Abstract

DEVELOPMENT AND ASSESSMENT OF ORAL NIFEDIPINE COLLOIDAL PROVESICLES

*Mai S. Ismail, Gihan Fetih and El-Sayed A. Ibrahim

ABSTRACT

Nifedipine(NIF), a well-known calcium channel blocker, is used in the management of hypertension especially if concomitant with kidney, heart or hormonal disorders in children. Colloidal vesicular systems were reported to improve oral absorption and bioavailability of hydrophobic drugs, so the current work embodies a new type of liquid oral colloidal provesicular nano-carrier of NIF. It was developed by simple slurry method. The optimum composition of appropriate lipid film, the effect of surfactant HLB values and cholesterol level on the entrapment efficiency of NIF within liberated vesicles were studied. Additionally, investigating the effect of both initial amount of NIF and the total lipid contents on NIF vesicular entrapment and drug loading were assessed. The morphology and particle size of both provesicles and liberated nano-vesicles were estimated microscopically and by TEM. The study revealed that 300 μmol total lipids of Span 20 /cholesterol at (9:1) molar ratio is an optimum lipid film for higher NIF encapsulation. The vesicular size attained was 209 nm and 79% EE. The in-vitro release study at pH6.8 revealed an extended release pattern controlling both the release rate and extent. Furthermore, The DSC study showed The successful of intercalating NIF within the vesicle bilayer. This indicate the ability of these provesicles to load NIF successfully.

Keywords: Nifedipine, Nano-proniosomes, colloidal vesicles, TEM, stability, DSC.