Revolutionizing Drug Delivery: A Design Professional's Approach to Drug-loaded Transferosomal Vesicles for Transdermal Use.

Q2 Pharmacology, Toxicology and Pharmaceutics
Gopinath Subramaniyan, Rubina Shaik, Bachu Venkata Ramana, Meriton Stanley A, Devasena Srinivasan
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引用次数: 0

Abstract

Aim: This study aimed to develop and evaluate lornoxicam (LXM) and thiocolchicoside (TCS) transferosomal transdermal patches.

Background: Oral administration of LXM and TCS can lead to gastric irritation, necessitating alternative delivery methods for pain and inflammation relief. Incorporating LXM & TCS into transferosomes within a transdermal patch offers a potential solution.

Objective: The objective of this study is to develop and evaluate transferosomal transdermal patches containing LXM and TCS, incorporating Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers. The aim is to enhance the skin permeation of these drugs while mitigating gastric irritation associated with their oral administration.

Method: Transferosomes were made by the thin film hydration tactic, with nine formulations based on three independent variables: phosphatidylcholine, span 80, and sonication time. Entrapment efficiency and drug release at 6th h were assessed as dependent variables. The optimized combination was then formulated into transdermal patches via central composite design, evaluating the impact of AVLM and LO on lornoxicam discharge and other physicochemical properties.

Results: The average weight and thickness of the patches ranged from 7.52±0.75 to 8.07±0.11g and from 1.69±0.01 to 1.82±0.02mm, respectively, representing minimal variance. The LXM/TCS content homogeneity ranged from 92.84±3.55 to 94.07±4.61% for LXM and from 90.17±1.98 to 93.18±2.98% for TCS, demonstrating robust uniformity. Higher proportions of phosphatidylcholine and span 80, along with lesser sonication time, led to improved entrapment of lornoxicam. In vitro, discharge studies demonstrated optimal discharge with a higher proportion of phosphatidylcholine, a medium proportion of span 80, and a longer sonication time. The transferosomal patches exhibited zero-order discharge kinetics, with LXM & TCS discharge % at 24, 48, and 72 h.

Conclusion: The study concludes that formulation TDP-8, which incorporates 3g of Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers, demonstrated favorable discharge characteristics. This indicates its potential as an effective transdermal delivery system for LXM and TCS, offering a promising substitute for pain and inflammation relief while minimizing gastric irritation. The study succeeded in developing and evaluating transferosomal transdermal patches for LXM and TCS, providing an alternative delivery method that minimizes gastric irritation.

革命性的药物传递:经皮使用的载药转移体囊泡的设计专业方法。
目的:研制氯诺昔康(LXM)硫代秋水仙苷(TCS)转移体透皮贴剂,并对其进行评价。背景:口服LXM和TCS可导致胃刺激,需要替代给药方式来缓解疼痛和炎症。将LXM和TCS结合到透皮贴片内的转移体中提供了一个潜在的解决方案。目的:本研究的目的是开发和评估含有LXM和TCS的转移体透皮贴剂,并将芦荟叶粘液(AVLM)和石灰油(LO)作为渗透性增强剂。目的是增强这些药物的皮肤渗透,同时减轻与口服药物相关的胃刺激。方法:采用薄膜水合法制备转移体,根据磷脂酰胆碱、反应时间、反应跨度80、超声时间3个自变量确定9个配方。作为因变量评估包封效率和第6 h药物释放。然后通过中心复合设计将优化后的组合配制成透皮贴剂,评估AVLM和LO对氯诺昔康排出及其他理化性质的影响。结果:斑块的平均重量和厚度分别为7.52±0.75 ~ 8.07±0.11g和1.69±0.01 ~ 1.82±0.02mm,差异最小。LXM/TCS含量均匀性范围为92.84±3.55 ~ 94.07±4.61%,TCS含量均匀性范围为90.17±1.98 ~ 93.18±2.98%。较高比例的磷脂酰胆碱和span 80,以及较短的超声时间,导致氯诺昔康的包埋改善。体外放液研究表明,最佳放液条件为较高的磷脂酰胆碱比例、中等比例的跨度80、较长的超声时间。转移体贴片在24、48和72 h时的LXM和TCS放电率均为零级,结论:TDP-8配方中加入了3g芦荟叶粘液(AVLM)和柠檬油(LO)作为渗透性增强剂,具有良好的放电特性。这表明其作为LXM和TCS的有效透皮给药系统的潜力,提供了一个有希望的替代疼痛和炎症缓解,同时最大限度地减少胃刺激。该研究成功地开发和评估了LXM和TCS的转移体透皮贴剂,提供了一种最小化胃刺激的替代给药方法。
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来源期刊
Pharmaceutical nanotechnology
Pharmaceutical nanotechnology Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
4.20
自引率
0.00%
发文量
46
期刊介绍: Pharmaceutical Nanotechnology publishes original manuscripts, full-length/mini reviews, thematic issues, rapid technical notes and commentaries that provide insights into the synthesis, characterisation and pharmaceutical (or diagnostic) application of materials at the nanoscale. The nanoscale is defined as a size range of below 1 µm. Scientific findings related to micro and macro systems with functionality residing within features defined at the nanoscale are also within the scope of the journal. Manuscripts detailing the synthesis, exhaustive characterisation, biological evaluation, clinical testing and/ or toxicological assessment of nanomaterials are of particular interest to the journal’s readership. Articles should be self contained, centred around a well founded hypothesis and should aim to showcase the pharmaceutical/ diagnostic implications of the nanotechnology approach. Manuscripts should aim, wherever possible, to demonstrate the in vivo impact of any nanotechnological intervention. As reducing a material to the nanoscale is capable of fundamentally altering the material’s properties, the journal’s readership is particularly interested in new characterisation techniques and the advanced properties that originate from this size reduction. Both bottom up and top down approaches to the realisation of nanomaterials lie within the scope of the journal.
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