title: Effects of organic solvents on drug incorporation into polymeric carriers and morphological analyses of drug-incorporated polymeric micelles.
abstract: We incorporated an anticancer agent, camptothecin (CPT), into polymeric micelle carriers by using two different solvents (TFE and chloroform) in the solvent-evaporation drug incorporation process. We observed significant differences in the drug-incorporation behaviors, in the morphologies of the incorporated drug and the polymeric micelles, and in the pharmacokinetic behaviors between the two solvents' cases. In particular, the CPT-incorporated polymeric micelles prepared with TFE as the incorporation solvent exhibited more stable circulation in blood than those prepared with chloroform. This contrast indicates a novel technological perspective regarding the drug incorporation into polymeric micelle carriers. Morphological analyses of the inner core have revealed the presence of the directed alignment of the CPT molecules and CPT crystals in the micelle inner core. This is the first report of the morphologies of the drug incorporated into the polymeric micelle inner cores. We believe these analyses are very important for further pharmaceutical developments of polymeric micelle drug-carrier systems.
authors.affiliation: Japan Science and Technology Agency, ERATO, Takahara Soft Interfaces Project, CE80, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan.
authors.forename: Yoshiko
authors.initials: Y
authors.lastname: Harada
authors.forename: Tatsuhiro
authors.initials: T
authors.lastname: Yamamoto
authors.forename: Masaru
authors.initials: M
authors.lastname: Sakai
authors.forename: Toshiharu
authors.initials: T
authors.lastname: Saiki
authors.forename: Kumi
authors.initials: K
authors.lastname: Kawano
authors.forename: Yoshie
authors.initials: Y
authors.lastname: Maitani
authors.forename: Masayuki
authors.initials: M
authors.lastname: Yokoyama
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D001224:Aspartic Acid / Q000737:chemistry*; D001704:Biopolymers / Q000737:chemistry*; D002166:Camptothecin / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D002725:Chloroform / Q000737:chemistry*; D004337:Drug Carriers; D004339:Drug Compounding; D007700:Kinetics; D008027:Light; D008297:Male; D051379:Mice; D008823:Micelles; D018625:Microscopy, Atomic Force; D008859:Microscopy, Polarization; D015394:Molecular Structure; D036103:Nanotechnology; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D012542:Scattering, Radiation; D012995:Solubility; D012997:Solvents / Q000737:chemistry*; D013050:Spectrometry, Fluorescence; D013056:Spectrophotometry, Ultraviolet; D013678:Technology, Pharmaceutical / Q000379:methods; D014270:Trifluoroethanol / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D001704:Biopolymers; D004337:Drug Carriers; D008823:Micelles; D012997:Solvents; C416210:poly(ethylene oxide)-block-poly(beta-benzyl aspartate); D001224:Aspartic Acid; D011092:Polyethylene Glycols; D014270:Trifluoroethanol; D002725:Chloroform; D002166:Camptothecin