Coaxial Electrospray Formulations for Improving Oral Absorption of a Poorly Water-Soluble Drug

被引:68
|
作者
Zhang, Shaoling [1 ]
Kawakami, Kohsaku [1 ,2 ]
Yamamoto, Marina [3 ]
Masaoka, Yoshie [3 ]
Kataoka, Makoto [3 ]
Yamashita, Shinji [3 ]
Sakuma, Shinji [3 ]
机构
[1] Natl Inst Mat Sci, Ctr Biomat, Tsukuba, Ibaraki 3050044, Japan
[2] Int Ctr Mat Nanoarchitecton, Tsukuba, Ibaraki 3050044, Japan
[3] Setsunan Univ, Fac Pharmaceut Sci, Osaka 5730101, Japan
关键词
griseofulvin; amorphous; electrospray deposition; core-shell particle; poorly water-soluble drug; MICROEMULSION FORMULATION; SURFACE CRYSTALLIZATION; ENHANCED ABSORPTION; DELIVERY-SYSTEMS; NANOPARTICLES; ENCAPSULATION; INDOMETHACIN; ATOMIZATION; PARTICLES; DISCOVERY;
D O I
10.1021/mp100401d
中图分类号
R-3 [医学研究方法]; R3 [基础医学];
学科分类号
1001 ;
摘要
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 mu m. 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.
引用
收藏
页码:807 / 813
页数:7
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