Strategic development of aceclofenac loaded organosomes for topical application: An explorative ex-vivo and in-vivo investigation for arthritis

IF 5.3 2区医学 Q1 PHARMACOLOGY & PHARMACY

International Journal of Pharmaceutics Pub Date : 2024-10-01 DOI:10.1016/j.ijpharm.2024.124762

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引用次数: 0

Abstract

Present study intends to develop aceclofenac-encapsulated organosomes (OS), which consist of phospholipids coupled with a combination of organic solvents, for the management of arthritis. The formulation was characterized and tested for efficacy using formalin-induced hyperalgesia, air pouch, and CFA-induced arthritic rat models. OS system exhibited spherical dimension, nanometric size with low PDI (278.3 ± 12.21 nm; 0.145), zeta potential (−24.56 ± 7.53 mV), drug entrapment (85.62 ± 7.2 %) and vesicles count (4.2x104 mm³). The gelled OS formulation demonstrated increased drug permeability and accumulation rate (51.77 ± 7.1 % and 396.19 ± 59.21 µg/cm²) compared to the MKT product (102.93 ± 13.78 µg/cm² and 16.14 ± 4.3 %). Dermatokinetic assessments exhibited significantly higher drug levels in dermal layers compared to MKT product (p < 0.001), and CLSM studies further supported the OS system’s deeper penetration. The results of arthritic index significantly better (9 times) in the OS-treated group than the MKT product. OS system treatment significantly reduced biochemicals and cytokines levels, such as CRP, ESR, TLC, lymphocytes, TNF-α, IL-6, and IL-1β to levels of the control group (p < 0.001). Pseudoplastic behaviour of the developed product was indicated by the rheological results, and it also demonstrated biocompatibility through skin compliance studies. Based on the current findings, it appears that OS may be a better choice for managing arthritis and related inflammations.

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用于局部应用的醋氯芬酸负载有机体的战略开发：针对关节炎的体内外探索性研究。

本研究旨在开发由磷脂和有机溶剂组合而成的醋氯芬酸包封有机体（OS），用于治疗关节炎。利用福尔马林诱导的痛觉减退、气囊和 CFA 诱导的关节炎大鼠模型对该制剂进行了表征和药效测试。OS 系统呈球形，尺寸为纳米级，具有较低的 PDI（278.3 ± 12.21 nm；0.145）、zeta 电位（-24.56 ± 7.53 mV）、药物夹带率（85.62 ± 7.2 %）和囊泡数（4.2x104 mm3）。与 MKT 产品（102.93 ± 13.78 µg/cm2 和 16.14 ± 4.3 %）相比，凝胶 OS 制剂显示出更高的药物渗透性和蓄积率（51.77 ± 7.1 % 和 396.19 ± 59.21 µg/cm2）。皮肤动力学评估显示，与 MKT 产品相比，药物在真皮层的含量明显更高（p

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来源期刊

International Journal of Pharmaceutics 医学-药学

CiteScore

10.70

自引率

8.60%

发文量

951

审稿时长

72 days

期刊介绍： The International Journal of Pharmaceutics is the third most cited journal in the "Pharmacy & Pharmacology" category out of 366 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.