Pub Date : 2024-08-12DOI: 10.2174/0115672018328954240801110200
Dyala M Khasawneh, Rami J Oweis, Mo'tasem Alsmadi
Bacterial skin and soft tissue infections (SSTIs) are widespread microbic invasions of the skin and deeper tissues. Topical drug delivery systems are the most favored administration pathway when treating SSTIs. This is down to their minimal risk of inducing systemic adverse events, reduced development of bacterial resistance, and ease of application. However, they have several drawbacks, including the lack of control over the drug release profile, skin irritations, and the limited permeability of certain compounds through the skin. To address these limitations, several nanocarrier systems were developed, with nanoliposomes standing out as the leading delivery system for the topical management of SSTIs. Despite considerable research into liposomes over the past decade, there remains a gap in detailed knowledge about designing these carriers specifically for SSTIs. Consequently, there is a pressing need for comprehensive research that focuses on the use of nanoliposomes for SSTIs and offers an extensive understanding of both SSTIs and liposomal formulations. This review explores bacterial SSTIs, covering their epidemiology, classification, microbiology, and management. It emphasizes the contribution of liposome-based nanovesicles in enhancing the local administration of antibiotics and natural antibacterial compounds for SSTI management. It also delves into the effects of liposomal formulation changes on the disease therapeutic outcomes. Additionally, it provides a guide for aligning the characteristics of the liposomes with the infection types, depths, properties, and causative agents. This signifies a substantial leap forward in the domains of drug design, development, and delivery.
{"title":"A Comprehensive Analysis of Liposomal-Based Nanocarriers for Treating Skin and Soft Tissue Infection.","authors":"Dyala M Khasawneh, Rami J Oweis, Mo'tasem Alsmadi","doi":"10.2174/0115672018328954240801110200","DOIUrl":"https://doi.org/10.2174/0115672018328954240801110200","url":null,"abstract":"<p><p>Bacterial skin and soft tissue infections (SSTIs) are widespread microbic invasions of the skin and deeper tissues. Topical drug delivery systems are the most favored administration pathway when treating SSTIs. This is down to their minimal risk of inducing systemic adverse events, reduced development of bacterial resistance, and ease of application. However, they have several drawbacks, including the lack of control over the drug release profile, skin irritations, and the limited permeability of certain compounds through the skin. To address these limitations, several nanocarrier systems were developed, with nanoliposomes standing out as the leading delivery system for the topical management of SSTIs. Despite considerable research into liposomes over the past decade, there remains a gap in detailed knowledge about designing these carriers specifically for SSTIs. Consequently, there is a pressing need for comprehensive research that focuses on the use of nanoliposomes for SSTIs and offers an extensive understanding of both SSTIs and liposomal formulations. This review explores bacterial SSTIs, covering their epidemiology, classification, microbiology, and management. It emphasizes the contribution of liposome-based nanovesicles in enhancing the local administration of antibiotics and natural antibacterial compounds for SSTI management. It also delves into the effects of liposomal formulation changes on the disease therapeutic outcomes. Additionally, it provides a guide for aligning the characteristics of the liposomes with the infection types, depths, properties, and causative agents. This signifies a substantial leap forward in the domains of drug design, development, and delivery.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-08-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141972519","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 : 2024-07-29DOI: 10.2174/0115672018309370240708113038
Muhammad Hadi Sultan, Yosif Almoshari, Syam Mohan, Mohamed Ahmed Al-Kasim, Hamad S Alyami, Mohammad Azam Ansari, Mohammad Intakhab Alam
Background: Cancer treatment often involves the use of potent antineoplastic drugs like Capecitabine [CAP], which can lead to serious toxicities. There is a need for dosage forms to manage these toxicities that can deliver the medication effectively to the target site while maintaining therapeutic efficacy at lower doses. To achieve the aforesaid objective, NLC containing capecitabine [NANOBIN] was prepared and evaluated. Different formulations of NANOBIN, denoted as CaTS, CaT1S, CaT2S, CaTS1, and CaTS2, were designed and evaluated to improve drug delivery and therapeutic outcomes.
Methods: The NANOBIN formulations were prepared using the hot homogenization method. The characterization of these formulations was conducted based on various parameters such as particle size, Polydispersity Index [PDI], Zeta Potential [ZP], Transmission Electron Microscopy [TEM] imaging, and Encapsulation Efficiency [EE]. In vitro evaluations included stability testing, release studies to assess drug release kinetics, and a cytotoxicity assay [MTT assay] to evaluate the efficacy of these formulations against human breast cancer cells [MCF-7].
Results: The characterization results revealed that all NANOBIN formulations exhibited particle sizes ranging from 65 to 193 nm, PDI values within the range of 0.26-0.37, ZP values between 46.47 to 61.87 mV [-ve], and high EE percentages ranging from 94.121% to 96.64%. Furthermore, all NANOBIN formulations demonstrated sustained and slow-release profiles of CAP. The MTT assay showed that the NANOBINs exhibited significantly enhanced cytotoxic efficacy, approximately 10 times greater than free CAP when tested on MCF-7 cells. These findings indicate the potential of NANOBINs to deliver CAP effectively to the target site, enabling prolonged drug availability and enhanced therapeutic effects at lower doses.
Conclusion: The study demonstrates that NANOBINs can effectively deliver CAP to target sites, prolonging drug exposure and enhancing therapeutic efficacy while reducing the required dose. Further studies are necessary to validate these findings and establish NANOBINs as a preferred treatment option for cancer therapy.
{"title":"Capecitabine-loaded NLC for Breast Cancer Treatment: Preparation, Characterization, and In vitro Evaluation.","authors":"Muhammad Hadi Sultan, Yosif Almoshari, Syam Mohan, Mohamed Ahmed Al-Kasim, Hamad S Alyami, Mohammad Azam Ansari, Mohammad Intakhab Alam","doi":"10.2174/0115672018309370240708113038","DOIUrl":"10.2174/0115672018309370240708113038","url":null,"abstract":"<p><strong>Background: </strong>Cancer treatment often involves the use of potent antineoplastic drugs like Capecitabine [CAP], which can lead to serious toxicities. There is a need for dosage forms to manage these toxicities that can deliver the medication effectively to the target site while maintaining therapeutic efficacy at lower doses. To achieve the aforesaid objective, NLC containing capecitabine [NANOBIN] was prepared and evaluated. Different formulations of NANOBIN, denoted as CaTS, CaT1S, CaT2S, CaTS1, and CaTS2, were designed and evaluated to improve drug delivery and therapeutic outcomes.</p><p><strong>Methods: </strong>The NANOBIN formulations were prepared using the hot homogenization method. The characterization of these formulations was conducted based on various parameters such as particle size, Polydispersity Index [PDI], Zeta Potential [ZP], Transmission Electron Microscopy [TEM] imaging, and Encapsulation Efficiency [EE]. In vitro evaluations included stability testing, release studies to assess drug release kinetics, and a cytotoxicity assay [MTT assay] to evaluate the efficacy of these formulations against human breast cancer cells [MCF-7].</p><p><strong>Results: </strong>The characterization results revealed that all NANOBIN formulations exhibited particle sizes ranging from 65 to 193 nm, PDI values within the range of 0.26-0.37, ZP values between 46.47 to 61.87 mV [-ve], and high EE percentages ranging from 94.121% to 96.64%. Furthermore, all NANOBIN formulations demonstrated sustained and slow-release profiles of CAP. The MTT assay showed that the NANOBINs exhibited significantly enhanced cytotoxic efficacy, approximately 10 times greater than free CAP when tested on MCF-7 cells. These findings indicate the potential of NANOBINs to deliver CAP effectively to the target site, enabling prolonged drug availability and enhanced therapeutic effects at lower doses.</p><p><strong>Conclusion: </strong>The study demonstrates that NANOBINs can effectively deliver CAP to target sites, prolonging drug exposure and enhancing therapeutic efficacy while reducing the required dose. Further studies are necessary to validate these findings and establish NANOBINs as a preferred treatment option for cancer therapy.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141794474","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}
Iron Deficiency Anaemia (IDA) is a prevalent global health issue characterized by inadequate iron levels in the body, leading to impaired red blood cell production and subsequent anaemia. Traditional treatment approaches for IDA, such as oral iron supplementation, often encounter challenges related to poor compliance, gastrointestinal side effects, and variable absorption rates. As a result, there is a growing interest in exploring novel drug delivery systems to enhance iron therapy efficacy and patient outcomes. This review discusses recent advances in IDA management, focusing on developing and utilizing innovative drug delivery systems for iron supplementation. Various strategies, including nanoformulations, microparticles, liposomes, and hydrogels, are explored for their potential to improve iron bioavailability, reduce adverse effects, and optimize therapeutic outcomes. Furthermore, promising strategies for the future management of IDA are explored, including the utilization of advanced technologies such as targeted drug delivery systems, controlled release mechanisms, and combination therapies. The integration of these novel drug delivery systems with advancements in diagnostics, personalized medicine, and patient-centered care holds great potential to revolutionize the management of IDA and improve the quality of life for individuals affected by this condition.
缺铁性贫血(IDA)是全球普遍存在的健康问题,其特点是体内铁含量不足,导致红细胞生成障碍,进而引发贫血。传统的 IDA 治疗方法(如口服铁质补充剂)经常遇到依从性差、胃肠道副作用和吸收率不稳定等难题。因此,人们对探索新型给药系统以提高铁治疗效果和患者预后的兴趣与日俱增。本综述讨论了 IDA 治疗的最新进展,重点是开发和利用创新的给药系统来补充铁剂。文中探讨了各种策略,包括纳米制剂、微颗粒、脂质体和水凝胶,以了解它们在提高铁的生物利用度、减少不良反应和优化治疗效果方面的潜力。此外,还探讨了未来治疗 IDA 的可行策略,包括利用靶向给药系统、控释机制和联合疗法等先进技术。将这些新型给药系统与诊断、个性化医疗和以患者为中心的护理等方面的进步相结合,有望彻底改变 IDA 的治疗方法,并提高受此疾病影响的患者的生活质量。
{"title":"Advances in Iron Deficiency Anaemia Management: Exploring Novel Drug Delivery Systems and Future Perspectives.","authors":"Muskan Saini, Karan Trehan, Shubham Thakur, Anuj Modi, Subheet Kumar Jain","doi":"10.2174/0115672018300804240426070552","DOIUrl":"https://doi.org/10.2174/0115672018300804240426070552","url":null,"abstract":"<p><p>Iron Deficiency Anaemia (IDA) is a prevalent global health issue characterized by inadequate iron levels in the body, leading to impaired red blood cell production and subsequent anaemia. Traditional treatment approaches for IDA, such as oral iron supplementation, often encounter challenges related to poor compliance, gastrointestinal side effects, and variable absorption rates. As a result, there is a growing interest in exploring novel drug delivery systems to enhance iron therapy efficacy and patient outcomes. This review discusses recent advances in IDA management, focusing on developing and utilizing innovative drug delivery systems for iron supplementation. Various strategies, including nanoformulations, microparticles, liposomes, and hydrogels, are explored for their potential to improve iron bioavailability, reduce adverse effects, and optimize therapeutic outcomes. Furthermore, promising strategies for the future management of IDA are explored, including the utilization of advanced technologies such as targeted drug delivery systems, controlled release mechanisms, and combination therapies. The integration of these novel drug delivery systems with advancements in diagnostics, personalized medicine, and patient-centered care holds great potential to revolutionize the management of IDA and improve the quality of life for individuals affected by this condition.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141790735","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: Polymer prodrug nanoparticles have become an emerging drug delivery system in cancer therapy due to their high drug loading. However, their poor drug release and lack of tumor cell targeting limit their clinical application.
Objective: This study aimed to prepare targeted and reduction-reactive polyprodrug nanocarriers based on curcumin (CUR) for co-delivery of doxorubicin (DOX), labeled as DOX/HAPCS NPs, and to investigate their anticancer activity.
Methods: The polymer was synthesized and characterized by chemical method. The drug loading and drug release behavior of DOX and CUR in polymer nanoparticles were determined. Moreover, the antitumor effects of polymer nanoparticles were evaluated using an MTT experiment and tumor inhibition experiment, and the synergistic effect of co-delivered DOX and CUR was explored.
Results: The particle size of DOX/HAPCS NPs was 152.5nm, and the potential was about -26.74 mV. The drug-carrying capacity of DOX and CUR was about 7.56% and 34.75%, respectively, indicating high drug-carrying capacity and good stability. DOX and CUR released over 90% within 24 hours in the tumor environment. Compared with free DOX, DOX/HAPCS NPs demonstrated significantly enhanced cell and tumor inhibitory effects (P< 0.05) in vivo and in vitro and changed drug distribution to avoid toxic side effects on normal tissues. The combined index showed that DOX and CUR showed synergistic anticancer effects at a set ratio.
Conclusion: The prepared reduction-responsive targeted polymer nanomedical DOX/HAPCS NPs exhibited a synergistic anti-cancer effect, with high drug loading capacity and the ability to release drugs in proportion, making it a promising polymer nanoparticle drug delivery system.
导言:聚合物原药纳米颗粒因其高载药量而成为癌症治疗中一种新兴的给药系统。然而,其药物释放性差和缺乏肿瘤细胞靶向性限制了其临床应用:本研究旨在制备基于姜黄素(CUR)的靶向性还原反应聚药纳米载体,用于联合递送多柔比星(DOX),标记为 DOX/HAPCS NPs,并研究其抗癌活性:方法:采用化学方法合成并表征了聚合物。方法:采用化学方法合成了聚合物并对其进行了表征,测定了聚合物纳米颗粒中 DOX 和 CUR 的载药量和药物释放行为。此外,还利用 MTT 实验和肿瘤抑制实验评估了聚合物纳米颗粒的抗肿瘤效果,并探讨了 DOX 和 CUR 共给药的协同效应:结果:DOX/HAPCS NPs的粒径为152.5nm,电位约为-26.74 mV。DOX和CUR的载药量分别约为7.56%和34.75%,显示出较高的载药量和良好的稳定性。DOX和CUR在肿瘤环境中24小时内的释放率超过90%。与游离 DOX 相比,DOX/HAPCS NPs 在体内和体外对细胞和肿瘤的抑制作用明显增强(P< 0.05),并改变了药物分布,避免了对正常组织的毒副作用。综合指标显示,DOX 和 CUR 在一定比例下具有协同抗癌作用:制备的还原响应靶向聚合物纳米药物 DOX/HAPCS NPs 具有协同抗癌作用,载药量大,能按比例释放药物,是一种很有前景的聚合物纳米颗粒给药系统。
{"title":"Reduction-Responsive Polyprodrug Nanoplatform Based on Curcumin for Tumor-Targeted Therapy.","authors":"Ziyi Zhang, Jinyuan Tian, Xiaoqing Xu, Wei Shi, Yajuan Qi, Zhanjun Liu","doi":"10.2174/0115672018314506240723080113","DOIUrl":"https://doi.org/10.2174/0115672018314506240723080113","url":null,"abstract":"<p><strong>Introduction: </strong>Polymer prodrug nanoparticles have become an emerging drug delivery system in cancer therapy due to their high drug loading. However, their poor drug release and lack of tumor cell targeting limit their clinical application.</p><p><strong>Objective: </strong>This study aimed to prepare targeted and reduction-reactive polyprodrug nanocarriers based on curcumin (CUR) for co-delivery of doxorubicin (DOX), labeled as DOX/HAPCS NPs, and to investigate their anticancer activity.</p><p><strong>Methods: </strong>The polymer was synthesized and characterized by chemical method. The drug loading and drug release behavior of DOX and CUR in polymer nanoparticles were determined. Moreover, the antitumor effects of polymer nanoparticles were evaluated using an MTT experiment and tumor inhibition experiment, and the synergistic effect of co-delivered DOX and CUR was explored.</p><p><strong>Results: </strong>The particle size of DOX/HAPCS NPs was 152.5nm, and the potential was about -26.74 mV. The drug-carrying capacity of DOX and CUR was about 7.56% and 34.75%, respectively, indicating high drug-carrying capacity and good stability. DOX and CUR released over 90% within 24 hours in the tumor environment. Compared with free DOX, DOX/HAPCS NPs demonstrated significantly enhanced cell and tumor inhibitory effects (P< 0.05) in vivo and in vitro and changed drug distribution to avoid toxic side effects on normal tissues. The combined index showed that DOX and CUR showed synergistic anticancer effects at a set ratio.</p><p><strong>Conclusion: </strong>The prepared reduction-responsive targeted polymer nanomedical DOX/HAPCS NPs exhibited a synergistic anti-cancer effect, with high drug loading capacity and the ability to release drugs in proportion, making it a promising polymer nanoparticle drug delivery system.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141763744","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 : 2024-07-18DOI: 10.2174/0115672018315676240715065750
Rui Gao, Qunbin Fan, Saeed Rohani
Introduction: Obesity has become a pressing global health crisis, reaching alarming proportions and bearing significant consequences for public health on a global scale.
Aim: In this research, chitosan nanoparticles were employed to encapsulate ginger extract, and the impact of this formulation on lipid metabolism and obesity was investigated using a rat model.
Methods: In vitro experiments, encompassing assessments of cell viability, microstructure, anti-inflammatory activity, and release dynamics, were conducted to comprehensively evaluate the nanoformulation. The study extended to examining the potential anti-obesity efficacy of the developed nanoformulation in rats induced with obesity through a high-fat diet.
Results: In vitro findings affirmed the safety of the carriers and revealed their robust anti-inflammatory properties. The average particle size for ginger-loaded and ginger-free chitosan nanoparticles was measured to be 458.92 ± 139.35 nm and 466.29 ± 142.71 nm, respectively. The in vivo investigation demonstrated the dose-dependent effects of ginger extract-loaded chitosan nanoparticles, manifesting in a reduction of obesity and improvement in liver function.
Conclusion: These promising results suggest that the developed nanoformulation could be considered a viable therapeutic option for individuals struggling with obesity.
{"title":"Ginger Extract-Loaded Chitosan Nanoparticles: Investigating their Impact on Lipid Metabolism and Obesity in a Rat Model through In vitro and In vivo Analysis.","authors":"Rui Gao, Qunbin Fan, Saeed Rohani","doi":"10.2174/0115672018315676240715065750","DOIUrl":"https://doi.org/10.2174/0115672018315676240715065750","url":null,"abstract":"<p><strong>Introduction: </strong>Obesity has become a pressing global health crisis, reaching alarming proportions and bearing significant consequences for public health on a global scale.</p><p><strong>Aim: </strong>In this research, chitosan nanoparticles were employed to encapsulate ginger extract, and the impact of this formulation on lipid metabolism and obesity was investigated using a rat model.</p><p><strong>Methods: </strong>In vitro experiments, encompassing assessments of cell viability, microstructure, anti-inflammatory activity, and release dynamics, were conducted to comprehensively evaluate the nanoformulation. The study extended to examining the potential anti-obesity efficacy of the developed nanoformulation in rats induced with obesity through a high-fat diet.</p><p><strong>Results: </strong>In vitro findings affirmed the safety of the carriers and revealed their robust anti-inflammatory properties. The average particle size for ginger-loaded and ginger-free chitosan nanoparticles was measured to be 458.92 ± 139.35 nm and 466.29 ± 142.71 nm, respectively. The in vivo investigation demonstrated the dose-dependent effects of ginger extract-loaded chitosan nanoparticles, manifesting in a reduction of obesity and improvement in liver function.</p><p><strong>Conclusion: </strong>These promising results suggest that the developed nanoformulation could be considered a viable therapeutic option for individuals struggling with obesity.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141736274","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}
Transdermal Drug Delivery Systems (TDDS) have gained attention as a viable substitute for traditional drug administration methods because of their controlled release capabilities and non-invasive design. Microneedles are a new and effective technology that has attracted a lot of attention recently to enhance the capabilities of TDDS further. The study on microneedles and their potential to improve transdermal medication delivery is thoroughly reviewed in this review article. The study initiates by clarifying the difficulties linked to traditional medication delivery techniques and the benefits provided by transdermal channels. The article then explores the development of microneedle technology, outlining the several kinds of microneedles-solid, hollow, and dissolving-as well as their uses. Because of their special capacity to penetrate the skin's protective layer painlessly and their ability to distribute drugs precisely and precisely, microneedles are a highly useful instrument in pharmaceutical research. The materials, geometry, and manufacturing processes that affect the design and creation of microneedles are critically analyzed and presented. The manuscript delves into the latest developments in microneedle technology, encompassing the utilization of biodegradable polymers, smart materials, and sensing components for in-the-- moment monitoring. This analysis concludes by highlighting the noteworthy advancements in the field of microneedles and their potential to transform transdermal drug delivery systems. This thorough knowledge seeks to further the current discussion in pharmaceutical research, encouraging creativity and opening the door for the creation of safer, more effective drug delivery systems.
{"title":"Microneedles: An Efficient Technique to Increase Transdermal Drug Delivery System.","authors":"Sanjit Kr Roy, Kazi Asraf Ali, Mahua Biswas, Abhijit Dey, Amlan Bishal, Abhradeep Kuiry","doi":"10.2174/0115672018301931240624072453","DOIUrl":"https://doi.org/10.2174/0115672018301931240624072453","url":null,"abstract":"<p><p>Transdermal Drug Delivery Systems (TDDS) have gained attention as a viable substitute for traditional drug administration methods because of their controlled release capabilities and non-invasive design. Microneedles are a new and effective technology that has attracted a lot of attention recently to enhance the capabilities of TDDS further. The study on microneedles and their potential to improve transdermal medication delivery is thoroughly reviewed in this review article. The study initiates by clarifying the difficulties linked to traditional medication delivery techniques and the benefits provided by transdermal channels. The article then explores the development of microneedle technology, outlining the several kinds of microneedles-solid, hollow, and dissolving-as well as their uses. Because of their special capacity to penetrate the skin's protective layer painlessly and their ability to distribute drugs precisely and precisely, microneedles are a highly useful instrument in pharmaceutical research. The materials, geometry, and manufacturing processes that affect the design and creation of microneedles are critically analyzed and presented. The manuscript delves into the latest developments in microneedle technology, encompassing the utilization of biodegradable polymers, smart materials, and sensing components for in-the-- moment monitoring. This analysis concludes by highlighting the noteworthy advancements in the field of microneedles and their potential to transform transdermal drug delivery systems. This thorough knowledge seeks to further the current discussion in pharmaceutical research, encouraging creativity and opening the door for the creation of safer, more effective drug delivery systems.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141736275","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 eye is a most delicate organ protected by several complex biological barriers that are static and dynamic. The presence of these ocular barriers retards drug absorption from topically applied dosage forms at the conjunctival sac. The efficient topical delivery of the drug into the globe is more difficult to achieve and there is a need to develop a topical formulation that may reduce the use of injections and increase patient compliance with decreased frequency of administration. In the advancements of research in nanotechnology, nanoemulsions can be used as biocompatible carriers to deliver the drug to the ocular cavity. The lipophilic globules can increase the solubility of hydrophobic cargos which provides increased permeation ability and ocular bioavailability which can sustain drug release and corneal retention. Because of their small size, these formulations do not cause blurring of vision. Nanoemulsions (NEs) over the past decade have been used to treat several ocular diseases in the anterior eye segment. This review summarizes the economic burden, pathology of ocular diseases, formulation considerations for ocular formulations, and recent advances of these NEs as effective carriers for ocular drug delivery highlighting their performance in pre-clinical studies.
{"title":"Expanding Arsenal against Ocular Diseases through Nanoemulsion: Success So Far and the Road Ahead.","authors":"Bala Vikash, Shashi, Narendra Kumar Pandey, Bimlesh Kumar, Sheetu Wadhwa, Ritu Gupta, Umesh Goutam, Amit Mittal, Dileep Singh Baghel, Sachin Kumar Singh, Saurabh Singh","doi":"10.2174/0115672018286288240705064730","DOIUrl":"https://doi.org/10.2174/0115672018286288240705064730","url":null,"abstract":"<p><p>The eye is a most delicate organ protected by several complex biological barriers that are static and dynamic. The presence of these ocular barriers retards drug absorption from topically applied dosage forms at the conjunctival sac. The efficient topical delivery of the drug into the globe is more difficult to achieve and there is a need to develop a topical formulation that may reduce the use of injections and increase patient compliance with decreased frequency of administration. In the advancements of research in nanotechnology, nanoemulsions can be used as biocompatible carriers to deliver the drug to the ocular cavity. The lipophilic globules can increase the solubility of hydrophobic cargos which provides increased permeation ability and ocular bioavailability which can sustain drug release and corneal retention. Because of their small size, these formulations do not cause blurring of vision. Nanoemulsions (NEs) over the past decade have been used to treat several ocular diseases in the anterior eye segment. This review summarizes the economic burden, pathology of ocular diseases, formulation considerations for ocular formulations, and recent advances of these NEs as effective carriers for ocular drug delivery highlighting their performance in pre-clinical studies.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141636387","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: The therapeutic effect of NS oil in mild to moderate psoriasis is limited owing to low play load of thymoquinone ( < 15 %w/w), irritation, dripping, low viscosity and thus, less contact time on the lesions.
Aims: This study aimed at developing and characterizing the ethanolic vesicular hydrogel system of Nigella sativa (NS) oil (NS EV hydrogel) for the enhancement of anti-psoriatic activity.
Objective: The objective of this study was to develop NS EV hydrogel and evaluate its anti-psoriatic activity.
Methods: The identification and quantification of TQ content in different NS seed extracts and marketed oil were measured by an HPTLC method using n-hexane and ethyl acetate as solvent systems. Preparation of ethanolic vesicles (EVs) was performed by solvent injection method, while its antipsoriatic activity was evaluated employing an Imiquad (IMQ)-induced plaque psoriasis animal model.
Results: A compact HPTLC band was obtained for TQ at an Rf value of 0.651. The calibration plot was linear in the range of 1-10 μg/spot, and the correlation coefficient of 0.990 was indicative of good linear dependence of peak area on concentration. From the different NS sources, the high TQ content was obtained in the marketed cold press oil, i.e., 1.45±0.08mg/ml. Out of various NS oilloaded EVs, the F6 formulation revealed the smallest particle size (278.1nm), with log-normal size distribution (0.459) and adequate entrapment efficiency. A non-uniform shape was observed in the transmission electron microscopy. The viscosity of F6 formulation hydrogel was 32.34 (Pa·s), which exhibited plastic behavior. In vivo, efficacy studies demonstrated decreased inflammation of the epidermis and dermis and a marked decrease in the levels of IL-17 by NS EV hydrogel compared to plain NS oil and standard drugs (Betamethasone and Dr. JRK Psorolin Oil).
Conclusion: It may be concluded from the findings that NS-loaded EV gel was as good as betamethasone cream but more efficacious than the other treatments.
{"title":"Nigella sativa Oil-loaded Ethanolic Vesicular Gel for Imiquimod-induced Plaque Psoriasis: Physicochemical Characterization, Rheological Studies, and In vivo Efficacy.","authors":"Samar Vihal, Swati Pundir, Charul Rathore, Uma Ranjan Lal, Gaurav Gupta, Sachin Kumar Singh, Kamal Dua, Dinesh Kumar Chellappan, Poonam Negi","doi":"10.2174/0115672018246645231019131748","DOIUrl":"https://doi.org/10.2174/0115672018246645231019131748","url":null,"abstract":"<p><strong>Background: </strong>The therapeutic effect of NS oil in mild to moderate psoriasis is limited owing to low play load of thymoquinone ( < 15 %w/w), irritation, dripping, low viscosity and thus, less contact time on the lesions.</p><p><strong>Aims: </strong>This study aimed at developing and characterizing the ethanolic vesicular hydrogel system of Nigella sativa (NS) oil (NS EV hydrogel) for the enhancement of anti-psoriatic activity.</p><p><strong>Objective: </strong>The objective of this study was to develop NS EV hydrogel and evaluate its anti-psoriatic activity.</p><p><strong>Methods: </strong>The identification and quantification of TQ content in different NS seed extracts and marketed oil were measured by an HPTLC method using n-hexane and ethyl acetate as solvent systems. Preparation of ethanolic vesicles (EVs) was performed by solvent injection method, while its antipsoriatic activity was evaluated employing an Imiquad (IMQ)-induced plaque psoriasis animal model.</p><p><strong>Results: </strong>A compact HPTLC band was obtained for TQ at an Rf value of 0.651. The calibration plot was linear in the range of 1-10 μg/spot, and the correlation coefficient of 0.990 was indicative of good linear dependence of peak area on concentration. From the different NS sources, the high TQ content was obtained in the marketed cold press oil, i.e., 1.45±0.08mg/ml. Out of various NS oilloaded EVs, the F6 formulation revealed the smallest particle size (278.1nm), with log-normal size distribution (0.459) and adequate entrapment efficiency. A non-uniform shape was observed in the transmission electron microscopy. The viscosity of F6 formulation hydrogel was 32.34 (Pa·s), which exhibited plastic behavior. In vivo, efficacy studies demonstrated decreased inflammation of the epidermis and dermis and a marked decrease in the levels of IL-17 by NS EV hydrogel compared to plain NS oil and standard drugs (Betamethasone and Dr. JRK Psorolin Oil).</p><p><strong>Conclusion: </strong>It may be concluded from the findings that NS-loaded EV gel was as good as betamethasone cream but more efficacious than the other treatments.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141494728","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 : 2024-06-27DOI: 10.2174/0115672018295087240620061102
Ziqin Wei, Hongfang Mu, Xiaojing Zhang, Wenbin Li, Rong Wang
Drug transporters are critical factors influencing the pharmacokinetics of drugs under hypoxic conditions. Studies have shown significant changes in drug transporter levels in the hypoxic environment. In addition to being regulated by HIF-1, nuclear receptors, and inflammatory factors, hypoxia can also regulate transporters through epigenetic modifications, thereby affecting drug absorption, distribution, metabolism, and excretion. In recent years, increasing attention has been paid to the role of epigenetic modifications in regulating drug transporters under hypoxic conditions at high altitude. In this paper, we comprehensively review the effects of hypoxia on drug transporters and epigenetic modifications and explore the regulatory mechanism of epigenetic modifications on drug transporter expression under hypoxic conditions. The aim is to provide a reference for exploring the epigenetic regulation mechanism of drug transporter expression in the hypoxic environment at high altitude, and then guide the study of pharmacokinetics and promote effective and safe medication at high altitude.
{"title":"Progress in Epigenetic Modification Regulating Drug Transporters in the Hypoxic Environment.","authors":"Ziqin Wei, Hongfang Mu, Xiaojing Zhang, Wenbin Li, Rong Wang","doi":"10.2174/0115672018295087240620061102","DOIUrl":"https://doi.org/10.2174/0115672018295087240620061102","url":null,"abstract":"<p><p>Drug transporters are critical factors influencing the pharmacokinetics of drugs under hypoxic conditions. Studies have shown significant changes in drug transporter levels in the hypoxic environment. In addition to being regulated by HIF-1, nuclear receptors, and inflammatory factors, hypoxia can also regulate transporters through epigenetic modifications, thereby affecting drug absorption, distribution, metabolism, and excretion. In recent years, increasing attention has been paid to the role of epigenetic modifications in regulating drug transporters under hypoxic conditions at high altitude. In this paper, we comprehensively review the effects of hypoxia on drug transporters and epigenetic modifications and explore the regulatory mechanism of epigenetic modifications on drug transporter expression under hypoxic conditions. The aim is to provide a reference for exploring the epigenetic regulation mechanism of drug transporter expression in the hypoxic environment at high altitude, and then guide the study of pharmacokinetics and promote effective and safe medication at high altitude.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141474411","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}
Nanoliposomal formulations, utilizing lipid bilayers to encapsulate therapeutic agents, hold promise for targeted drug delivery. Recent studies have explored the application of machine learning (ML) techniques in this field. This study aims to elucidate the motivations behind integrating ML into liposomal formulations, providing a nuanced understanding of its applications and highlighting potential advantages. The review begins with an overview of liposomal formulations and their role in targeted drug delivery. It then systematically progresses through current research on ML in this area, discussing the principles guiding ML adaptation for liposomal preparation and characterization. Additionally, the review proposes a conceptual model for effective ML incorporation. The review explores popular ML techniques, including ensemble learning, decision trees, instance- based learning, and neural networks. It discusses feature extraction and selection, emphasizing the influence of dataset nature and ML method choice on technique relevance. The review underscores the importance of supervised learning models for structured liposomal formulations, where labeled data is essential. It acknowledges the merits of K-fold cross-validation but notes the prevalent use of single train/test splits in liposomal formulation studies. This practice facilitates the visualization of results through 3D plots for practical interpretation. While highlighting the mean absolute error as a crucial metric, the review emphasizes consistency between predicted and actual values. It clearly demonstrates ML techniques' effectiveness in optimizing critical formulation parameters such as encapsulation efficiency, particle size, drug loading efficiency, polydispersity index, and liposomal flux. In conclusion, the review navigates the nuances of various ML algorithms, illustrating ML's role as a decision support system for liposomal formulation development. It proposes a structured framework involving experimentation, physicochemical analysis, and iterative ML model refinement through human-centered evaluation, guiding future studies. Emphasizing meticulous experimentation, interdisciplinary collaboration, and continuous validation, the review advocates seamless ML integration into liposomal drug delivery research for robust advancements. Future endeavors are encouraged to uphold these principles.
利用脂质双层膜包裹治疗药物的纳米脂质体制剂有望实现靶向给药。最近的研究探索了机器学习(ML)技术在这一领域的应用。本研究旨在阐明将 ML 集成到脂质体制剂中的动机,提供对其应用的细致理解,并强调其潜在优势。综述首先概述了脂质体制剂及其在靶向给药中的作用。然后,系统地介绍了该领域目前对 ML 的研究,讨论了指导 ML 适应脂质体制备和表征的原则。此外,该综述还提出了有效结合 ML 的概念模型。综述探讨了流行的 ML 技术,包括集合学习、决策树、基于实例的学习和神经网络。它讨论了特征提取和选择,强调了数据集性质和 ML 方法选择对技术相关性的影响。综述强调了监督学习模型对于结构化脂质体配方的重要性,在这种配方中,标记数据至关重要。它承认 K 倍交叉验证的优点,但指出在脂质体制剂研究中普遍使用单一的训练/测试分割。这种做法有利于通过三维图对结果进行可视化的实际解释。在强调平均绝对误差这一关键指标的同时,综述还强调了预测值与实际值之间的一致性。综述清楚地展示了 ML 技术在优化封装效率、粒度、药物负载效率、多分散指数和脂质体通量等关键制剂参数方面的有效性。总之,综述介绍了各种 ML 算法的细微差别,说明了 ML 作为脂质体制剂开发决策支持系统的作用。它提出了一个结构化框架,包括实验、理化分析以及通过以人为本的评估迭代完善 ML 模型,为未来的研究提供指导。该综述强调细致的实验、跨学科合作和持续验证,主张将 ML 无缝集成到脂质体给药研究中,以实现强劲的进步。我们鼓励未来的努力坚持这些原则。
{"title":"Machine Learning-Driven Advancements in Liposomal Formulations for Targeted Drug Delivery: A Narrative Literature Review.","authors":"Benyamin Hoseini, Mahmoud Reza Jaafari, Amin Golabpour, Zahra Rahmatinejad, Maryam Karimi, Saeid Eslami","doi":"10.2174/0115672018302321240620072039","DOIUrl":"https://doi.org/10.2174/0115672018302321240620072039","url":null,"abstract":"<p><p>Nanoliposomal formulations, utilizing lipid bilayers to encapsulate therapeutic agents, hold promise for targeted drug delivery. Recent studies have explored the application of machine learning (ML) techniques in this field. This study aims to elucidate the motivations behind integrating ML into liposomal formulations, providing a nuanced understanding of its applications and highlighting potential advantages. The review begins with an overview of liposomal formulations and their role in targeted drug delivery. It then systematically progresses through current research on ML in this area, discussing the principles guiding ML adaptation for liposomal preparation and characterization. Additionally, the review proposes a conceptual model for effective ML incorporation. The review explores popular ML techniques, including ensemble learning, decision trees, instance- based learning, and neural networks. It discusses feature extraction and selection, emphasizing the influence of dataset nature and ML method choice on technique relevance. The review underscores the importance of supervised learning models for structured liposomal formulations, where labeled data is essential. It acknowledges the merits of K-fold cross-validation but notes the prevalent use of single train/test splits in liposomal formulation studies. This practice facilitates the visualization of results through 3D plots for practical interpretation. While highlighting the mean absolute error as a crucial metric, the review emphasizes consistency between predicted and actual values. It clearly demonstrates ML techniques' effectiveness in optimizing critical formulation parameters such as encapsulation efficiency, particle size, drug loading efficiency, polydispersity index, and liposomal flux. In conclusion, the review navigates the nuances of various ML algorithms, illustrating ML's role as a decision support system for liposomal formulation development. It proposes a structured framework involving experimentation, physicochemical analysis, and iterative ML model refinement through human-centered evaluation, guiding future studies. Emphasizing meticulous experimentation, interdisciplinary collaboration, and continuous validation, the review advocates seamless ML integration into liposomal drug delivery research for robust advancements. Future endeavors are encouraged to uphold these principles.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141474410","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}