title: Preparation and characterization of injectable Mitoxantrone poly (lactic acid)/fullerene implants for in vivo chemo-photodynamic therapy.
abstract: Fullerene (C60) L-phenylalanine derivative attached with poly (lactic acid) (C60-phe-PLA) was developed to prepare injectable Mitoxantrone (MTX) multifunctional implants. C60-phe-PLA was self-assembled to form microspheres consisting of a hydrophilic antitumor drug (MTX) and a hydrophobic block (C60) by dispersion-solvent diffusion method. The self-assembled microspheres showed sustained release pattern almost 15days in vitro release experiments. According to the tissue distribution of C57BL mice after intratumoral administration of the microspheres, the MTX mainly distributed in tumors, and rarely in heart, liver, spleen, lung, and kidney. Photodynamic antitumor efficacy of blank microsphere was realized. Microspheres afforded high antitumor efficacy without obvious toxic effects to normal organs, owing to its significantly increased MTX tumor retention time, low MTX levels in normal organs and strong photodynamic activity of PLA-phe-C60. These C60-phe-PLA microspheres may be promising for the efficacy with minimal side effects in future treatment of solid tumors.
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou 450001, PR China.
authors.forename: Zhi
authors.initials: Z
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou 450001, PR China.
authors.forename: Fei-long
authors.initials: FL
authors.lastname: Zhang
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou 450001, PR China.
authors.forename: Li-li
authors.initials: LL
authors.lastname: Pan
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou 450001, PR China.
authors.forename: Xia-li
authors.initials: XL
authors.lastname: Zhu
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou 450001, PR China. Electronic address: zhenzhongz@126.com.
authors.forename: Zhen-zhong
authors.initials: ZZ
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical; D003131:Combined Modality Therapy; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D037741:Fullerenes / Q000737:chemistry*; D007267:Injections; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D008545:Melanoma / Q000188:drug therapy; D051379:Mice; D008863:Microspheres; D008942:Mitoxantrone / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D010649:Phenylalanine / Q000737:chemistry; D010778:Photochemotherapy / Q000379:methods*; D011091:Polyesters; D011108:Polymers / Q000737:chemistry*; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D037741:Fullerenes; D011091:Polyesters; D011108:Polymers; D019344:Lactic Acid; C033616:poly(lactide); D010649:Phenylalanine; D008942:Mitoxantrone; C069837:fullerene C60
keywords: Chemo-photodynamic therapy; Fullerene (C60); Implants; Mitoxantrone; Poly (lactic acid); Sustained release