Solid Dispersion Technology As a Strategy to Improve the Bioavailability of Poorly Soluble Drugs

Abstract

Over the last half-century, solid dispersions (SDs) have been intensively investigated as a strategy to improve drugs solubility and dissolution rate, enhancing oral bioavailability. In this review, an overview of the state of the art of SDs technology is presented, focusing on their classification, the main preparation methods, the limitations associated with their instability, and the marketed products. To fully take advantage of SDs potential, an improvement in their physical stability and the ability to prolong the supersaturation of the drug in gastrointestinal fluids is required, as well as a better scientific understanding of scale-up for defining a robust manufacturing process. Taking these limitations into account will contribute to increase the number of marketed pharmaceutical products based on SD technology.

Recent Advances in the Design of Self‐Delivery Amphiphilic Drugs and Vaccines

“…Possible loading efficiency, stability, and toxicological issues including immunogenicity greatly restrict the clinical applications of some of the delivery systems in the short term . An emerging new strategy to overcome the above limitations is the design of drug self‐delivery systems (DSDSs) that eliminate the need for external delivery carriers . The term DSDSs refers to drugs or drug conjugates that are capable of achieving efficient tissue, cellular, and/or subcellular targeting without the assistant of conventional carriers.…”

Drug Release Control and Enhancement Using Carriers With Different Concentrations of Capmul® MCM C8

“…This has increased the attention towards the continuous development and improvement of drug delivery systems, capable to enhance the solubility of poorly soluble drugs; thus enhancing the drug bioavailability and therapeutic efficacy [1]. Various methods and technologies have been reported to improve the bioavailability of poorly soluble drugs, such as mesoporous silica based systems, solid dispersion technology, nanocrystals technology, liposomes, supercritical fluid technology, selfemulsifying systems and melt extrusion [2][3][4][5][6][7][8]. The crystalline drug form might be converted to the more soluble amorphous form (no energy is required to break the intermolecular forces of the crystal lattice) in these approaches.…”

Hyperbranched poly(glycerol esteramide): A biocompatible drug carrier from glycerol feedstock and dicarboxylic acid

“…In this context, the bioavailability of BCS Class II drug is rate‐limited by its solubility 47 . Solubility is closely related to dissolution, which is a kinetic process that involves the diffusion of drug molecules after their detachment from the solid surface 48 . Hence, improving the dissolution and solubility of the drug plays the key role in improving the overall bioavailability of BCS class II drugs and the use of biopolymers to tackle this issue is very much appreciated by the pharmaceutical industry.…”