Recent strategies in spray drying for the enhanced bioavailability of poorly water-soluble drugs.

Hydroxypropyl methylcellulose acetate succinate as an exceptional polymer for amorphous solid dispersion formulations: A review from bench to clinic.

Benzimidazole anthelmintics have long been employed for the control of soil-transmitted helminth infections. Flubendazole (FBZ) was approved in 1980 for the treatment of gastrointestinal nematode infections in both veterinary and human medicine. It has also long been known that parenteral administration of FBZ can lead to high macrofilaricidal efficacy in a variety of preclinical models and in humans. As part of an effort to stimulate the discovery and development of new macrofilaricides, particularly for onchocerciasis, research has recently been devoted to the development of new formulations that would afford high oral bioavailability of FBZ, paving the way for potential clinical development of this repurposed drug for the treatment of human filariases. This review summarizes the background information that led to this program and summarizes some of the lessons learned from it.

Flubendazole as a macrofilaricide: History and background.

Ordered mesoporous silica materials have shown great potential as oral drug delivery systems for poorly soluble drugs. However, the ability of these delivery systems to generate drug supersaturation has not been widely investigated, and the recently noted phenomenon of incomplete drug release is not well understood. Therefore, the aim of this study was to comprehensively evaluate the release of hydrophobic drug molecules into solution from ordered mesoporous silica, focusing on the extent and duration of drug supersaturation. The dissolution and supersaturation behavior of ritonavir, following loading into mesoporous SBA-15 silica particles, was investigated by undertaking simple in vitro dissolution studies in phosphate buffer pH 6.8 and fasted state simulated intestinal fluid, as well as membrane flux studies using a side-by-side diffusion cell apparatus. It was found that supersaturated ritonavir solutions were generated from ritonavir-loaded mesoporous SBA-15 particles; however, drug release was alway...

Supersaturation Potential of Ordered Mesoporous Silica Delivery Systems. Part 1: Dissolution Performance and Drug Membrane Transport Rates.

Stable amorphous solid dispersion of flubendazole with high loading via electrospinning.

Evaluation of Three Amorphous Drug Delivery Technologies to Improve the Oral Absorption of Flubendazole

This study investigates 3 amorphous technologies to improve the dissolution rate and oral bioavailability of flubendazole (FLU). The selected approaches are (1) a standard spray-dried dispersion with hydroxypropylmethylcellulose (HPMC) E5 or polyvinylpyrrolidone-vinyl acetate 64, both with Vitamin E d-atocopheryl polyethylene glycol succinate; (2) a modified process spray-dried dispersion (MPSDD) with either HPMC E3 or hydroxypropylmethylcellulose acetate succinate (HPMCAS-M); and (3) confining FLU in ordered mesoporous silica (OMS). The physicochemical stability and in vitro release of optimized formulations were evaluated following 2 weeks of open conditions at 25 � C/60% relative humidity (RH)

Pharmaceutics, Drug Delivery and Pharmaceutical Technology Evaluation of Three Amorphous Drug Delivery Technologies to Improve the Oral Absorption of Flubendazole

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Evaluation of Three Amorphous Drug Delivery Technologies to Improve the Oral Absorption of Flubendazole

Pharmaceutics, Drug Delivery and Pharmaceutical Technology Evaluation of Three Amorphous Drug Delivery Technologies to Improve the Oral Absorption of Flubendazole