Biomaterials Center, National Institute for Materials Science, Tsukuba 305-0044, Japan.
Mol Pharm. 2011 Jun 6;8(3):807-13. doi: 10.1021/mp100401d. Epub 2011 Mar 25.
Development of oral dosage forms containing poorly water-soluble drugs is a major challenge in the pharmaceutical industry. This paper describes the use of coaxial electrospray deposition as a promising formulation technology for oral delivery of poorly water-soluble drugs. The technology produced core-shell particles composed of griseofulvin and poly(methacrylic acid-co-methyl methacrylate) (Eudragit L-100), with a diameter of around 1 μm. The drug phase was in an amorphous state when the griseofulvin core was coated with the Eudragit L-100 shell. The in vitro dissolution and in vivo oral absorption studies revealed that the core-shell formulation significantly improved dissolution and absorption behaviors, presumably because of a reduction in particle size, improvement in dispersity, and amorphization. Results demonstrated that coaxial electrospray deposition possesses great potential as novel formulation technology for enhancing oral absorption of poorly water-soluble drugs.
开发含有难溶性药物的口服剂型是制药行业面临的主要挑战。本文介绍了同轴电喷雾沉积作为一种有前途的难溶性药物口服传递制剂技术的应用。该技术生产了由灰黄霉素和聚（甲基丙烯酸-co-甲基丙烯酸甲酯）（Eudragit L-100）组成的核壳颗粒，直径约为 1 μm。当灰黄霉素核被 Eudragit L-100 壳包裹时，药物相处于无定形态。体外溶解和体内口服吸收研究表明，核壳制剂显著改善了溶解和吸收行为，这可能是由于粒径减小、分散性提高和无定形化。结果表明，同轴电喷雾沉积作为一种新型制剂技术，具有增强难溶性药物口服吸收的巨大潜力。
