title: High loading of hydrophilic/hydrophobic doxorubicin into polyphosphazene polymersome for breast cancer therapy.
abstract: Breast cancer remains one of the most common cancers for females. Drug delivery based on cancer nanotechnology could improve the performance of some chemotherapeutic medicines already used in clinic. The emergence of polymersomes provided the potential to encapsulate hydrophobic/hydrophilic drugs. By modifying the weight ratio of methoxy-poly (ethylene glycol) (mPEG) chain to ethyl-p-aminobenzoate (EAB) side group, a series of amphiphilic graft polyphosphazenes (PEPs) was prepared. PEP can be tuned from micelles to polymersomes with the decrease of mPEG content via dialysis. Either hydrophilic doxorubicin hydrochloride (DOX·HCl) or hydrophobic doxorubicin base (DOX) could be encapsulated into PEP polymersomes with high payload and high encapsulation efficiency due to the strong intermolecular interaction with PEP. Compared with free DOX·HCl administration, in vivo investigation in growth inhibition of MCF-7 xenograft tumors in nude mice demonstrated that PEP polymersomes could enhance life safety without compromise of therapeutic efficacy, especially DOX·HCl loaded delivery system.
  
  
  BACKGROUND
  In this preclinical study, polymerosomes based on PEPs were investigated as doxorubicin delivery systems, demonstrating similar efficacy but less toxicity compared to standard delivery methods.
authors: College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
authors: Jing
authors: J
authors: Xu
authors: College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
authors: Qinghe
authors: Q
authors: Zhao
authors: College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
authors: Yangmin
authors: Y
authors: Jin
authors: College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China. Electronic address: lyqiu@zju.edu.cn.
authors: Liyan
authors: L
authors: Qiu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage*; D001566:Benzocaine / Q000737:chemistry; D001835:Body Weight; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D004317:Doxorubicin / Q000737:chemistry*; D004337:Drug Carriers; D005260:Female; D005434:Flow Cytometry; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D008823:Micelles; D053758:Nanoparticles; D009368:Neoplasm Transplantation; D009943:Organophosphorus Compounds / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D009943:Organophosphorus Compounds; D011108:Polymers; C108974:poly(phosphazene); D011092:Polyethylene Glycols; D004317:Doxorubicin; D001566:Benzocaine
keywords: Cancer therapy; Doxorubicin; Drug resistance; Polymersomes; Polyphosphazene