Abstract

PHARMACEUTICAL PARTICLE SIZE REDUCTION TECHNIQUES: AN APPROACH TO IMPROVE DRUG SOLUBILITY, DISSOLUTION AND BIOAVAILABILITY

Anju Thomas*, Aiswarya K., Adithya E. K., Jolly Samu and Deepu Ravindran

Abstract

Poorly soluble molecules have been successfully formulated by employing a variety of techniques to modify the physico-chemical and biopharmaceutical properties of drugs such as: (i) solubilization in surfactant solutions; (ii) use of co-solvents, salt formation, complexation with cyclodextrins, crystallization, amorphization, milling, etc. Among various techniques for solubility enhancement, physical modifications of drug products such as reducing the particle size and modifying crystal habit are common approaches to increase drug solubility. According to the Noyes-Whitney equation, the reduction of the particle sizes of drug crystals increases the specific surface area, which can improve the rate of dissolution of the drug. With a reproducible and controlled particle size of active pharmaceutical ingredients and excipients, manufacturing of finished dosage form could be improved. The present review deals with the different particle size reduction technologies commonly applied to produce micro or nanosized drug crystals in order to increase the dissolution rate and absorption, and hence the bioavailability of poorlysoluble materials and allowing to optimize the formulation of the product and reduce the therapeutic dose.

Keywords: Particle size reduction, poorly soluble drugs, Solubility enhancement, Micronization, Nanosization.