title: Doxorubicin-loaded biodegradable self-assembly zein nanoparticle and its anti-cancer effect: Preparation, in vitro evaluation, and cellular uptake.
abstract: Cancer is one top leading cause of the deaths worldwide. Various anticancer drugs, which can effectively kill cancer cells, have been developed in the last decade. However, the problem is still about the low therapeutic index of the drugs, which means that the effective dose of drugs will cause cytotoxicity to normal cells. A strategy based on drug nano-encapsulation is applied to achieve an effective anti-cancer therapy. In this study, we use zein, which is an amphiphilic protein, to make the anti-cancer drug nano-encapsulation. Doxorubicin (DOX), a popular anti-cancer drug, is selected as the core drug. The results show that DOX could be successfully encapsulated into zein to form spherical nanoparticles. The encapsulation efficiency and loading efficiency could reach as high as 90.06% and 15.01 mg/g, respectively. The cumulative release result showed a desired pH-responsible release behavior: DOX could be released faster in acidic buffer solutions (pH 5.0 and 6.5) than neutral one (pH 7.4). The effects of the nano-encapsulation on the anti-proliferation of HeLa cells were also examined. It indicated that, compared with free DOX, the DOX-loaded zein nanoparticles (DOX-zein-NPs) had a better effect on cancer cell killing at low DOX concentrations. We also investigated the cellular uptake of DOX-zein-NPs using confocal laser scanning microscopy (CLSM), flow cytometry, and transmission electron microscopy (TEM). And the endocytosis mechanism of DOX-zein-NPs entering into HeLa cells was studied using various endocytosis pathway inhibitors.
authors.affiliation: Shenzhen Key Laboratory of Food Biological Safety Control, Shenzhen, PRC; Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Hum, Kowloon, Hong Kong Special Administrative Region. Electronic address: fangyuan.dong@polyu.edu.hk.
authors.forename: Fangyuan
authors.initials: F
authors.lastname: Dong
authors.affiliation: Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Hum, Kowloon, Hong Kong Special Administrative Region. Electronic address: xiaoli.dong@polyu.edu.hk.
authors.forename: Xiaoli
authors.initials: X
authors.lastname: Dong
authors.affiliation: Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Hum, Kowloon, Hong Kong Special Administrative Region. Electronic address: liping.zhou@connect.polyu.hk.
authors.forename: Liping
authors.initials: L
authors.lastname: Zhou
authors.affiliation: Shenzhen Key Laboratory of Food Biological Safety Control, Shenzhen, PRC. Electronic address: irene.xiao@polyu.edu.hk.
authors.forename: Huihui
authors.initials: H
authors.lastname: Xiao
authors.affiliation: Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Hum, Kowloon, Hong Kong Special Administrative Region. Electronic address: nicole.py.ho@connect.polyu.hk.
authors.forename: Pui-Yu
authors.initials: PY
authors.lastname: Ho
authors.affiliation: Shenzhen Key Laboratory of Food Biological Safety Control, Shenzhen, PRC; Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Hum, Kowloon, Hong Kong Special Administrative Region. Electronic address: bcmswong@polyu.edu.hk.
authors.forename: Man-Sau
authors.initials: MS
authors.lastname: Wong
authors.affiliation: Shenzhen Key Laboratory of Food Biological Safety Control, Shenzhen, PRC; Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Hum, Kowloon, Hong Kong Special Administrative Region. Electronic address: yi.wy.wang@polyu.edu.hk.
authors.forename: Yi
authors.initials: Y
authors.lastname: Wang
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D004339:Drug Compounding / Q000379:methods; D065546:Drug Liberation; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D018613:Microscopy, Confocal; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D015028:Zein / Q000737:chemistry*
chemical_list: D000903:Antibiotics, Antineoplastic; D004317:Doxorubicin; D015028:Zein
keywords: Cellular uptake; Doxorubicin; Drug delivery; Nano-encapsulation; Zein