title: Antitumor drug effect of betulinic acid mediated by polyethylene glycol modified liposomes.
abstract: Betulinic acid (BA), as a natural pentacyclic lupine-type triterpene, principally derives from bark of white birch, due to its potent pharmacological properties and low side-effect, which has been demonstrated a prominent efficiency on cancer therapy. However, the poor solubility and low bioavailability limit its pharmaceutical effect. Herein, we reported the rapid efficient synthesis of the polyethylene glycol modified (PEGylated) BA liposomes using ethanol injection technique for the first time. In the study, hydrophobic BA was encapsulated in the lipid bilayer of liposomes, meanwhile hydrophilic PEG layer covered the surface of liposomes. The mean diameter of PEGylated BA liposomes was 142nm, which can effectively accumulate in the tumor tissues. In vitro drug release study showed that the PEGylated BA liposomes had a better sustained drug release effect than BA liposomes. The PEGylated BA liposomes also exhibited a better tumor inhibitory effect compared with those of free BA or BA liposomes in vitro and in vivo experiments. Therefore, the PEGylated BA liposomes could serve as a better alternative for the cancer therapy in future.
authors.affiliation: Chemical Key Lab of Hebei Province, Department of Biological Engineering, Yanshan University, No. 438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Yanping
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Chemical Key Lab of Hebei Province, Department of Biological Engineering, Yanshan University, No. 438 Hebei Street, Qinhuangdao 066004, China. Electronic address: dwgao@ysu.edu.cn.
authors.forename: Dawei
authors.initials: D
authors.lastname: Gao
authors.affiliation: Chemical Key Lab of Hebei Province, Department of Biological Engineering, Yanshan University, No. 438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Xuwu
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Chemical Key Lab of Hebei Province, Department of Biological Engineering, Yanshan University, No. 438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Zhiwei
authors.initials: Z
authors.lastname: Liu
authors.affiliation: Chemical Key Lab of Hebei Province, Department of Biological Engineering, Yanshan University, No. 438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Kun
authors.initials: K
authors.lastname: Dai
authors.affiliation: Chemical Key Lab of Hebei Province, Department of Biological Engineering, Yanshan University, No. 438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Bingshuo
authors.initials: B
authors.lastname: Ji
authors.affiliation: Chemical Key Lab of Hebei Province, Department of Biological Engineering, Yanshan University, No. 438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Qianqian
authors.initials: Q
authors.lastname: Wang
authors.affiliation: Chemical Key Lab of Hebei Province, Department of Biological Engineering, Yanshan University, No. 438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Liyao
authors.initials: L
authors.lastname: Luo
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D008081:Liposomes; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D053978:Pentacyclic Triterpenes; D011092:Polyethylene Glycols / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D014315:Triterpenes / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000094062:Betulinic Acid
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D008081:Liposomes; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D011092:Polyethylene Glycols; C000595209:polyethylene glycol 1000; D000094062:Betulinic Acid
keywords: Antitumor; Betulinic acid; Liposome; Polyethylene glycol; Sustained release