Review on Solubility enhancement of Metoclopramide base by solid dispersion technique for Transdermal drug delivery system

Abstract

Modern drug discovery has led to the development of drug molecules that exhibit high lipophilicity and poor water solubility, which leads to problematic bioavailability. Approaches have thus been made to enhance dissolution of poorly water soluble drugs through modifications and creation of specific formulations. Metoclopramide is an antiemetic and gastroprokinetic agent, commonly used to treat nausea and vomiting. It is absorbed well after oral administration but a significant first pass effect in some human patients may reduce systemic bioavailability to 30%.The Metoclopramide base is thus modified from Metoclopramide hydrochloride to enhance solubility .This has been achieved by the formulating in solid dispersion since Metoclopramide is poorly water soluble. Though it is absorbed well after oral administration,a significant first pass effect in some patients reduces systemic bioavailability, which can cause adverse side effects. This solid dispersion has then been used through transdermal drug delivery. Enhancement of solubility of poorly water soluble drug by solid dispersion may be attributed to particles modified characters such as particle size reduction, improved wettability, higher porosity, decreased lattice energy, amorphous state. Transdermal drug delivery system has a lot of advantages such as bypassing hepatic first pass, avoidance of risks of I.V therapy, enhancing therapeutic efficiency and others but limitations like skin irritations are also prevalent.

Keywords: Solid dispersion, Metoclopramide, solubility, bioavailability, transdermal drug delivery system.