Improvement in solubility of poor water-soluble drugs by solid dispersion

Abstract

This article is intended to combine recent literature on solid dispersion technology for solubility enhancement with special emphasis on mechanism responsible for the same by solid dispersion, various preparation methods, and evaluation parameters. Solubility behavior is the most challenging aspect for various new chemical entities as 60% of the new potential products possess solubility problems. This is the biggest reason for new drug molecules not reaching to the market or not reaches to full potential. There are various techniques to enhance the drug solubility such as particle size reduction, nanosuspension, use of surfactants, salt formation, solid dispersion, etc. From this article it may be concluded that solid dispersion is an important approach for improvement of bioavailability of poor water-soluble drugs.

Nanoemulsions in Translational Research—Opportunities and Challenges in Targeted Cancer Therapy

“…Many of these highly promising agents are dropped from the development pipeline because of their poor aqueous solubility. About 40% of newly discovered drugs are highly hydrophobic and fail to reach market due to their poor aqueous solubility (1). In recent years, nanoemulsions, a heterogeneous liquid dispersion of nanoscale droplets of one liquid within another, have started evolving as a feasible carrier for the delivery of hydrophobic drugs.…”

A Menthol-Based Solid Dispersion Technique for Enhanced Solubility and Dissolution of Sulfamethoxazole from an Oral Tablet Matrix

“…The modification of the physicochemical property of the molecule, the use of supercritical fluid processes, surfactants, solubilizers, and novel excipients are some of the approaches used to improve solubility of poorly soluble drug molecules (1,(3)(4)(5). Modification of the physicochemical property of a molecule includes the reduction of the particle size to increase the surface area through micronization and nanosuspensions as well as crystal engineering to decrease the crystallinity through the formation of solid dispersions (1,6).…”

Development of Glimepiride Solid Dispersion using The Coprocessed Excipients of Polyvinylpyrrolidone, Maltodextrin, and Polyethylene Glycol

“…17 The smaller size in compared to pure glimepiride were caused by its reduction when glimepiride and the co-processed excipient were melted into one and dried with spray-drying. 16 Morphology affects flow properties, glimepiride in solid dispersion had an ideal form to have good flow properties. 18 Solid dispersion morphology was finer and more uniform due to the use of spray dryer.…”