Subramaniyan Gopinath, Shaik Rubina, Ramana Bachu Venkata, A Meriton Stanley, Srinivasan Devasena
Department of Pharmaceutics, Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (DU), Porur, Chennai-600 116. Tamil Nadu, India.
Department of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (DU), Porur, Chennai-600 116, Tamil Nadu, India.
Pharm Nanotechnol. 2025 Jan 27. doi: 10.2174/0122117385346215250109142123.
This study aimed to develop and evaluate lornoxicam (LXM) and thiocolchicoside (TCS) transferosomal transdermal patches.
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.
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.
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.
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.
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.
本研究旨在研发并评估氯诺昔康（LXM）和硫代秋水仙碱（TCS）传递体透皮贴剂。
口服LXM和TCS会导致胃部刺激，因此需要其他给药方式来缓解疼痛和炎症。将LXM和TCS纳入透皮贴剂中的传递体提供了一种潜在的解决方案。
本研究的目的是研发并评估含有LXM和TCS的传递体透皮贴剂，将芦荟叶黏液（AVLM）和柠檬油（LO）作为渗透促进剂。目的是增强这些药物的皮肤渗透性，同时减轻口服给药相关的胃部刺激。
采用薄膜水化法制备传递体，基于磷脂酰胆碱、司盘80和超声处理时间这三个独立变量制备了九种制剂。将包封率和第6小时的药物释放作为因变量进行评估。然后通过中心复合设计将优化后的组合制成透皮贴剂，评估AVLM和LO对氯诺昔康释放及其他理化性质的影响。
贴剂的平均重量和厚度分别在7.52±0.75至8.07±0.11g和1.69±0.01至1.82±0.02mm范围内，差异极小。LXM/TCS含量均匀度方面，LXM为92.84±3.55至94.07±4.61%，TCS为90.17±1.98至93.18±2.98%，显示出良好的均匀性。较高比例的磷脂酰胆碱和司盘80以及较短的超声处理时间可提高氯诺昔康的包封率。体外释放研究表明，较高比例的磷脂酰胆碱、中等比例的司盘80和较长的超声处理时间可实现最佳释放。传递体透皮贴剂呈现零级释放动力学，在24、48和72小时时LXM和TCS的释放百分比。
该研究得出结论，含有3g芦荟叶黏液（AVLM）和柠檬油（LO）作为渗透促进剂的制剂TDP - 8表现出良好的释放特性。这表明其作为LXM和TCS的有效透皮给药系统的潜力，为缓解疼痛和炎症提供了一种有前景的替代方法，同时将胃部刺激降至最低。该研究成功研发并评估了LXM和TCS的传递体透皮贴剂，提供了一种将胃部刺激降至最低的替代给药方式。
