ABSTRACT

The prime objective of this investigation was to develop a self-nanoemulsifying drug delivery system (SNEDDS) of a poorly water-soluble drug i. e. Lercanidipine hydrochloride (LRCH) in order to enhance its solubility, dissolution rate and ex-vivo diffusion through transdermal route. Numerous oils, surfactants and co-surfactants were examined. Preliminary studies were carried out for the selection of the proper ingredients of the self-emulsifying system depending on the drug solubility and the emulsification power. Pseudo-ternary phase diagrams were constructed at surfactant/co-surfactant ratios of 1:1, 1:2, 1:3, 2:1 and 3:1 (% v/v) by using aqueous titration method to identify the most effective self-nano emulsification region. 32 factorial design was applied to optimize SNEDDS. Oil (X1) and Suractant: cosurfactant ratio (X2) were selected as independent variable whereas globule size, emulsification time (Y2), and drug released at 15 minutes (Y3) were taken as dependent variables. Prepared SNEDDS formulations were evaluated for different parameters like globule size (Y1), emulsification time, zeta potential, poly-dispersibility index, phase separation behaviour and percentage transmission. The optimized formulation LFB-6 was composed of 36.36% Capmul® MCM C8 as an oil, 42.42% Cremophor® RH 40 as a surfactant, and 21.22% Transcutol® P as a cosurfactant. Carbomer 941 was added as a gel matrix forming agent to convert nanoemulsion into nanoemulgel. Nanoemulgel was evaluated for rheological characteristics and imbibed in the transdermal patch to check the ex- vivo diffusion through pig abdominal skin by using Franz diffusion cell. The drugdiffusion was found to be 99.24 % after 24 h with permeation flux about 375.48 (?g/cm2/hr). The results indicated that nanoemulsion based nanoemulgel worked as a promising vehicle for transdermal delivery of LRCH. Keyword: Self-nano-drug delivery systems, pseudo ternary phase diagram, factorial design, Transdermal drug delivery, nanoemulgel, ex-vivo diffusion
Publication date: 01/03/21

https://ijbpas.com/pdf/2021/March/MS_IJBPAS_2021_5396.pdf

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https://doi.org/10.31032/IJBPAS/2021/10.3.5396