Design and Development of Solid Self Microemulsifying Drug Delivery System of Nicardipne Hydrochloride

Abstract

PREFACE newlinexxxvi newlineThe present study enlightens to enhance the dissolution rate of Nicardipine Hydrochloride (NHCl), a poorly soluble-highly permeable drug, by preparing self-microemulsifying mixtures, an antihypertension drug, NHCl is used to treat high blood pressure and to control angina (chest pain),NHCl is a class of calcium channel blockers. It lowers blood pressure by relaxing the blood vessels so the heart does not have to pump as hard. NHCl-loaded self-microemulsifying mixtures were prepared by using Capmul MCM C8 EP as oil, Labrasol as surfactant and polyethylene glycol 400 as co-surfactant. Ternary phase diagram were used to identify the efficient self-microemulsifying region. NHCl -loaded SMEDDS were optimized by using Box-behnken design (BBD) and Principal component analysis (PCA) technique. The prepared self-microemulsifying mixtures were evaluated for % transmittance, emulsification time, cloud point, drug content, Particle Size (nm) and Zeta Potential (mV) For optimization Response surface methodology (BBD) was employed to study the effect of independent variables i.e. amount of oil (X1), amount of surfactant (X2) and amount of co-surfactant (X3) on dependent variables i.e. Emulsification Time (Sec) (Y1) and Particle Size (nm). From the optimized batch shows emulsification time of 32.73 sec and particle size as 97.745 nm. In-vitro drug release shows faster release of drug as 90.82 % within 15 minutes. The data were statistically analysed using ANOVA and was found to be statistically significant (P lt 0.05). S-SMEDDS were obtained by using Neusilin as an adsorbent in Optimized formulation. DSC of solid SMEDDS showed no peak indicates that the drug was completely converted into amorphous form or was present in solublized form. From SEM it was revealed that S-SMEDDS were appeared as smooth-surfaced, which indicated that the liquid SMEDDS is adsorbed or coated within the pores of Neusilin US2. TEM results showed that globules of all composition formula were well