Kollidon® VA 64 and Soluplus® as modern polymeric carriers for amorphous solid dispersions

Abstract

As the number of new drug candidates that are poorly soluble in water grows, new technologies that enable the enhancement of their solubility are needed. This is the case with amorphous solid dispersions (ASDs) that, nowadays, not only ensure the solubility, but can also be used to control the release rate of poorly soluble drugs. However, this dosage form must overcome the major disadvantage of ASDs, which is limited stability upon storage. Thus, a thorough knowledge on polymeric carriers that can enhance drug solubility while ensuring stability in the amorphous form is necessary. In this review, the state of the art in the application of Kollidon® VA 64 (copovidone) and Soluplus® (graft copolymer of polyvinyl caprolactam-polyvinyl acetate and poly(ethylene glycol) (PEG)) in the manufacturing of ASDs over the last 20 years is presented. Apart from the classical methods, namely solvent evaporation or melting, more advanced technologies such as pulse combustion drying, high-speed electrospinning and single-step 3D printing are described. It has been shown that both the dissolution rate (in vitro) and enhancement in bioavailability (in vivo) regarding poorly soluble active ingredients of natural or synthetic origin are possible using these matrix-forming polymers.

QbD-Based Development and Evaluation of Pazopanib Hydrochloride Extrudates Prepared by Hot-Melt Extrusion Technique: In Vitro and In Vivo Evaluation

“…Mendes et al prepared an amorphous solid dispersion of poorly soluble sulfamethoxazole drug to maintain the supersaturation in a biorelevant medium by spray drying and the hot-melt extrusion method. When the Eudragit EPO polymer was employed, the results show that supersaturation was maintained up to 24 h at all the drug–polymer proportions [ 48 ].…”

Hot Melt Extrusion for Improving the Physicochemical Properties of Polydatin Derived from Polygoni cuspidati Extract; A Solution Recommended for Buccal Applications

“…Therefore, better surface wetting, transformation of solid active substance from crystalline to amorphous form, and their dispersion into glassy matrix of amorphous polymer (Kollidon ® VA64) are the mechanisms underlying the increase in the dissolution rate [21]. Because the dissolution rate of the matrices prepared using Soluplus ® can be slowed by a viscous hydrogel layer that is formed on the surface of its particles, the release rate from hot-melt extrudates may be significantly reduced [22]. This phenomenon is clearly observed here, where with the same content of the extract in the products, the release of polydatin from the Soluplus-based system was slower after 1 h and reached only 80% release after 6 h. In addition, permeability coefficients for active compounds using PAMPA-GIT model were established.…”

Design of Experiments and Optimization of Amorphous Solid Dispersion of a BCS Class Iv Anti-Platelet Drug Through Factorial Design

“…Also, copovidone VA 64 being an excellent crystallization inhibitor and a matrix-forming agent with a glass transition temperature (Tg) of 101 °C, favouring one thermodynamically stable form during in vitro and in vivo dissolution. The absence of any exothermic peak in the DSC thermogram of the solid dispersion is indicative of a low crystallization driving force (CDF) [17].…”