title: Fabrication of doxorubicin and heparin co-loaded microcapsules for synergistic cancer therapy.
abstract: In this study, a layer-by-layer (LbL) assembly (HEP/CHI)5 microcapsule with doxorubicin hydrochloride (DOX) encapsulating inside was fabricated via alternatively depositing heparin (HEP) and chitosan (CHI) onto DOX-loaded CaCO3 templates. The microcapsules were of stable architecture and had good dispersity in aqueous medium. Fluorescence observation showed that DOX distributed both in the wall and in the cavity of microcapsules, while HEP presented in the capsule wall. The release rate of DOX increased at acidic pH as compared with that at basic pH, suggesting a pH-responsive drug release behavior. The microcapsules with positively charged CHI lying on the outer layer could protect HEP from heparanase degradation and achieve intracellular co-delivery of both DOX and HEP. Thus, the DOX-loaded microcapsules could have improved inhibition activity against A549 cells by combining pharmacological actions of DOX and HEP.
authors: School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, PR China; Key Laboratory of Carbohydrate Chemistry and Biotechnology, Ministry of Education, Jiangnan University, Wuxi 214122, PR China.
authors: Jing-Xiao
authors: JX
authors: Chen
authors: School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, PR China.
authors: Yan
authors: Y
authors: Liang
authors: School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, PR China.
authors: Wen
authors: W
authors: Liu
authors: School of Chemical Engineering, Wuhan University of Technology, Wuhan 430070, PR China.
authors: Jin
authors: J
authors: Huang
authors: School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, PR China; Key Laboratory of Carbohydrate Chemistry and Biotechnology, Ministry of Education, Jiangnan University, Wuxi 214122, PR China. Electronic address: jhchenwhut@126.com.
authors: Jing-Hua
authors: JH
authors: Chen
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D001692:Biological Transport; D002119:Calcium Carbonate / Q000737:chemistry; D002214:Capsules; D045744:Cell Line, Tumor; D048271:Chitosan / Q000737:chemistry; D003692:Delayed-Action Preparations; D004317:Doxorubicin / Q000737:chemistry* / Q000494:pharmacology*; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism; D004357:Drug Synergism; D005966:Glucuronidase / Q000378:metabolism; D006493:Heparin / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D000099175:Heparanase
chemical_list: D000970:Antineoplastic Agents; D002119:Calcium Carbonate; D002214:Capsules; D048271:Chitosan; D003692:Delayed-Action Preparations; D004317:Doxorubicin; D004337:Drug Carriers; D005966:Glucuronidase; D006493:Heparin; D000099175:Heparanase
keywords: Co-delivery; Microcapsules; Synergistic effect