Solid Dispersion in Pharmaceutical Drug Development: From Basics to Clinical Applications

Abstract

The solubility of drugs is one of the most challenging aspects in developing formulations for novel drug discovery. Myriad of approaches have been developed and tested to overcome the associated intricacies involved with poor water soluble drugs. Out of the available technologies, solid dispersion (SD) method that significantly enhances the solubility and bioavailability by reducing particle size to a micro-molecular level is often viewed as a promising strategy. Although conceptual basis of manufacturing processes involved in SD method have been reported, formulation characteristics addressing solubility issues remains yet elusive. The current review portray the historical milestones, classification, probable mechanisms for enhancement of solubility, manufacturing processes at commercial level along with pioneer breakthroughs in field that enunciates the versatile pharmaceutical application for categories including anti-cancer and anti-retroviral drugs. Besides, our article also highlights the translational implications of drug development by SD method hitherto unreported.

Formulation development and systematic optimization of stabilized ziprasidone hydrochloride capsules devoid of any food effect

“…On coming in contact with the aqueous medium, the polymer helps the drug to attain sufficient wettability and consequently enhanced solubility. The results are in accordance with published literature where improved solubility profiles of low soluble drugs have been attained with solid dispersions [29][30][31][32][33] .…”

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

“…Conclusive results from both studies displayed the improvement of solubility and dissolution by the use of solid dispersions. Since its innovation in 1961, solid dispersions have become the cornerstone for improvement in the oral delivery of poorly water-soluble drugs today (12).…”

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“…Solid dispersion (SD) technology has been explored by formulation scientists as one of the suitable approaches to formulate poorly watersoluble drugs to enhance their solubility and dissolution rate [12][13][14][15][16][17][18] . This technology was first introduced by Sekiguchi and Obi 19, where they enhanced the solubility of poorly soluble sulfathiazole by using crystalline carriers like urea.…”

“…They provide information on physical and chemical changes that include endothermic/exothermic processes or changes in heat capacity 26 . Differential Scanning calorimeter (DSC 60, Shimadzu, Tokyo, Japan) was used to study the thermal behavior of the samples of CFZ, EE PO, PM, and SDs 18 . The samples were subjected to the temperature range of 25°-200 ºC at a heating rate of 10 °C min -1 under nitrogen atmosphere at a flow rate of 100 ml min -1 .…”

“…The X-ray diffraction study was carried out to characterize the physical form of CFZ in its pure state and samples of solid dispersion 18 . The X-ray diffractometer (Rigaku SmartLab) recorded the XRD pattern using Cu Kα line at a voltage of 40k V and current 30mA.…”