title: Preparation of camptothecin-loaded targeting nanoparticles and their antitumor effects on hepatocellular carcinoma cell line H22.
abstract: Camptothecin (CPT) is an effective anticancer agent against various cancers but the clinical application is limited because of its poor water solubility, low bioavailability and severe toxic side effects. The aim of the present study was to evaluate the feasibility of using targeted NPs as a high-performance CPT delivery system that targets liver cancer cells through intravenous (i.v.) administration route. CPT was incorporated into biotin-F127-PLA or F127-PLA polymeric nanoparticles (NPs) by a dialysis method. The preparation of the targeting NPs was performed by conjugating biotin-F127-PLA NPs with anti-3A5 antibody. The antitumor effect of the CPT-loaded nanoparticles against H22 cells in vitro was determined using an MTT assay. Tissue distribution and tumor inhibition in vivo were also evaluated. Survivin mRNA expression was assessed by real-time polymerase chain reaction. Results showed that the targeted CPT NPs exhibited regular spherical shapes with a mean diameter of approximately 180 nm. In vitro release of the targeted CPT NPs exhibited an initial burst (40%) within 12 h, followed by a slow release. Cytotoxicity test against H22 cells indicated that the targeted CPT NPs exerted significant antitumor effects. Compared with free CPT and non-targeted CPT NPs, the targeted CPT NPs showed superior inhibition ratio against tumor in vivo, which may be associated with reduced survivin mRNA expression. The results suggested that the new targeted CPT NPs may be a promising injectable delivery system for cancer therapy.
authors.affiliation: a State Key Laboratory of Food Science and Technology , Nanchang University , Nanchang , China .|b Sino-German Joint Research Institute, Nanchang University , Nanchang , China .
authors.forename: Anshu
authors.initials: A
authors.lastname: Yang
authors.affiliation: c Laboratory Animal Center of Science and Technology , Jiangxi University of Traditional Chinese Medicine , Nanchang , China .|d Experimental Animal Center , Jiangxi Institute of Occupational Disease Prevention , Nanchang , China , and.
authors.forename: Zhiyong
authors.initials: Z
authors.lastname: Liu
authors.affiliation: d Experimental Animal Center , Jiangxi Institute of Occupational Disease Prevention , Nanchang , China , and.
authors.forename: Bin
authors.initials: B
authors.lastname: Yan
authors.affiliation: d Experimental Animal Center , Jiangxi Institute of Occupational Disease Prevention , Nanchang , China , and.
authors.forename: Ming
authors.initials: M
authors.lastname: Zhou
authors.affiliation: e School of Life Science , Jiangxi Science & Technology Normal University , Nanchang , China.
authors.forename: Xiangyuan
authors.initials: X
authors.lastname: Xiong
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001710:Biotin / Q000737:chemistry / Q000494:pharmacology; D002166:Camptothecin / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology*; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy* / Q000378:metabolism; D045744:Cell Line, Tumor; D004337:Drug Carriers; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry* / Q000378:metabolism; D012995:Solubility; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D011108:Polymers; D001710:Biotin; D002166:Camptothecin
keywords: Antitumor effect; H22 cell; camptothecin; survivin; targeted nanoparticles