title: Biodegradable Polymersomes as Nanocarriers for Doxorubicin Hydrochloride: Enhanced Cytotoxicity in MCF-7/ADR Cells and Prolonged Blood Circulation.
abstract: DOX is one of the most potent anticancer drugs. But its short half-life and the occurrence of multi-drug resistance (MDR) markedly limit its clinical application. To solve these problems, we develop DOX loaded polymersomes (DOX polymersomes).
  
  
  
  An methoxy poly(ethylene glycol)-b-poly(epsilon-caprolactone) (mPEG-b-PCL) copolymer was synthesized and used to prepare DOX polymersomes. The pharmaceutical properties of DOX polymersomes were characterized. The in vitro release profile of DOX from polymersomes was investigated. The in vitro cytotoxicity and cell uptake studies were performed on MCF-7 and MCF-7/ADR cells. The in vivo pharmacokinetic profiles were investigated on Sprague-Dawley rats.
  
  
  
  DOX polymersomes had a nano-scale particle size of about 60 nm with a hydrophobic membrane about 10 nm in thickness. Release of DOX from the polymersomes took place in a sustained manner. Cell experiments showed DOX polymersomes enhanced the cytotoxicity and the intracellular accumulation of DOX in MCF-7/ADR cells, compared with free DOX. In vivo pharmacokinetic study showed the DOX polymersomes increased the bioavailability and prolonged the circulation time in rats.
  
  
  
  The entrapment of DOX in biodegradable polymersomes could enhance cytotoxicity in MCF-7/ADR cells and improve its in vivo pharmacokinetic profile.
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
authors.forename: Yanhui
authors.initials: Y
authors.lastname: Chao
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
authors.forename: Yuheng
authors.initials: Y
authors.lastname: Liang
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
authors.forename: Guihua
authors.initials: G
authors.lastname: Fang
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
authors.forename: Haibing
authors.initials: H
authors.lastname: He
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
authors.forename: Qing
authors.initials: Q
authors.lastname: Yao
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
authors.forename: Hang
authors.initials: H
authors.lastname: Xu
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
authors.forename: Yinrong
authors.initials: Y
authors.lastname: Chen
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China. tanglab@126.com.
authors.forename: Xing
authors.initials: X
authors.lastname: Tang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000633:toxicity; D045744:Cell Line, Tumor; D002470:Cell Survival; D004317:Doxorubicin / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000633:toxicity; D065546:Drug Liberation; D018432:Drug Resistance, Multiple; D005026:Ethylene Glycols / Q000737:chemistry*; D006207:Half-Life; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008297:Male; D053769:Nanocapsules / Q000737:chemistry*; D011091:Polyesters / Q000737:chemistry*; D017207:Rats, Sprague-Dawley
chemical_list: D000970:Antineoplastic Agents; D005026:Ethylene Glycols; D053769:Nanocapsules; D011091:Polyesters; C476300:poly(epsilon-caprolactone)-b-poly(ethylene glycol); D004317:Doxorubicin
keywords: controlled-release; doxorubicin; multidrug resistance; pharmacokinetic; polymersomes