Enhancing Skin Penetration of Meloxicam: Liposomal Formulation Development and Optimization

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Aryan YousefiFard, Anayatollah Salimi, Eskandar Moghimipour, Nasim Karami
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引用次数: 0

Abstract

Background

Meloxicam is a potent nonsteroidal anti-inflammatory drug (NSAID) utilized for the treatment of acute pain and inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Despite its therapeutic benefits, meloxicam’s oral use can be associated with significant gastrointestinal risks, such as bleeding, ulcerations, and perforations, which pose challenges to patient safety and treatment adherence. Transdermal drug delivery effectively reduces these limitations, with liposomes providing an appropriate system for this route of administration. The study aimed to develop a liposomal formulation of meloxicam that could pass through skin barriers and facilitate transdermal drug delivery.

Materials and Methods

The study was based on a full factorial design, and the effect of independent variables, namely lecithin, cholesterol, and sonication time, was investigated to determine the liposomes constructed by the thin film hydration method.

Results

The particle sizes of liposomes ranged from 146 to 268 nm, with drug loading percentages between 26.24% and 63.13%. Higuchi’s model best matched the drug release profiles. The findings indicated that reducing the amounts of both lecithin and cholesterol resulted in an increased percentage of drug release. Additionally, enhanced sonication time led to higher steady-state fluxes (Jss) and permeability coefficients, as well as a reduction in lag time (Tlag).

Conclusion

This study showed that the liposomal formulation improved skin penetration by getting around meloxicam’s physicochemical limitations. This suggests a promising way to deliver the drug topically.

Graphical Abstract

Graphical abstract shows increased penetration of meloxicam into the skin by optimizing liposomal formulation

促进美洛昔康皮肤渗透:脂质体配方开发与优化
美洛昔康是一种有效的非甾体抗炎药(NSAID),用于治疗急性疼痛和炎症性疾病,包括骨关节炎和类风湿关节炎。尽管具有治疗益处,但口服美洛昔康可能与显著的胃肠道风险相关,如出血、溃疡和穿孔,这对患者安全和治疗依从性构成挑战。经皮给药有效地减少了这些限制,脂质体为这种给药途径提供了适当的系统。该研究旨在开发一种可以通过皮肤屏障并促进透皮给药的美洛昔康脂质体配方。材料与方法本研究采用全因子设计,考察了卵磷脂、胆固醇、超声时间等自变量对薄膜水合法制备脂质体的影响。结果脂质体粒径为146 ~ 268 nm,载药率为26.24% ~ 63.13%。Higuchi的模型最符合药物释放谱。研究结果表明,减少卵磷脂和胆固醇的含量会增加药物释放的百分比。此外,增强的超声时间导致更高的稳态通量(Jss)和渗透率系数,以及延迟时间(lag)的减少。结论本研究表明,脂质体制剂绕过美洛昔康的物理化学限制,改善了皮肤渗透。这为局部给药提供了一种很有希望的方法。图形摘要图形摘要显示通过优化脂质体配方可以增加美洛昔康对皮肤的渗透
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Journal of Pharmaceutical Innovation
Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-
CiteScore
3.70
自引率
3.80%
发文量
90
审稿时长
>12 weeks
期刊介绍: The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.
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