Formulation, characterization, in vitro and in vivo evaluation of castor oil based self-nano emulsifying levosulpiride delivery systems

Abstract

Context: Levosulpiride (LSP) is a hydrophobic benzamide derivative used in the treatment of schizophrenia. SNEDDS were extensively practiced for systemic delivery of poorly aqueous soluble drugs to achieve maximum bioavailability.

Objective: The present study was focussed on the formulation, optimisation and evaluation of LSP SNEDDS using castor oil, for enhancement of drug absorption and bioavailability.

Materials and methods: Pseudo-ternary phase diagram was plotted to identify the range of SNEDDS components. Twenty formulations were designed, prepared and characterised by its particle size, zeta potential, viscosity, and stability. In vitro dissolution data modelling was performed. Microscopy, FTIR and in vivo bioavailability studies were conducted for optimum formulation.

Results, discussion and conclusion: F18 containing castor oil, 0.9 mL; PEG 600, 1.36 mL and Tween 80, 2.74 mL was found to be optimum. The optimised formulation had shown uniform globule size, no interactions of LSP with SNEDDS components and higher pharmacokinetic parameters than that of commercial preparation.

Keywords:

• Levosulpiride
• pseudo-ternary diagram
• castor oil
• optimisation
• SNEDDS
• dissolution modelling
• bioavailability

Disclosure statement

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the article.

Funding

KBU acknowledges the financial support from the Prof. T.R. Rajagopalan research fund sanctioned by SASTRA University, Thanjavur, India.