atneriya@gmail.com, BM College of Pharmaceutical Education and Research, Pharmaceutics, Professor, IndoreIndia
Keywords:Transdermal, Aceclofenac, Permeation enhancer, Amino acid, Release rate, L-lysine.
The study aims at developing and testing aceclofenac transdermal patches using alternative polymers and permeation enhancers, especially naturally occurring amino acids, to enhance skin penetration rate as well as provide a safe and stable state. Aceclofenac, a commonly used NSAID, has poor water solubility and causes gastrointestinal discomfort when taken orally. In order to address these disadvantages, transdermal patches have been produced by employing polymers like HPMC E-15, Eudragit RS100 and PVA. Different penetration enhancers such as DMSO, urea, and amino acids such as L-lysine, L-serine and L-arginine were added to determine their effect on the permeation of drugs. DSC, UV-visible spectroscopy, and in vitro diffusion test compatibility studies established the stability of the drug in the formulations. L-lysine was found to have the most significant enhancement effect, although, with an enhancement of 78.31% in 24h, the drug permeated better than the traditional enhancers (DMSO 68.24%). The most effective drug release was shown by the following formulations C5 (HPMC E-15 + Eudragit RS100) and D5 (HPMC E-15 + PVA), where the cumulative permeation was 70.01% and 72.28% correspondingly. There was also the uniform thickness of the patches, even distribution of drugs, high degree of flexibility, low amounts of moisture absorption as well as appropriate pH. Stability testing The optimization formulation (B5) was also found to maintain its activity and physical characteristics over time under accelerated conditions. The results of this study lead to a conclusion that amino acids, and specifically L-lysine can also be considered as safe agents to enhance the delivery of aceclofenac using the transdermal route as a viable option to the oral one with the added advantage of sustained release and lesser side effects.
Copyright (c) 2022 Umesh Kumar Atneriya,