Targeted and pH-sensitive polyzwitterionic liposomes for oral anticancer drug delivery  

作　　者：Mingyang Hu Rui Zheng Qi Pan Chen Peng Xinyue Zhang Wei He Wenlong Yao Yan Li 

机构地区：[1]Beijing Key Laboratory for Bioengineering and Sensing Technology,School of Chemistry and Biological Engineering,University of Science and Technology Beijing,Beijing,100083,China [2]State Key Laboratory of Natural and Biomimetic Drugs,School of Pharmaceutical Sciences,Chemical Biology Center,Peking University,Beijing,100191,China [3]School of Materials Science and Engineering,University of Science and Technology Beijing,Beijing,100083,China

出　　处：《Particuology》2025年第3期13-20,共8页颗粒学报(英文版)

基　　金：financially supported by the Fundamental Research Funds for the Central Universities(grant No.06500230,FRF-BR-23-02B);the National Natural Science Foundation of China(grant No.32071391);the Interdisciplinary Research Project for Young Teachers of USTB(Fundamental Research Funds for the Central Universities,FRF-IDRY-23-019);the Beijing Nova Program(grant No.20230484423).

摘　　要：Compared to intravenous injection,oral administration is attractive due to its many advantages for cancer therapy.Taken physiological barriers and other profiles of oral anticancer drug carriers into consideration,targeted and pH-sensitive polyzwitterionic liposomes(ZL)based on zwitterionic poly(carboxybetaine)(PCB)were constructed for oral delivery of doxorubicin hydrochloride(DOX·HCl)for cancer therapy.The DOX-ZL with 40%trehalose had good lyophilization stability,which would be packaged into enteric capsules to enhance their stability in stomach.In addition,DOX-ZL exhibited good storage stability and serum stability.The DOX-ZL could achieve controlled release of DOX·HCl at the endosomal pH 5.0 due to the pH-sensitive of zwitterionic PCB.Importantly,DOX-ZL could targeted deliver DOX·HCl to Caco-2 cells to cross the intestinal epithelial cell layer.The empty ZL had good biocompatibility,while DOX-ZL significantly inhibited tumor cells growth due to their high cellular uptake and controlled drug release ability.Therefore,this work provided a promising approach for oral cancer therapy.

关 键 词：Polyzwitterionic liposomes Poly(carboxybetaine) Doxorubicin hydrochloride Oral administration Cancer therapy 

分 类 号：R943[医药卫生—药剂学]