Self-assembled filomicelles prepared from polylactide-poly(ethylene glycol) diblock copolymers for sustained delivery of cycloprotoberberine derivatives

Saudi Pharmaceutical Journal

Danqing Song¹  Suming Li²  Peng Yun³  Xue Liu⁴  Xin Shen⁴  Yangsheng Chen⁴  Feng Su⁵  Yanxiang Wang⁶ 

[1] Corresponding authors at: College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao 266042, China (F. Su). Institut Europeen des Membranes, UMR CNRS 5635, Universite de Montpellier, 34095 Montpellier, France (S. Li).;Institute of High Performance Polymers, Qingdao University of Science and Technology, Qingdao 266042, China;Peking Union Medical College, Beijing 100050, China;College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao 266042, China;Institute of High Performance Polymers, Qingdao University of Science and Technology, Qingdao 266042, China;;Institute of Medicinal Biotechnology, Chinese Academy of Medical Science &

关键词: Polymeric micelles;    Filomicelles;    PLA-PEG;    A35;    Drug delivery;   

DOI  :  10.1016/j.jsps.2018.01.008

来源: DOAJ

【 摘 要 】

Polylactide-poly(ethylene glycol) (PLA-PEG) block copolymers were synthesized by ring opening polymerization of l-lactide using a monomethoxy PEG (mPEG) as macroinitiator and zinc lactate as catalyst. The resulting diblock copolymers were characterized by 1H NMR and GPC. Polymeric micelles were prepared by self-assembly of copolymers in distilled water using co-solvent evaporation or membrane hydration methods. The resulting micelles are worm-like in shape as shown by TEM measurements. A hydrophobic anticancer drug, cycloprotoberberine derivative A35, was successfully loaded in PLA-PEG filomicelles with high encapsulation efficiency (above 88%). Berberine (BBR) was studied for comparison. In both methods, PLA-PEG filomicelles were prepared with a theoretical loading of 5%, 10% and 20%. Physical stability studies indicated that BBR/A35-loaded filomicelles were more stable when stored at 4 °C than at 25 °C. Compared with BBR-loaded filomicelles, A35-loaded filomicelles exhibited higher antitumor activity. Importantly, the in vitro cytotoxicity and stability of A35-loaded filomicelles evidenced the potential of drug-loaded filomicelles in the development of drug delivery systems.

【 授权许可】

Unknown