Abstract

Poor aqueous solubility (<0.1 mg/mL) affects a significant number of drugs currently on the market or under development. Several formulation strategies including salt formation, particle size reduction, and solid dispersion approaches have been employed with varied success. In this review, we focus primarily on the emerging trends in the generation of amorphous and micro/nano-crystalline solid dispersions using electrospinning to improve the dissolution rate and in turn the bioavailability of poorly water-soluble drugs. Electrospinning is a simple but versatile process that utilizes electrostatic forces to generate polymeric fibers and has been used for over 100 years to generate synthetic fibers. We discuss the various electrospinning studies and spinneret types that have been used to generate amorphous and crystalline solid dispersions.

Highlights

  • 40% of marketed oral drugs are categorized as having poor aqueous solubility (i.e.,

  • In 1961, Sekiguchi and Obi suggested that when the drug was formulated as a solid dispersion (SD), it was present in a microcrystalline state as a eutectic mixture i.e., a combination of crystalline components that are miscible in the molten liquid state, but show little to no miscibility in the solid state and on cooling would crystallize as two components [8]

  • We focused on the emerging trends in the generation of amorphous and micro/nano-crystalline solid dispersions using electrospinning to improve the dissolution rate and in turn the bioavailability of poorly water-soluble drugs

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Summary

Introduction

40% of marketed oral drugs are categorized as having poor aqueous solubility (i.e.,

Schematic
Nanofibrous Amorphous Solid Dispersions
Electrospinning
Mono-Axial Electrospinning
Coaxial and Multi-Axial Electrospinning
Others
Findings
Conclusions
Full Text
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