","doi":"10.2174/0122117385350610250112112855","DOIUrl":"https://doi.org/10.2174/0122117385350610250112112855","url":null,"abstract":"<p><p>The development of targeted cancer therapies has become crucial in addressing the limitations of conventional chemotherapy, particularly its lack of specificity and severe side effects. Polymeric nanocarriers have emerged as a transformative solution, providing enhanced drug solubility, selective targeting, and controlled release of therapeutics. This review discusses recent advances in polymeric nanocarriers, emphasizing their capacity to incorporate multiple drugs and optimize delivery through both active and passive targeting strategies, and especially the transition to targeted cancer therapy through the various applied methods in the field. Mechanisms such as the enhanced permeability and retention (EPR) effect for passive targeting, and the use of ligands, peptides, and proteins for active targeting, are explored in depth. Furthermore, the potential of these nanocarriers to improve therapeutic outcomes through targeting specific cellular and subcellular sites, including the nucleus, mitochondria, and endoplasmic reticulum, is examined. These innovations pave the way for the development of safer and more effective cancer treatments with the potential to enhance clinical outcomes.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143365457","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}
引用次数: 0
Diosgenin-Loaded Silver Nanoparticles Mitigate B[a]P-Induced Lung Fibrosis Through Modulation of Oxidative Stress and Inflammatory Pathways.
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-31 DOI: 10.2174/0122117385337401250116040312
Ahmed Salah, Maiven M Edward, Mohammed A Hussein, Mohamed S Basiouny, Tamer Roshdy
<p><strong>Background: </strong>Lung fibrosis, characterized by the thickening and scarring of lung tissue, is a serious condition often triggered by environmental toxins like Benzo[a]pyrene (B[a]P). Diosgenin, a natural steroidal sapogenin found in plants such as fenugreek and wild yam, has shown potential to protect against lung damage due to its anti-inflammatory and antioxidant properties. However, its clinical application is limited by poor solubility and bioavailability.</p><p><strong>Objective: </strong>The current investigation aims at developing diosgenin-loaded silver nanoparticles (DioAgNPs) to enhance their delivery and efficacy. This study investigates the preparation, characterization, and protective effects of Dio-AgNPs against B[a]P-induced lung fibrosis in mice.</p><p><strong>Methods: </strong>Acute toxicity studies in mice were conducted to determine the lethal dose (LD50) of DioAgNPs. Sub-lethal doses (1/50 and 1/20 LD50) were selected for subsequent experiments. Mice were exposed to B[a]P to induce lung fibrosis. Dio-AgNPs were administered to assess their protective effects. Biochemical assays measured levels of total cholesterol (TC), triglycerides (TG), malondialdehyde (MDA), nuclear factor kappa B (NF-κB), interleukin-6 (IL-6), matrix metalloproteinase-2 (MMP2), and matrix metalloproteinase-12 (MMP12). Additionally, high-density lipoprotein cholesterol (HDL-C), glutathione (GSH), catalase (CAT), and glutathione peroxidase (GPx) levels were evaluated. Quantitative PCR (qPCR) was used to analyze the expression levels of lung signal transducer and activator of transcription 3 (STAT3), transforming growth factor- β1(TGF-β1), and Sirtuin 1 genes. Insilico molecular docking studies were performed to evaluate the binding affinity of diosgenin with SIRT1, STAT3, and TGF-β1 proteins, with binding energies (ΔG) calculated to predict interaction strength.</p><p><strong>Results: </strong>The synthesized Dio-AgNPs exhibited a mean diameter of 51.60±1.54 nm, a zeta potential of -19.5 mV, and encapsulation efficiency of 84.98%, confirming their stability through spectral analysis. In B[a]P-exposed mice, there was a significant elevation in TC, TG, MDA, NF-κB, IL-6, MMP2, and MMP12 levels, alongside a reduction in HDL-C, GSH, CAT, and glutathione peroxidase (GPx) levels. Additionally, lung STAT3 and TGF-β1 gene expression was upregulated, while SIRT1 gene expression was downregulated. Administration of Dio-AgNPs to B[a]P-treated mice resulted in a significant reduction in TC, TG, and HDL-C levels, improvement in lung MDA, NF-κB, IL-6, MMP2, and MMP12 levels, downregulation of lung STAT3 and TGF-β1, and upregulation of SIRT1 gene expression. In-silico molecular docking studies demonstrated strong binding affinities of diosgenin with SIRT1, STAT3, and TGF-β1 proteins, with binding energies (ΔG) of -9.7, -9.6, - 10.1, and -9.7 kcal/mol, respectively.</p><p><strong>Conclusion: </strong>This study innovatively enhances the delivery and efficac
{"title":"Diosgenin-Loaded Silver Nanoparticles Mitigate B[a]P-Induced Lung Fibrosis Through Modulation of Oxidative Stress and Inflammatory Pathways.","authors":"Ahmed Salah, Maiven M Edward, Mohammed A Hussein, Mohamed S Basiouny, Tamer Roshdy","doi":"10.2174/0122117385337401250116040312","DOIUrl":"https://doi.org/10.2174/0122117385337401250116040312","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Background: &lt;/strong&gt;Lung fibrosis, characterized by the thickening and scarring of lung tissue, is a serious condition often triggered by environmental toxins like Benzo[a]pyrene (B[a]P). Diosgenin, a natural steroidal sapogenin found in plants such as fenugreek and wild yam, has shown potential to protect against lung damage due to its anti-inflammatory and antioxidant properties. However, its clinical application is limited by poor solubility and bioavailability.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Objective: &lt;/strong&gt;The current investigation aims at developing diosgenin-loaded silver nanoparticles (DioAgNPs) to enhance their delivery and efficacy. This study investigates the preparation, characterization, and protective effects of Dio-AgNPs against B[a]P-induced lung fibrosis in mice.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;Acute toxicity studies in mice were conducted to determine the lethal dose (LD50) of DioAgNPs. Sub-lethal doses (1/50 and 1/20 LD50) were selected for subsequent experiments. Mice were exposed to B[a]P to induce lung fibrosis. Dio-AgNPs were administered to assess their protective effects. Biochemical assays measured levels of total cholesterol (TC), triglycerides (TG), malondialdehyde (MDA), nuclear factor kappa B (NF-κB), interleukin-6 (IL-6), matrix metalloproteinase-2 (MMP2), and matrix metalloproteinase-12 (MMP12). Additionally, high-density lipoprotein cholesterol (HDL-C), glutathione (GSH), catalase (CAT), and glutathione peroxidase (GPx) levels were evaluated. Quantitative PCR (qPCR) was used to analyze the expression levels of lung signal transducer and activator of transcription 3 (STAT3), transforming growth factor- β1(TGF-β1), and Sirtuin 1 genes. Insilico molecular docking studies were performed to evaluate the binding affinity of diosgenin with SIRT1, STAT3, and TGF-β1 proteins, with binding energies (ΔG) calculated to predict interaction strength.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;The synthesized Dio-AgNPs exhibited a mean diameter of 51.60±1.54 nm, a zeta potential of -19.5 mV, and encapsulation efficiency of 84.98%, confirming their stability through spectral analysis. In B[a]P-exposed mice, there was a significant elevation in TC, TG, MDA, NF-κB, IL-6, MMP2, and MMP12 levels, alongside a reduction in HDL-C, GSH, CAT, and glutathione peroxidase (GPx) levels. Additionally, lung STAT3 and TGF-β1 gene expression was upregulated, while SIRT1 gene expression was downregulated. Administration of Dio-AgNPs to B[a]P-treated mice resulted in a significant reduction in TC, TG, and HDL-C levels, improvement in lung MDA, NF-κB, IL-6, MMP2, and MMP12 levels, downregulation of lung STAT3 and TGF-β1, and upregulation of SIRT1 gene expression. In-silico molecular docking studies demonstrated strong binding affinities of diosgenin with SIRT1, STAT3, and TGF-β1 proteins, with binding energies (ΔG) of -9.7, -9.6, - 10.1, and -9.7 kcal/mol, respectively.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;This study innovatively enhances the delivery and efficac","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":"143123360","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}
引用次数: 0
Innovations in Glycosaminoglycan Delivery: Transforming Joint Health Therapies.
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-31 DOI: 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.

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引用次数: 0
Crocin and Nano-Crocin Mitigate Paraquat Hepatotoxicity by Modulating Expression of Genes Involved in Oxidative Stress and Inflammation.
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-30 DOI: 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":"&lt;p&gt;&lt;strong&gt;Introduction: &lt;/strong&gt;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.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Materials and methods: &lt;/strong&gt;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.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;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&lt;0.0001), with the nano-crocin group showing the most significant reduction (p&lt;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&lt;0.0001). Notably, nano-crocin exhibited superior protective effects, with a greater reduction in inflammatory markers and oxidative stress indicators compared to crocin (p&lt;0.01).&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Discussion: &lt;/strong&gt;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.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;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}
引用次数: 0
Metallic Nanostructures: An Updated Review on Synthesis, Stability, Safety, and Applications with Tremendous Multifunctional Opportunities.
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-27 DOI: 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}
引用次数: 0
Revolutionizing Drug Delivery: A Design Professional's Approach to Drug-loaded Transferosomal Vesicles for Transdermal Use.
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-27 DOI: 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}
引用次数: 0
Unraveling the Mysteries of Brain Cancer from Diagnosis to Treatment.
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-24 DOI: 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}
引用次数: 0
Enhancing Solubility of a BCS Class II Drug- Itraconazole by Developing and Optimizing Solid Lipid Nanoparticles using a Central Composite Design.
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-21 DOI: 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}
引用次数: 0
Polymeric Nano-discs: A Versatile Nanocarrier Platform for Delivering Topical Theranostics. 聚合纳米片:一种用于局部治疗的多功能纳米载体平台。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-17 DOI: 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.

聚合物纳米片提供了一个有前途的和适应性强的纳米载体平台,用于局部应用,包括靶向给药。这些生物相容性聚合物基的圆盘状纳米结构因其封装各种治疗药物的特殊能力而引起了人们的兴趣。将治疗和诊断结合为一个单一系统的治疗学概念是吸引人的核心。聚合物纳米片提供了精确和更少的不良反应,提供了这些药物的调节和延长释放。它们还为跟踪治疗效果提供了完美的基础。选择具有生物相容性和定制释放机制的聚合物材料是有效实现聚合物纳米片的关键。最近的临床前和临床研究已经证明了靶向治疗干预的有效性。然而,在实际应用中存在障碍和限制,需要更多的研究来充分发挥其潜力。因此,聚合物纳米片提供了控制药物释放和同时诊断能力,使其成为局部治疗的灵活可行的途径。它们的进步有机会改善治疗效果;然而,需要更多的研究来妥善解决障碍并发挥其治疗潜力。
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引用次数: 0
Preparation and In-Vitro Characterization of Solid Lipid Nanoparticles Containing Artemisinin and Curcumin. 含青蒿素和姜黄素的固体脂质纳米颗粒的制备和体外表征
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385296893240626061552
Bhagyashri Khatri, Vaishali Thakkar, Saloni Dalwadi, Avani Shah, Hardik Rana, Purvi Shah, Tejal Gandhi, Bhupendra Prajapati

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.

背景:疟疾仍然是非洲、东南亚和南美洲部分地区的一个严重公共卫生障碍,对青蒿素类复方制剂等抗疟药物的抗药性加剧了这一问题。姜黄素和青蒿素的复方制剂具有减少剂量、降低毒性、协同增效以及改善给药方式的潜力,因此前景广阔:本研究旨在利用固体脂质纳米颗粒(SLNs)提高姜黄素和青蒿素的溶解度和溶出率。由于这两种药物的水溶性差、吸收效率低、代谢和消除速度快,口服给药面临挑战:研究重点是配制和优化包裹青蒿素(ART)和姜黄素(CUR)的固体脂质纳米颗粒(SLNs)。固体脂质纳米颗粒是采用热均质法和超声波法研制而成的。使用差示扫描量热法(DSC)评估了药物与赋形剂的相容性。对脂质和表面活性剂进行了筛选,以选出合适的成分。采用 3² 全因子设计研究了脂质和表面活性剂浓度对夹持效率(%EE)和累积药物释放率(%CDR)等关键参数的影响。此外,还对夹带率、药物负载、粒度、ZETA电位和体外药物释放进行了评估:结果:采用全因子设计成功开发了青蒿素和姜黄素 SLNs,显示出药物释放受控和较高的夹持效率。优化后的纳米颗粒大小为 114.7nm,均匀度(PDI:0.261)和 zeta 电位为 -9.24 mV。青蒿素和姜黄素的 %EE 值分别为 79.1% 和 74.5%,累积药物释放率分别为 85.1% 和 80.9%。全因子设计表明,增加脂质浓度可提高释放率,而增加表面活性剂浓度则可提高药物释放率和释放率。对优化批次的稳定性研究表明,其物理和化学特性没有发生变化:该研究成功开发了青蒿素和姜黄素的固体脂质纳米颗粒(SLNs),实现了药物的可控释放、高包埋效率以及理想的粒度和均匀性。这一进步有望提高草药制剂的给药效果。
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引用次数: 0
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Pharmaceutical nanotechnology
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