title: Preparation and cytotoxicity of poly (DL-lactide-co-glycolide) microspheres encapsulating 2-methoxyestradiol.
abstract: Injectable implant would be a potential way for 2-methoxyestradiol (2-ME) for the therapy of breast cancer because of its water-insolubility, short half-life, and low oral bioavailability. So 2-ME microspheres based on poly (DL-lactide-co-glycolide) were prepared by emulsion solvent extraction method and characterized for morphology, particle size, drug physical state, entrapment efficiency and drug release in vitro and in vivo. Their cytotoxicity on MCF-7 cells was evaluated by sulforhodamine B (SRB) method. The 2-ME was successfully entrapped in the interior of microspheres with particle size of 55.44 ± 12.21 μm and could exist in an amorphism. In vitro and in vivo release of 2-ME from the microspheres occurred in a Ritger-Peppas and zero-order manner with a slow release over 46 days, respectively, and their better correlation was found. The 2-ME even with very low concentration in the microspheres could efficiently inhibit the growth of MCF-7 cells compared to the equivalent amount of drug in free solution, which indicated that the release rate from the microspheres and local water-solubility of 2-ME could maintain effective drug concentration in target site. The above results indicated that the microspheres prepared could not only control prolonged release of 2-ME in vitro and in vivo but also maintain effective drug concentration in target site. So 2-ME microspheres are acceptable for controlled release devices for effective treatment of breast cancer.
authors.affiliation: School of Pharmacy, Zhengzhou University, Zhengzhou, P. R. China.
authors.forename: Xinhong
authors.initials: X
authors.lastname: Guo
authors.forename: Qian
authors.initials: Q
authors.lastname: Mei
authors.forename: Yabing
authors.initials: Y
authors.lastname: Xing
authors.forename: Ling
authors.initials: L
authors.lastname: Ye
authors.forename: Hongling
authors.initials: H
authors.lastname: Zhang
authors.forename: Xiufang
authors.initials: X
authors.lastname: Shi
authors.forename: Zhenzhong
authors.initials: Z
authors.lastname: Zhang
mesh_terms: D000077584:2-Methoxyestradiol; D000818:Animals; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical; D003603:Cytotoxins / Q000138:chemical synthesis* / Q000633:toxicity; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D005260:Female; D019344:Lactic Acid / Q000138:chemical synthesis* / Q000633:toxicity; D051379:Mice; D008863:Microspheres; D011100:Polyglycolic Acid / Q000138:chemical synthesis* / Q000633:toxicity; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D003603:Cytotoxins; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D004958:Estradiol; D000077584:2-Methoxyestradiol