title: Oridonin-loaded poly(epsilon-caprolactone)-poly(ethylene oxide)-poly(epsilon-caprolactone) copolymer nanoparticles: preparation, characterization, and antitumor activity on mice with transplanted hepatoma.
abstract: The aim of the present study was to develop a polymeric delivery system for water-insoluble drug oridonin. Amphiphilic block copolymers, poly(epsilon-caprolactone)-poly(ethylene glycol)-poly (epsilon-caprolactone) (PCL-PEO-PCL), were synthesized by ring-opening polymerization of caprolactone initiated by the hydroxyl groups of poly(ethylene glycol)6000 (PEG-6000) with stannous octoate as catalyzer. Oridonin-loaded PCL-PEO-PCL copolymer nanoparticles (ORI-PCL-PEO-PCL-NPs) were prepared by the interfacial deposition method. The mean particle size of the drug-loaded nanoparticles was 97.5 nm and the zeta potential was - 25 mV. The entrapment efficiency and actual drug loading of the nanoparticles were 87.52% +/- 1.86% and 8.63% +/- 0.49%, respectively. The antitumor activity of ORI-PCL-PEO-PCL-NPs was evaluated by measuring changes in tumor volumes, tumor weights, and survival rates of mice with grafted hepatoma (H22). The results indicated that ORI-PCL-PEO-PCL-NPs prolonged the survival time of mice and exhibited higher therapeutic efficacy compared with free oridonin. Thus, ORI-PCL-PEO-PCL-NPs may be used as a promising delivery system for liver cancer treatment.
authors.affiliation: Department of Pharmaceutics, Shanghai University of Traditional Chinese Medicine, Shanghai, P. R. China. npfeng@hotmail.com
authors.forename: Nianping
authors.initials: N
authors.lastname: Feng
authors.forename: Peiyi
authors.initials: P
authors.lastname: Wu
authors.forename: Qi
authors.initials: Q
authors.lastname: Li
authors.forename: Yinghao
authors.initials: Y
authors.lastname: Mei
authors.forename: Shuiping
authors.initials: S
authors.lastname: Shi
authors.forename: Jing
authors.initials: J
authors.lastname: Yu
authors.forename: Jie
authors.initials: J
authors.lastname: Xu
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
authors.forename: Yan
authors.initials: Y
authors.lastname: Wang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000627:therapeutic use; D002152:Calorimetry, Differential Scanning; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy*; D045786:Diterpenes, Kaurane / Q000008:administration & dosage* / Q000737:chemistry / Q000627:therapeutic use; D004337:Drug Carriers; D016503:Drug Delivery Systems; D008114:Liver Neoplasms, Experimental / Q000188:drug therapy*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D009368:Neoplasm Transplantation; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D000970:Antineoplastic Agents; D045786:Diterpenes, Kaurane; D004337:Drug Carriers; D011091:Polyesters; C492324:poly(epsilon-caprolactone)-poly(oxyethylene)-poly(epsilon-caprolactone); C011959:oridonin; D011092:Polyethylene Glycols