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

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.