Preparation and pharmaceutical evaluation of nano-fiber matrix supported drug delivery system using the solvent-based electrospinning method.
In this study, utilizing the solvent-based electrospinning (ES) method, which is mainly employed in the textile industry, we prepared nanofiber-based capsules including drugs for controlled-release delivery systems using methacrylic acid copolymer (EUDRAGIT(®) S100, MAC) as a polymer, and evaluated their in vitro drug dissolution profiles and in vivo pharmacokinetics in rats. As the model drugs, uranine (UN) was used as a water-soluble drug and nifedipine (NP) as a water-insoluble drug. The mean diameters of drug free nano-fiber and nano-fiber including NP or UN were 751.5 ± 67.2, 703.3 ± 71.2 and 2477.8 ± 206.1 nm, respectively. X-ray diffraction for the nano-fibrotic sheet showed that UN and/or NP were packed in nano-fiber in an amorphous form. The in vitro release of UN or NP from the nano-fiber packed capsules (NFPC) and milled-powder of nano-fiber packed capsules (MPPC) showed controlled release of UN or NP as compared to capsules of a physical mixture of MAC and each drug. An in vivo pharmacokinetic study in rats after intraduodenal administration of NFPC or MPPC including UN and/or NP clearly demonstrated that application of nano-fibrotic technique as a drug delivery system offers drastic changes in pharmacokinetic profiles for both water-soluble and water-insoluble drugs. The ES method is a useful technique to prepare a nano-fiber like solid dispersion for polar or nonpolar drugs, and has wide potential pharmaceutical applications.
Department of Bioharmaceutics, Faculty of Pharmaceutical Science, Doshisha Women's College of Liberal Arts, Kyotanabe, Kyoto 610-0395, Japan.
Mami
M
Hamori
Department of Bioharmaceutics, Faculty of Pharmaceutical Science, Doshisha Women's College of Liberal Arts, Kyotanabe, Kyoto 610-0395, Japan.
Shiori
S
Yoshimatsu
Department of Bioharmaceutics, Faculty of Pharmaceutical Science, Doshisha Women's College of Liberal Arts, Kyotanabe, Kyoto 610-0395, Japan.
Yuki
Y
Hukuchi
Department of Bioharmaceutics, Faculty of Pharmaceutical Science, Doshisha Women's College of Liberal Arts, Kyotanabe, Kyoto 610-0395, Japan.
Yuki
Y
Shimizu
Department of Clinical Pharmacokinetics, Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Hyogo 650-8586, Japan.
Keizo
K
Fukushima
Department of Clinical Pharmacokinetics, Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Hyogo 650-8586, Japan.
Nobuyuki
N
Sugioka
Department of Bioharmaceutics, Faculty of Pharmaceutical Science, Doshisha Women's College of Liberal Arts, Kyotanabe, Kyoto 610-0395, Japan.
Asako
A
Nishimura
Department of Bioharmaceutics, Faculty of Pharmaceutical Science, Doshisha Women's College of Liberal Arts, Kyotanabe, Kyoto 610-0395, Japan. Electronic address: nshibata@dwc.doshisha.ac.jp.
Nobuhito
N
Shibata
D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D016503:Drug Delivery Systems / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D008297:Male; D057139:Nanofibers / Q000032:analysis / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D012997:Solvents / Q000032:analysis / Q000138:chemical synthesis*; D013113:Spin Labels / Q000138:chemical synthesis*; D014961:X-Ray Diffraction / Q000379:methods
D012997:Solvents; D013113:Spin Labels
Controlled-release; Drug delivery system; Electrospinning; Nanofiber; Pharmacokinetics