“Development And Optimization Of Microemulsion Based Transdermal Drug Delivery For Paroxetine Hydrochloride”
Background and Objectives: The aim of this work was to design and evaluate a microemulsion transdermal gel of Paroxetine Hydrochloride for the treatment of depression. Paroxetine is the most potent serotonin reuptake blocker antidepressant.
Methods: Phase-Titration method, D-Optimal design, Factorial design were used for the development of Paroxetine HCl microemulsions gel. Using pseudo-ternary phase diagram microemulsion area was selected and according to that ratio of % oil, % surfactant and % co-surfactant, microemulsion was optimized. Based on phase diagrams, formulations were prepared and evaluated for various parameters including compatibility test within the drug and excipient by FT-IR. The prepared microemulsion gel was subjected for various tests like size distribution study, zeta potential, DSC, % CDR, % transmittance, globule size, Cmax, Tmax, drug content, in-vitro diffusion and ex-vivo permeation studies.
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. 65% in 8h. The optimized formulation having the combination of Flaxseed Oil (3ml), surfactant mixture consisted of Tween®80 & Propylene glycol in 1:3 ratio (17.06ml) and double distilled water (29.93ml) as an aqueous phase showed best physicochemical parameters with 60.82 % 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.
Interpretation and Conclusion: Based on the results it can be concluded that Microemulsion transdermal gel of Paroxetine Hydrochloride could be a potential candidate for the treatment of depression.