Abstract

FORMULATION AND EVALUATION OF LERCARNIDIPINE HYDROCHLORIDE PRONIOSOMAL GEL WITH IMPROVED SOLUBILITY AND PERMEABILITY

Gaurang Sawant* and Geeta Bhagwat

ABSTRACT

Objective:Aim of the present study was to formulate and evaluate Lercarnidpine Hydrochloride proniosomal gel with improved solublity and permeability for treatment of hypertension. Methods: Lercarnidipine Hydrochloride proniosomal gel was made by incorporating it’s proniosomal suspension which was made by coacervation phase seperation method and incorpoating the suspension into gel base. Results: The particle size was found to be between 300 and 400nm while the zeta potential was found to be 2.9mV of all formulations and polydispersity index was found to be between 0.50 and 0.60.Entrapment eficiency was found to be 92% of highest batch.In-vitro permeation of gel was found to be 92.10 % with flux (J) was found to be 107.4 µg/cm2/hr and permeability coefficient of 7.32 cm/hr while ex vivo goat skin permeability data of gel showed permeation of 105.3 µg/cm2/hr and permeability coefficient of 6.24 cm/hr. In-Vitro drug release was found to be 45±1.5% with initial burst release followed by sustained release. The Stability study showed that the proniosomal gel was found to be more stable at 4°C than at other temperatures. Conclusion: The proniosomal suspension of Lercarnidipine Hydrochloride was successfully prepared by Coacervation Phase Separation method. The particle size was small enough that are required for transdermal drug delivery and showed high drug entrapment and high drug content. The proniosomal gel showed high permeation across the skin and the drug release was dual in nature showing an initial burst release with sustained release later on. The stability studies showed that the proniosomal gel was stable for upto 3 months when stored at different temperatures as specified by the ICH guidelines.

Keywords: Lercarnidipine Hydrochloride, Proniosomal gel, Coacervation Phase seperation, Hypertension.