ABSTRACT

Tretinoin (TRT) is principally used in the management of different kinds of acne. However, the applications of TRT are restricted due to its poor aqueous solubility, stability and associated side effects. Therefore, the main objective of the present research was to develop and characterize TRT pharmacosomes with improved solubility and stability, and reduced side effects in the treatment of acne. The pharmacosomes of TRT was prepared with hydroxylated Soyalecithin (HS) using the conventional solvent evaporation technique at different ratio of TRT to HS. The pharmacosomes were optimized based on the % yield and drug content, and optimized pharmacosomes were further characterized for Fourier transforms infrared spectroscopy (FTIR), saturated solubility, particle size and zeta potential, and in vitro dissolution study. The batch F2 of pharmacosomes displayed maximum % yield (79.22±0.77%) and TRT content (90±2.3%) when compared to other batches. The FTIR analysis confirmed the reaction between the carboxyl group of TRT and the polar moiety of HS. The pharmacosomes displayed significantly (p<0.05) increased (50-folds) solubility of TRT when compared to plain TRT in phosphate buffer solution (PBS) of pH 7.2. The optimized batch of TRT pharmacosomes showed a particle size of 152±7nm with PDI of 0.3693±0.009 and zeta potential of -3.3mV. Furthermore, in vitro dissolution study demonstrated remarkable release of TRT from pharmacosomes (97.6±7.2%) than plain TRT solution (39.5±4.5%) after 12hr in PBS of pH 7.2. Thus, the pharmacosomes could be a promising strategy for the delivery of TRT with enhanced solubility and therapeutic efficacy. Keywords: Tretinoin, Hydroxylated soyalecithin, Pharmacosomes, Acne, Saturated solubility, In vitro dissolution study
Publication date: 01/04/2022

https://ijbpas.com/pdf/2022/April/MS_IJBPAS_2022_6016.pdf

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https://doi.org/10.31032/IJBPAS/2022/11.4.6016