Pub Date : 2024-12-10DOI: 10.2174/0122117385332757241104104727
Sampath Kumar, Mothilal Mohan
Background: The necessity for extended drug discharge to alleviate pain without adverse effects underscores the importance of innovative drug delivery systems. Achieving sustained pain relief without compromising patient safety is a critical objective in healthcare. By extending the duration of drug action while suppressing side effects, such systems offer enhanced therapeutic outcomes and improved patient quality of life.
Objective: This study endeavors to develop and appraise an innovative implantable drug delivery system by integrating NSAID-loaded gelatin microcapsules into a gelatin scaffold designed to augment drug delivery efficiency and sustain drug release.
Method: Piroxicam-loaded microcapsules with a 1:1 ratio of poly lactic acid and poly lacto glycolic acid showed smaller particle size, good yield, entrapment efficiency, and discharge. They were selected to make gelatin scaffolds with Box Behnken Design using Design Expert software for optimization. The better scaffolds were made in the form of rod-shaped sub-dermal implants. The primary focus of the investigation was the evaluation of critical parameters, specifically entrapment efficiency and drug discharge properties as dependent variables.
Results: Microcapsules with a 1:1 ratio of PLA and PLGA showed smaller particle sizes, good yield, entrapment efficiency, and discharge. Notably, the Design Expert-driven optimization yields highly favorable results. Furthermore, the scaffolds loaded with microcapsules exhibited favorable physicochemical assets, including drug discharge, for an extended period, underscoring their versatility for drug delivery.
Conclusion: By employing Design Expert software for optimization, the study demonstrates promising results, particularly in sustained pain management for arthritis, potentially improving therapeutic outcomes and patient quality of life. The study concludes that the prepared implants (holding scaffolds impregnated with piroxicam-loaded microcapsules) can be promising for relieving arthritis all day.
{"title":"Empowering Arthritis Patients: Optimized Drug Delivery through Piroxicam Microcapsule-Embedded Scaffold Implants via Box-Behnken Experimental Design.","authors":"Sampath Kumar, Mothilal Mohan","doi":"10.2174/0122117385332757241104104727","DOIUrl":"https://doi.org/10.2174/0122117385332757241104104727","url":null,"abstract":"<p><strong>Background: </strong>The necessity for extended drug discharge to alleviate pain without adverse effects underscores the importance of innovative drug delivery systems. Achieving sustained pain relief without compromising patient safety is a critical objective in healthcare. By extending the duration of drug action while suppressing side effects, such systems offer enhanced therapeutic outcomes and improved patient quality of life.</p><p><strong>Objective: </strong>This study endeavors to develop and appraise an innovative implantable drug delivery system by integrating NSAID-loaded gelatin microcapsules into a gelatin scaffold designed to augment drug delivery efficiency and sustain drug release.</p><p><strong>Method: </strong>Piroxicam-loaded microcapsules with a 1:1 ratio of poly lactic acid and poly lacto glycolic acid showed smaller particle size, good yield, entrapment efficiency, and discharge. They were selected to make gelatin scaffolds with Box Behnken Design using Design Expert software for optimization. The better scaffolds were made in the form of rod-shaped sub-dermal implants. The primary focus of the investigation was the evaluation of critical parameters, specifically entrapment efficiency and drug discharge properties as dependent variables.</p><p><strong>Results: </strong>Microcapsules with a 1:1 ratio of PLA and PLGA showed smaller particle sizes, good yield, entrapment efficiency, and discharge. Notably, the Design Expert-driven optimization yields highly favorable results. Furthermore, the scaffolds loaded with microcapsules exhibited favorable physicochemical assets, including drug discharge, for an extended period, underscoring their versatility for drug delivery.</p><p><strong>Conclusion: </strong>By employing Design Expert software for optimization, the study demonstrates promising results, particularly in sustained pain management for arthritis, potentially improving therapeutic outcomes and patient quality of life. The study concludes that the prepared implants (holding scaffolds impregnated with piroxicam-loaded microcapsules) can be promising for relieving arthritis all day.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142807689","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}
Introduction: The pharmaceutical industry has paid a lot of attention to solid lipid nanoparticles (SLN) because they show promising drug delivery vehicles.
Method: This work aimed to design and optimize the SLN of β-sitosterol, a hydrophobic drug, to improve solubility and sustained action. An ultrasonication technique after melting was used to design SLN using a randomized response surface Box-Behnken design (BBD). Network pharmacology analysis was performed to explore the interactions between genes. According to the findings, Compritol ATO 888 was the most soluble at a drug: lipid ratio of 1:3. Particle size, PDI, zeta, and entrapment efficiency (EE) were observed as 168.83nm, 0.231 -28.9 Mv, and 68.29%, respectively. The optimized formulation did not undergo any chemical changes, as depicted through DSC. The in vitro drug release investigation showed that the SLN released the drug continuously for 28 hours. Scanning Electron Microscopy (SEM) revealed homogenous, spherical particles.
Result: The antidiabetic potential of the formulation was assessed through the potential of glucose uptake by yeast, and the α-amylase inhibitory assay revealed its significant antidiabetic potential when compared with that of the standard drug metformin. The network pharmacology of β-sitosterol demonstrated gene interaction with hexokinase, phosphoglucomutases, glucose-6-phosphate dehydrogenase, hexose-6-phosphate dehydrogenase, and glutathione disulfide reductase.
Conclusion: The β-sitosterol-loaded SLN generated by BBD was found to be a potential method for improving drug solubility with sustained drug release and was found to be long-term storage stable.
固体脂质纳米颗粒(SLN)是一种很有前途的给药载体,因此受到了制药行业的广泛关注。方法:设计并优化疏水药物β-谷甾醇的单肽网,以提高其溶解度和持续作用。采用随机响应面Box-Behnken设计(BBD),采用熔融后超声技术设计SLN。网络药理学分析探讨基因间的相互作用。结果表明,当药脂比为1:3时,Compritol ATO 888最易溶。粒径为168.83nm, PDI为0.231 ~ 28.9 Mv, EE为68.29%。通过DSC显示,优化后的配方没有发生任何化学变化。体外释药研究表明,SLN可连续释药28小时。扫描电子显微镜(SEM)显示均匀的球形颗粒。结果:通过酵母葡萄糖摄取电位评价该制剂的降糖潜力,α-淀粉酶抑制实验与标准药二甲双胍比较,显示其具有显著的降糖潜力。网络药理学表明,β-谷甾醇与己糖激酶、磷酸葡萄糖酶、葡萄糖-6-磷酸脱氢酶、己糖-6-磷酸脱氢酶和谷胱甘肽二硫还原酶存在基因相互作用。结论:BBD制备的β-谷甾醇负载SLN是提高药物溶解度和缓释药物的潜在方法,且长期储存稳定。
{"title":"Network Pharmacology and Optimization of β-Sitosterol-Loaded Solid Lipid Nanoparticles Using Box-Behnken Design for Enhanced Solubility and Sustained Drug Release in Diabetes.","authors":"Ramsha Aslam, Varsha Tiwari, Prashant Upadhyay, Abhishek Tiwari","doi":"10.2174/0122117385321110241110170903","DOIUrl":"https://doi.org/10.2174/0122117385321110241110170903","url":null,"abstract":"<p><strong>Introduction: </strong>The pharmaceutical industry has paid a lot of attention to solid lipid nanoparticles (SLN) because they show promising drug delivery vehicles.</p><p><strong>Method: </strong>This work aimed to design and optimize the SLN of β-sitosterol, a hydrophobic drug, to improve solubility and sustained action. An ultrasonication technique after melting was used to design SLN using a randomized response surface Box-Behnken design (BBD). Network pharmacology analysis was performed to explore the interactions between genes. According to the findings, Compritol ATO 888 was the most soluble at a drug: lipid ratio of 1:3. Particle size, PDI, zeta, and entrapment efficiency (EE) were observed as 168.83nm, 0.231 -28.9 Mv, and 68.29%, respectively. The optimized formulation did not undergo any chemical changes, as depicted through DSC. The in vitro drug release investigation showed that the SLN released the drug continuously for 28 hours. Scanning Electron Microscopy (SEM) revealed homogenous, spherical particles.</p><p><strong>Result: </strong>The antidiabetic potential of the formulation was assessed through the potential of glucose uptake by yeast, and the α-amylase inhibitory assay revealed its significant antidiabetic potential when compared with that of the standard drug metformin. The network pharmacology of β-sitosterol demonstrated gene interaction with hexokinase, phosphoglucomutases, glucose-6-phosphate dehydrogenase, hexose-6-phosphate dehydrogenase, and glutathione disulfide reductase.</p><p><strong>Conclusion: </strong>The β-sitosterol-loaded SLN generated by BBD was found to be a potential method for improving drug solubility with sustained drug release and was found to be long-term storage stable.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142807701","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}
The exploration of hydrogel materials has gained significant attention due to the ongoing period of collaborative interdisciplinary advancements. Silk fibroin (SF) possesses remarkable attributes, such as less immunogenicity, sterilization efficacy, processability without chemical crosslinkers, excellent biocompatibility, low immunogenicity, non-toxicity, mechanical strength, thermal stability, non-carcinogenicity, and adjustable biodegradability make it a highly valuable biomaterial. Silk fibroin hydrogel (SFH), a versatile biomaterial, has garnered significant attention due to its unique properties. Its biocompatibility, tunable mechanical properties, water retention capacity, and bioactive nature offer a unique combination of features that can effectively promote tissue regeneration and enhance wound healing. The utilization of SF for hydrogel production presents a valuable opportunity to leverage natural resources and promote eco-friendly production practices. With their exceptional properties and versatile applications in biomedicine, silk protein- based hydrogels hold promise for various research fields. This review aims to discuss the potential properties and recent advancements in the application of SF-based hydrogels for preclinical skin wound healing.
{"title":"Silk Fibroin Hydrogels: Cutting-Edge Developments and Future Directions.","authors":"Govindaraj Sabarees, Ganesan Padmini Tamilarasi, Rajangam Jayaraman, Veerachamy Alagarsamy, Viswas Raja Solomon","doi":"10.2174/0122117385339249241102165029","DOIUrl":"https://doi.org/10.2174/0122117385339249241102165029","url":null,"abstract":"<p><p>The exploration of hydrogel materials has gained significant attention due to the ongoing period of collaborative interdisciplinary advancements. Silk fibroin (SF) possesses remarkable attributes, such as less immunogenicity, sterilization efficacy, processability without chemical crosslinkers, excellent biocompatibility, low immunogenicity, non-toxicity, mechanical strength, thermal stability, non-carcinogenicity, and adjustable biodegradability make it a highly valuable biomaterial. Silk fibroin hydrogel (SFH), a versatile biomaterial, has garnered significant attention due to its unique properties. Its biocompatibility, tunable mechanical properties, water retention capacity, and bioactive nature offer a unique combination of features that can effectively promote tissue regeneration and enhance wound healing. The utilization of SF for hydrogel production presents a valuable opportunity to leverage natural resources and promote eco-friendly production practices. With their exceptional properties and versatile applications in biomedicine, silk protein- based hydrogels hold promise for various research fields. This review aims to discuss the potential properties and recent advancements in the application of SF-based hydrogels for preclinical skin wound healing.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142807703","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 : 2024-12-10DOI: 10.2174/0122117385332427241112034005
Harshad Kapare, Sunil Kanadje, Ritesh Bhole
Quercetin, a natural flavonoid, is well-proven for anticancer properties in a variety of cancers. Quercetin's anticancer action is driven by its anti-inflammatory and antioxidant properties. It inhibits pro-inflammatory cytokines (e.g., TNF-α, IL-6) and suppresses NF-κB and COX-2, reducing tumor growth. Its antioxidant activity neutralizes reactive oxygen species (ROS), preventing oxidative damage that can lead to cancer. However, quercetin faces challenges such as poor solubility, bioavailability, instability, low skin penetration, rapid metabolism, and potential systemic toxicity at high doses, which limit its therapeutic application. Nanocarrier systems such as liposomes, polymeric nanoparticles (PLGA-based), solid lipid nanoparticles (SLNs), and nanoemulsions have been developed to address these issues. These formulations enhance quercetin's penetration, stability, and bioavailability, improving its effectiveness against skin cancers by promoting controlled release and targeted delivery. Nanocarriers offer a promising solution to overcome these limitations and enhance its anticancer potential.
{"title":"Quercetin Nano-formulations as a Potential Approach for Skin Cancer.","authors":"Harshad Kapare, Sunil Kanadje, Ritesh Bhole","doi":"10.2174/0122117385332427241112034005","DOIUrl":"https://doi.org/10.2174/0122117385332427241112034005","url":null,"abstract":"<p><p>Quercetin, a natural flavonoid, is well-proven for anticancer properties in a variety of cancers. Quercetin's anticancer action is driven by its anti-inflammatory and antioxidant properties. It inhibits pro-inflammatory cytokines (e.g., TNF-α, IL-6) and suppresses NF-κB and COX-2, reducing tumor growth. Its antioxidant activity neutralizes reactive oxygen species (ROS), preventing oxidative damage that can lead to cancer. However, quercetin faces challenges such as poor solubility, bioavailability, instability, low skin penetration, rapid metabolism, and potential systemic toxicity at high doses, which limit its therapeutic application. Nanocarrier systems such as liposomes, polymeric nanoparticles (PLGA-based), solid lipid nanoparticles (SLNs), and nanoemulsions have been developed to address these issues. These formulations enhance quercetin's penetration, stability, and bioavailability, improving its effectiveness against skin cancers by promoting controlled release and targeted delivery. Nanocarriers offer a promising solution to overcome these limitations and enhance its anticancer potential.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142807702","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}
Lipid-based nanocarriers have emerged as promising vehicles for the delivery of various therapeutic agents, owing to their biocompatibility, stability, and ability to encapsulate both hydrophilic and hydrophobic drugs. Among these lipid-based nanocarriers, Solid Lipid Nanoparticles (SLNs) and Nanostructured Lipid Carriers (NLCs) have gained significant attention in the field of drug delivery. This comparative review aims to provide a comprehensive analysis of SLNs and NLCs, focusing on their formulation, physicochemical properties, drug-loading capacity, stability, and drug release profiles. The review highlights the differences in preparation techniques, particle size, zeta potential, drug encapsulation efficiency, stability, drug delivery, cosmetic and personal care, and food industry applications between SLN and NLC. Furthermore, the review discusses the toxicity and safety profiles of these nanoparticles, including cytotoxicity, genotoxicity, acute toxicity, and long-term toxicity. Finally, the review identifies the potential applications, limitations, and future research directions of SLN and NLC.In summary, this comparative review provides valuable insights into the formulation, physicochemical properties, drug-loading capacity, stability, and drug release profiles of SLNs and NLCs. By understanding the similarities and differences between these lipid-based nanocarriers, researchers and pharmaceutical scientists can make informed decisions regarding the selection of the most suitable nanocarrier for specific therapeutic applications.
{"title":"Solid Lipid Nanoparticles and Nanostructured Lipid Particles: A Comparative Review on Lipid-Based Nanocarriers.","authors":"Anjali Sharma, Devkant Sharma, Pritish Kumar Panda, Niladry Shekhar Ghosh","doi":"10.2174/0122117385318686241003103005","DOIUrl":"https://doi.org/10.2174/0122117385318686241003103005","url":null,"abstract":"<p><p>Lipid-based nanocarriers have emerged as promising vehicles for the delivery of various therapeutic agents, owing to their biocompatibility, stability, and ability to encapsulate both hydrophilic and hydrophobic drugs. Among these lipid-based nanocarriers, Solid Lipid Nanoparticles (SLNs) and Nanostructured Lipid Carriers (NLCs) have gained significant attention in the field of drug delivery. This comparative review aims to provide a comprehensive analysis of SLNs and NLCs, focusing on their formulation, physicochemical properties, drug-loading capacity, stability, and drug release profiles. The review highlights the differences in preparation techniques, particle size, zeta potential, drug encapsulation efficiency, stability, drug delivery, cosmetic and personal care, and food industry applications between SLN and NLC. Furthermore, the review discusses the toxicity and safety profiles of these nanoparticles, including cytotoxicity, genotoxicity, acute toxicity, and long-term toxicity. Finally, the review identifies the potential applications, limitations, and future research directions of SLN and NLC.In summary, this comparative review provides valuable insights into the formulation, physicochemical properties, drug-loading capacity, stability, and drug release profiles of SLNs and NLCs. By understanding the similarities and differences between these lipid-based nanocarriers, researchers and pharmaceutical scientists can make informed decisions regarding the selection of the most suitable nanocarrier for specific therapeutic applications.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142807628","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 : 2024-12-10DOI: 10.2174/0122117385337841241031104420
Ali Zaheri Khosroshahi, Mohammad Ali Ghavimi, Simin Sharifi, Samin Baghban Vazirabadi, Tara Deljavanghodrati, Solmaz Maleki Dizaj
Introduction: A variety of hemostatic materials have been provided to accelerate the blood clotting process in dentistry. The purpose of this study was to investigate the biocompatibility and biodegradability of a hemostatic dental sponge containing aloe vera nanoparticles in rat animal models.
Methods and materials: Twelve adult Wistar rats in the weight range of 200 ± 30 grams and the same age range were randomly divided into two groups of test and control, and each group was divided into three subgroups of 3 days, 7 days, and 14 days. For implantation of the sponge, the animals were anesthetized with xylazine and ketamine, and a piece of the sponge was implanted under the skin at the cut site. In the control group of rats, only the skin was cut and sutured. After the specified number of days, the rats were anesthetized, and in addition to blood sampling, a tissue sample was taken from the animal's surgical site and fixed in 10% formalin. Then the samples were examined in macroscopic and microscopic conditions and finally, the obtained data were statistically analyzed.
Results: The results obtained in the present study indicated that the hemostat sponge had no side effects (biocompatible). In addition, it was completely absorbed during the 14 days of the study (biodegradable).
Conclusion: According to the characteristics of biocompatibility and biodegradability, the studied sponge can be used to control bleeding during dental surgeries or tooth extraction.
{"title":"A Biodegradable and Biocompatible Dental Hemostatic Gelatin Sponge Containing Aloe Vera Nanoparticles; Investigation in Rat Animal Model.","authors":"Ali Zaheri Khosroshahi, Mohammad Ali Ghavimi, Simin Sharifi, Samin Baghban Vazirabadi, Tara Deljavanghodrati, Solmaz Maleki Dizaj","doi":"10.2174/0122117385337841241031104420","DOIUrl":"https://doi.org/10.2174/0122117385337841241031104420","url":null,"abstract":"<p><strong>Introduction: </strong>A variety of hemostatic materials have been provided to accelerate the blood clotting process in dentistry. The purpose of this study was to investigate the biocompatibility and biodegradability of a hemostatic dental sponge containing aloe vera nanoparticles in rat animal models.</p><p><strong>Methods and materials: </strong>Twelve adult Wistar rats in the weight range of 200 ± 30 grams and the same age range were randomly divided into two groups of test and control, and each group was divided into three subgroups of 3 days, 7 days, and 14 days. For implantation of the sponge, the animals were anesthetized with xylazine and ketamine, and a piece of the sponge was implanted under the skin at the cut site. In the control group of rats, only the skin was cut and sutured. After the specified number of days, the rats were anesthetized, and in addition to blood sampling, a tissue sample was taken from the animal's surgical site and fixed in 10% formalin. Then the samples were examined in macroscopic and microscopic conditions and finally, the obtained data were statistically analyzed.</p><p><strong>Results: </strong>The results obtained in the present study indicated that the hemostat sponge had no side effects (biocompatible). In addition, it was completely absorbed during the 14 days of the study (biodegradable).</p><p><strong>Conclusion: </strong>According to the characteristics of biocompatibility and biodegradability, the studied sponge can be used to control bleeding during dental surgeries or tooth extraction.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142807673","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 : 2024-11-04DOI: 10.2174/0122117385334963241015164501
D Maheswara Reddy, Mothilal M
Objective: The study aimed to address the limitations of oral delivery and enhance the bioavailability of Cilnidipine (often prescribed as antihypertensive drug) (CND) through the development of transdermal patches containing ultra-deformable transferosomes.
Methods: CND, known for its low oral bioavailability and adverse effects, was encapsulated in transferosomes using a thin film hydration method. Seventeen formulations were made (using Box Behnken Design), varying Soya lecithin, Tween-80, and rotary evaporator's speed, and evaluated for vesicle size, polydispersity index (PDI), and entrapment efficiency (EE %). The better formulation was selected based on these parameters and incorporated into transdermal patches. Physicochemical properties, in-vitro and ex-vivo permeation, and skin irritancy studies were conducted on the patches. Pharmacokinetic studies were conducted using male Wistar albino rats.
Results: The study found that the developed transferosomal formulations had vesicle sizes between 185 nm and 401 nm, entrapment efficiency (EE%) between 63% and 92%, and zeta potential ranging from -52 mV to -20 mV. Both in-vitro and ex-vivo permeation studies showed that transferosomal formulations provided significantly better drug permeation than plain Cilnidipine patches, with increased permeation linked to higher PEG-400 concentrations. The transferosomal patches did not cause skin irritation. The optimized formulation exhibited a higher % drug release (85.7±1.5%). In pharmacokinetic studies using male Wistar albino rats, the transferosomal patch CTP-17 demonstrated a higher maximum concentration (Cmax) of 1565.068 mcg/ml and a greater area under the curve (AUC) of 13225.352 μg h/ml compared to oral administration.
Conclusion: The study concludes that the transferosomal patches of CND offer a promising approach for effective transdermal delivery, potentially improving hypertension management for prolonged periods in a controlled manner.
{"title":"Enhanced Transdermal Delivery of Cilnidpine Via Ultradeformable Vesicle Loaded Patch: Statistical Optimization, Characterization and Pharmacokinetic Assessment.","authors":"D Maheswara Reddy, Mothilal M","doi":"10.2174/0122117385334963241015164501","DOIUrl":"https://doi.org/10.2174/0122117385334963241015164501","url":null,"abstract":"<p><strong>Objective: </strong>The study aimed to address the limitations of oral delivery and enhance the bioavailability of Cilnidipine (often prescribed as antihypertensive drug) (CND) through the development of transdermal patches containing ultra-deformable transferosomes.</p><p><strong>Methods: </strong>CND, known for its low oral bioavailability and adverse effects, was encapsulated in transferosomes using a thin film hydration method. Seventeen formulations were made (using Box Behnken Design), varying Soya lecithin, Tween-80, and rotary evaporator's speed, and evaluated for vesicle size, polydispersity index (PDI), and entrapment efficiency (EE %). The better formulation was selected based on these parameters and incorporated into transdermal patches. Physicochemical properties, in-vitro and ex-vivo permeation, and skin irritancy studies were conducted on the patches. Pharmacokinetic studies were conducted using male Wistar albino rats.</p><p><strong>Results: </strong>The study found that the developed transferosomal formulations had vesicle sizes between 185 nm and 401 nm, entrapment efficiency (EE%) between 63% and 92%, and zeta potential ranging from -52 mV to -20 mV. Both in-vitro and ex-vivo permeation studies showed that transferosomal formulations provided significantly better drug permeation than plain Cilnidipine patches, with increased permeation linked to higher PEG-400 concentrations. The transferosomal patches did not cause skin irritation. The optimized formulation exhibited a higher % drug release (85.7±1.5%). In pharmacokinetic studies using male Wistar albino rats, the transferosomal patch CTP-17 demonstrated a higher maximum concentration (Cmax) of 1565.068 mcg/ml and a greater area under the curve (AUC) of 13225.352 μg h/ml compared to oral administration.</p><p><strong>Conclusion: </strong>The study concludes that the transferosomal patches of CND offer a promising approach for effective transdermal delivery, potentially improving hypertension management for prolonged periods in a controlled manner.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-11-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142583427","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 : 2024-11-04DOI: 10.2174/0122117385348551241028102256
Hussein K Alkufi, Hanan J Kassab
Background: Nimodipine (ND) is a vasodilator drug that is used for acute subarachnoid hemorrhage. It has a predominant hydrophobic property, causing low solubility and low bioavailability. Spanlastics are elastic nanovesicular systems based on non-ionic surfactants and edge activators as major components. The goal of this work is to formulate ND as spanlastic nanovesicles to improve the drug's bioavailability.
Methods: Spanlastic formulations containing ND were prepared by using the ethanol injection method. The composition of the ND formulation includes Span60 as a nonionic surfactant and Tween 20 as edge activators in different ratios. Stabilizers like Soluplus are used in some formulations and then compared with other formulations without that stabilizer. The evaluation study involved Vesicle Size (VS), PolyDispersity Index (PDI), and Entrapment Efficiency (%EE). Then, the optimized formula was subjected to an in vitro release study and zeta potential, additionally comparing the optimized formula with the formula without soluplus in the same concentration in Scanning Electron Microscopy (SEM), solubility study, Deformability Index (DI), and stability study.
Results: The results indicated a significant shift in some evaluation criteria and a non-significant change in other characterizations, including the difference in polymer ratio, sonication time, and the existence of a stabilizer. The best formula, F27, was found to have VS, PDI, %EE, and zeta potential of 125.7±0.29 nm, 0.4744±0.002, and 85.43±0.17% and -20.01 ± 0.89 mV, respectively. The photomicrographs of the prepared spanlastic revealed a more uniform and spherical spanlastic, indicating a greater capacity for continuous release. With the addition of Soluplus, the formula became more stable in one month and had a higher deformability index.
Discussion: A significant shift was observed in both VS and PDI. As the stabilizer concentration increases, VS and PDI will decrease. The non-significant shift was noted in the %EE with the presence of a stabilizer. Soluplus has the ability to spontaneously self-assemble into spherical particles. Additionally, PEG 6000, as a component of Soluplus's structure, has a tendency to form strong or tightly bound bilayers and prevent aggregation and formulation of large vesicles.
Conclusion: This study explains the accessibility of the formulation of ND as spanlastic nanovesicles by using the ethanol injection method. This spanlastic formulation contains non-ionic surfactants and edge activators (Span 40 and Tween 20) in varying ratios. To get a stable formula, Soluplus is added to prevent the development of crystals and agglomeration.
{"title":"Soluplus-Stabilized Nimodipine-Entrapped Spanlastic Formulations Prepared with Edge Activator (Tween20): Comparative Physicochemical Evaluation.","authors":"Hussein K Alkufi, Hanan J Kassab","doi":"10.2174/0122117385348551241028102256","DOIUrl":"https://doi.org/10.2174/0122117385348551241028102256","url":null,"abstract":"<p><strong>Background: </strong>Nimodipine (ND) is a vasodilator drug that is used for acute subarachnoid hemorrhage. It has a predominant hydrophobic property, causing low solubility and low bioavailability. Spanlastics are elastic nanovesicular systems based on non-ionic surfactants and edge activators as major components. The goal of this work is to formulate ND as spanlastic nanovesicles to improve the drug's bioavailability.</p><p><strong>Methods: </strong>Spanlastic formulations containing ND were prepared by using the ethanol injection method. The composition of the ND formulation includes Span60 as a nonionic surfactant and Tween 20 as edge activators in different ratios. Stabilizers like Soluplus are used in some formulations and then compared with other formulations without that stabilizer. The evaluation study involved Vesicle Size (VS), PolyDispersity Index (PDI), and Entrapment Efficiency (%EE). Then, the optimized formula was subjected to an in vitro release study and zeta potential, additionally comparing the optimized formula with the formula without soluplus in the same concentration in Scanning Electron Microscopy (SEM), solubility study, Deformability Index (DI), and stability study.</p><p><strong>Results: </strong>The results indicated a significant shift in some evaluation criteria and a non-significant change in other characterizations, including the difference in polymer ratio, sonication time, and the existence of a stabilizer. The best formula, F27, was found to have VS, PDI, %EE, and zeta potential of 125.7±0.29 nm, 0.4744±0.002, and 85.43±0.17% and -20.01 ± 0.89 mV, respectively. The photomicrographs of the prepared spanlastic revealed a more uniform and spherical spanlastic, indicating a greater capacity for continuous release. With the addition of Soluplus, the formula became more stable in one month and had a higher deformability index.</p><p><strong>Discussion: </strong>A significant shift was observed in both VS and PDI. As the stabilizer concentration increases, VS and PDI will decrease. The non-significant shift was noted in the %EE with the presence of a stabilizer. Soluplus has the ability to spontaneously self-assemble into spherical particles. Additionally, PEG 6000, as a component of Soluplus's structure, has a tendency to form strong or tightly bound bilayers and prevent aggregation and formulation of large vesicles.</p><p><strong>Conclusion: </strong>This study explains the accessibility of the formulation of ND as spanlastic nanovesicles by using the ethanol injection method. This spanlastic formulation contains non-ionic surfactants and edge activators (Span 40 and Tween 20) in varying ratios. To get a stable formula, Soluplus is added to prevent the development of crystals and agglomeration.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-11-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142583435","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 : 2024-11-01DOI: 10.2174/0122117385313643241010060814
Vishveshwaraiah C K, Kirankumar G B, Harshitha M, Madhu B K
Nanoparticles are a significant topic due to their applications in various fields, including biology, optics, catalysis, pharmaceutics, health, agriculture, and industry, with biosynthesis processes being quick, easy, and environmentally friendly. Due to their applications across multiple industries, silver nanoparticles, or AgNPs, have become the most desired nanoparticles with the recent development of nanotechnology. The physical, chemical, and biological characteristics of AgNPs are being studied. These characteristics are crucial for limiting the hazards associated with silver nanoparticles while optimizing their potential applications in many fields. A higher degree of toxicity in both the environment and living things could arise from the increasing use of silver nanoparticles in the product. Silver nanoparticles find application in wound care, anti-infective therapy, food, pharmaceutical, and cosmetic industries. As antioxidant, antiviral, anticancer, antifungal, antiinflammatory, and microbiological agents, silver nanoparticles are widely used. Not only must the particles be nanoscale in order for silver nanoparticles to be present, but their production must also be simple and inexpensive to achieve. This paper aims to review the different methods of synthesis of silver nanoparticles, properties, characterization, and their applications. In specific, several chemical and green synthesis approaches for synthesising silver nanoparticles have been discussed. The morphology, size, thermal properties, toxicity properties, electrical properties, catalytic properties, and applications of silver nanoparticles are focused. The main focus is on the effective and efficient synthesis of pure silver nanoparticles and their potential applications.
{"title":"A Review on Silver Nanoparticles: Synthesis Approaches, Properties, Characterization and Applications.","authors":"Vishveshwaraiah C K, Kirankumar G B, Harshitha M, Madhu B K","doi":"10.2174/0122117385313643241010060814","DOIUrl":"https://doi.org/10.2174/0122117385313643241010060814","url":null,"abstract":"<p><p>Nanoparticles are a significant topic due to their applications in various fields, including biology, optics, catalysis, pharmaceutics, health, agriculture, and industry, with biosynthesis processes being quick, easy, and environmentally friendly. Due to their applications across multiple industries, silver nanoparticles, or AgNPs, have become the most desired nanoparticles with the recent development of nanotechnology. The physical, chemical, and biological characteristics of AgNPs are being studied. These characteristics are crucial for limiting the hazards associated with silver nanoparticles while optimizing their potential applications in many fields. A higher degree of toxicity in both the environment and living things could arise from the increasing use of silver nanoparticles in the product. Silver nanoparticles find application in wound care, anti-infective therapy, food, pharmaceutical, and cosmetic industries. As antioxidant, antiviral, anticancer, antifungal, antiinflammatory, and microbiological agents, silver nanoparticles are widely used. Not only must the particles be nanoscale in order for silver nanoparticles to be present, but their production must also be simple and inexpensive to achieve. This paper aims to review the different methods of synthesis of silver nanoparticles, properties, characterization, and their applications. In specific, several chemical and green synthesis approaches for synthesising silver nanoparticles have been discussed. The morphology, size, thermal properties, toxicity properties, electrical properties, catalytic properties, and applications of silver nanoparticles are focused. The main focus is on the effective and efficient synthesis of pure silver nanoparticles and their potential applications.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142569251","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 : 2024-10-24DOI: 10.2174/0122117385317956241008074909
Sandhya S, Jayatheertha S Lokapur, Prakash S Goudanavar
The implementation of several innovative drug delivery technologies has made medication distribution more focused and managed in recent years. These days, a vesicular drug delivery system defines the rate of distribution and the site of action in order to improve the action and increase patient compliance; there are various kinds of newly developed vesicular drug delivery systems, including transferosomes, niosomes, aquasomes, ufasomes, pharmacosomes, and phytosomes. Ufasomes are unsaturated fatty acid vesicles with a limited pH range of 7 to 9. They are a suspension of closed lipid bilayers made of fatty acids and their ionized species. The hydrocarbon tails of fatty acid molecules are oriented toward the membrane's inner core, and their carboxyl groups are in contact with water. The two fatty acids that are most frequently employed in the ufasomes' manufacturing process are oleic and linoleic acids. It is a common practice to produce fatty acid vesicles via the thin film hydration process. The manufacture of stable ufasomes is mostly dependent on the choice of fatty acids, amount of cholesterol, pH range, buffer, etc. This article goes into additional detail regarding unsaturated fatty acids' characteristics, benefits, and drawbacks.
{"title":"A Comprehensive Review on Oleic Acid Vesicles: A Novel Approach to Drug Delivery.","authors":"Sandhya S, Jayatheertha S Lokapur, Prakash S Goudanavar","doi":"10.2174/0122117385317956241008074909","DOIUrl":"https://doi.org/10.2174/0122117385317956241008074909","url":null,"abstract":"<p><p>The implementation of several innovative drug delivery technologies has made medication distribution more focused and managed in recent years. These days, a vesicular drug delivery system defines the rate of distribution and the site of action in order to improve the action and increase patient compliance; there are various kinds of newly developed vesicular drug delivery systems, including transferosomes, niosomes, aquasomes, ufasomes, pharmacosomes, and phytosomes. Ufasomes are unsaturated fatty acid vesicles with a limited pH range of 7 to 9. They are a suspension of closed lipid bilayers made of fatty acids and their ionized species. The hydrocarbon tails of fatty acid molecules are oriented toward the membrane's inner core, and their carboxyl groups are in contact with water. The two fatty acids that are most frequently employed in the ufasomes' manufacturing process are oleic and linoleic acids. It is a common practice to produce fatty acid vesicles via the thin film hydration process. The manufacture of stable ufasomes is mostly dependent on the choice of fatty acids, amount of cholesterol, pH range, buffer, etc. This article goes into additional detail regarding unsaturated fatty acids' characteristics, benefits, and drawbacks.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142505462","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}