Controlled release of solid-reversed-micellar-solution (SRMS) suppositories containing metoclopramide-HCl

Area of Science:

• Pharmaceutics
• Drug Delivery Systems
• Materials Science

Background:

• Conventional drug delivery systems often face challenges with controlled release and bioavailability.
• Metoclopramide-HCl (MCP) is a widely used antiemetic drug requiring effective delivery methods.

Purpose of the Study:

• To develop and evaluate a novel solid-reversed-micellar-solution (SRMS) for rectal delivery of metoclopramide-HCl (MCP).
• To investigate the in vitro and in vivo performance of SRMS suppositories for controlled drug release.

Main Methods:

• Formulation of SRMS using Witepsol W35 and lecithin, incorporating MCP.
• Characterization of SRMS transformation into a liquid crystalline lamellar mesophase upon contact with aqueous media.
• In vitro drug release studies (zero-order kinetics) and in vivo bioavailability studies in rabbits comparing SRMS suppositories with commercial ones.

Main Results:

• SRMS demonstrated application-induced transformation into a liquid crystalline lamellar mesophase.
• In vitro studies showed zero-order kinetics and sustained release of MCP from SRMS suppositories.
• In vivo studies revealed a five-fold longer mean residence time for SRMS suppositories compared to commercial formulations.

Conclusions:

• Rectal application of SRMS suppositories is an effective strategy for controlled release of MCP.
• The unique liquid crystalline microstructure of SRMS facilitates sustained drug release and enhanced bioavailability.