QbD-assisted optimisation of liposomes in chitosan gel for dermal delivery of aceclofenac as synergistic approach to combat pain and inflammation.

Autor: Amisha; Department of Pharmaceutics, ISF College of Pharmacy, Moga, 142 001, India., Das Gupta G; Department of Pharmaceutics, ISF College of Pharmacy, Moga, 142 001, India., Singh H; GEM Lab, Department of Pathology, Augusta University, Augusta, GA, USA., Singh S; Department of Pharmacology, ISF College of Pharmacy, Moga, 142001, India., Singh A; Department of Pharmaceutics, ISF College of Pharmacy, Moga, 142 001, India. amrinder.aulakh@yahoo.com.; Chitkara College of Pharmacy, Chitkara University, Rajpura, Punjab, India. amrinder.aulakh@yahoo.com.
Jazyk: angličtina
Zdroj: Drug delivery and translational research [Drug Deliv Transl Res] 2024 Sep; Vol. 14 (9), pp. 2403-2416. Date of Electronic Publication: 2024 Jan 30.
DOI: 10.1007/s13346-024-01514-z
Abstrakt: Aceclofenac (ACE) is a drug that was precisely devised to circumvent the shortcomings associated with diclofenac. However, ACE too corresponds to nonsteroidal anti-inflammatory drug (NSAID)-related adverse effects, but with a lower amplitude. The present investigation seeks to develop liposomes loaded with ACE adopting a central composite design (CCD) and formulate a chitosan-based hydrogel for synergistic anti-inflammatory efficacy and improved ACE dermal administration. On the basis of preliminary vesicle size, Poly Dispersity Index (PDI), and drug entrapment, the composition of lipid, cholesterol, and vitamin E TPGS were chosen as independent variables. The formulation composition met the specifications for an optimum liposomal formulation, with total lipid concentration (13.5% w/w), cholesterol concentration (10% w/w), and surfactant concentration (2% w/w). With particle size and PDI of 174.22 ± 5.46 nm and 0.285 ± 0.01 respectively, the optimised formulation achieved an entrapment effectiveness of 92.08 ± 3.56%. Based on the CCD design, the optimised formulation Acec-Lipo opt was chosen and was subsequently transformed to a chitosan-based gel formulation for in vitro drug release, penetration through the skin, in vivo analgesic therapeutic activity, and skin irritation testing. % age oedema inhibition was found to be greatest with the Acec-Lipo opt gel formulation, followed by Acec gel. These results reinforce the notion that the inclusion of chitosan resulted in a synergistic effect despite the same strength of the drug. The findings suggested that Acec-Lipo incorporated in chitosan gel for skin targeting might be an effective formulation for topical ACE administration in clinical subjects.
(© 2024. Controlled Release Society.)
Databáze: MEDLINE
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