Oral Fast-Release Solid Dispersion-Paradigm Shift to Nanoparticles

Abstract

Design of oral fast-release solid dispersion of poorly water-soluble drugs has been a great challenge over past decades on issues of drug recrystallization, drug polymorphism, formulation limited to low drug-to-carrier ratio and drug particle aggregation in matrix. The complexity in solid dispersion design is envisaged to be resolvable by the use of nanoparticulate system as solid dosage form. This manuscript reviews several patented processing approaches of nanoparticulate solid dispersion that have been reported recently. Through drug nanoencapsulation, a higher content of drug may be delivered with less aggregation via placing the same drug mass in a greater number of tinier carriers. Nanoencapsulation, by its own process of formation, brings about submicron particles. Keeping drug in these nanoparticles, a remarkable rise in specific surface area of drug is realized for dissolution. The augmentation of drug dissolution can be sufficiently high to the extent that the influences of polymorphism and crystallization phenomenon on drug dissolution in a solid dispersion may be negligible.

Nonlinear Effects of Nanoparticles: Biological Variability from Hormetic Doses, Small Particle Sizes, and Dynamic Adaptive Interactions

“…Sizes typically range from a fraction of one nanometer (nm) in diameter on at least one side up to 100 nanometers (European Commission on the Environment, 2011; International Organization for Standardization, 2005). Although submicron particles between 100-1000 nanometers in size have some advantages toward improving drug delivery (Oyewumi et al, 2010;Stovbun et al, 2012;Wong, 2011), much of the focus of research interest in NPs has been on particles whose size falls below 100 nm. Their small size leads to a large surface area to volume ratio, resulting in variations of properties that differ markedly from those of bulk forms of the "same" material (Buzea et al, 2007;Cao and Wang, 2011;Roduner, 2006).…”