“Development And Optimization Of Paroxetine Hydrochloride Loaded Microemulsion Almond Oil Based Transdermal Drug Delivery”

Abstract

Background: Paroxetine HCl is the antidepressant drug which is known to be a most potent serotonin reuptake blocker. This study was aimed to reduce the consequences accompanied with the fluctuations in concentration of plasma level after oral administration of drug and additionally in imitation to minimize broad metabolism of the same in the hepatic by flourishing and optimizing the formulation of transdermal paroxetine hydrochloride in order to increase its bioavailability and safety. Objectives: In the present research, paroxetine Hydrochloride microemulsion transdermal gel as alternative route of drug administration have been prepared and characterized. Methods: A pseudo-ternary phase diagram, D optimal and Factorial designs have been used to observe and optimize the microemulsion. Using pseudo-ternary phase diagram microemulsion area was subjected to select and according to that ratio of percentage oil, percentage surfactant and percentage co-surfactant, microemulsion were optimized. Based on phase diagrams, formulations have been prepared and elucidate for various parameters including compatibility test within the drug and excipient by FT-IR. The prepared transdermal gel was tests for analysis of size distribution, Zeta potential, thermal analysis, % CDR, % transmittance, globule size, Cmax, Tmax, drug content, in-vitro diffusion, ex-vivo permeation, and accelerated stability studies were performed. Results: Microemulsion based gel of Paroxetine HCl formulations results revealed that all the physicochemical parameters were found to be desirable. The best formulation passed thermodynamic stability studies, robust to dilutions of different medium and showed drug release of approx. 79.23% in 8h. The optimized formulation having the combination of Almond Oil (3ml), surfactant mixtures were consisted of Tween®80 & Propylene glycol in 1:3 ratio (15ml) and DDW (32ml) as an aqueous phase showed best physicochemical parameters with 89.12 % of in-vitro drug release at 8h i.e. close to predicted values obtained from d-optimal design. The optimized formulation showed no significant changes on physiochemical studies when subjected to accelerated stability studies according to ICH guidelines. Conclusion: The developed Paroxetine HCl microemulsion based transdermal gel showed good physicochemical properties. It is concluded from the present studies that Paroxetine HCl microemulsions shown a potential transdermal drug delivery system with virtuous stability and drug release profile.