title: Self-assembly and cytotoxicity study of PEG-modified ursolic acid liposomes.
abstract: While ursolic acid (UA), one of the most broadly known triterpene compounds, has proved to be effective in cancer therapy, the applications of UA is limited due to its poor aqueous solubility and low bioavailability. The aim of our study was to prolong circulation time and enhance uptake of liposomes in tumor tissues through the modification of UA liposomes via water-soluble polyethylene glycol (PEG). In addition, this research also focuses on physicochemical properties of the liposome formulations, including encapsulation efficiency, particle morphology, size, stability, release rate in vitro and cytotoxicity test. The obtained liposomes were spherical particles with mean particle diameters around 100-200 nm. And the Fourier transform infrared spectroscopy (FTIR) indicated that PEG had been anchored successfully to the liposomes. Based on our experimental data achieved, PEG-modified UA liposomes possessed higher stability than conventional liposomes, and the release rate of UA from PEG-modified liposomes was slower when compared with those of UA solution and conventional liposomes. Meanwhile, the liposomal UA showed relatively low cytotoxic effect than UA conventional liposomes within 24h, which was consistent with their release rates.
authors.affiliation: Chemical Key Lab of Hebei Province, Department of Biological Engineering, Yanshan University, No. 438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Tingting
authors.initials: T
authors.lastname: Zhao
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: Department of Surgery, Beijing Ditan Hospital, Beijing, China.
authors.forename: Zhengrong
authors.initials: Z
authors.lastname: Gao
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: Nan
authors.initials: N
authors.lastname: Li
authors.affiliation: Chemical Key Lab of Hebei Province, Department of Biological Engineering, Yanshan University, No. 438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Yanhong
authors.initials: Y
authors.lastname: Bian
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: Zhiwei
authors.initials: Z
authors.lastname: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000633:toxicity; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004355:Drug Stability; D006801:Humans; D008081:Liposomes / Q000737:chemistry* / Q000633:toxicity*; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000633:toxicity*; D014315:Triterpenes / Q000737:chemistry* / Q000633:toxicity*; D000097245:Ursolic Acid
chemical_list: D000970:Antineoplastic Agents; D008081:Liposomes; D011092:Polyethylene Glycols; D014315:Triterpenes; D000097245:Ursolic Acid
keywords: Long circulation; MTT assay; PEG-modified liposomes; Ursolic acid