title: Ursolic acid liposomes with chitosan modification: Promising antitumor drug delivery and efficacy.
abstract: There are tremendous challenges on antitumor and its therapeutic drugs, and preparation of highly efficient nano-vehicles represents one of the novel topics in antitumor pharmaceutical field. Herein, the novel chitosan-coated ursolic acid (UA) liposome (CS-UA-L) was efficiently prepared with highly tumor targeting, drug controlled release and low side-effect. The CS-UA-L was uniformly spherical particles with diameter of ~130nm, and the size was more easily trapped into the tumor tissues. Chitosan modification can make liposomes carrying positive charges, which were inclined to combine with the negative charges on the surface of tumor cells, and then the CS-UA-L could release UA rapidly at pH5.0 comparing with pH7.4. Meanwhile, the CS-UA-L exhibited obvious anti-proliferative effect (76.46%) on HeLa cells and significantly antitumor activity (61.26%) in mice bearing U14 cervical cancer. The tumor tissues of CS-UA-L treated mice had enhanced cell apoptosis, extensive necrosis and low cell proliferation activity. These results demonstrated that the multifunctional CS-UA-L allowed a precision treatment for localized tumor, and reducing the total drug dose and side-effect, which hold a great promise in new safe and effective tumor therapy.
authors.affiliation: Applying Chemistry Key Lab of Hebei Province, Yanshan University, No.438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Meili
authors.initials: M
authors.lastname: Wang
authors.affiliation: Applying Chemistry Key Lab of Hebei Province, Yanshan University, No.438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Tingting
authors.initials: T
authors.lastname: Zhao
authors.affiliation: Applying Chemistry Key Lab of Hebei Province, Yanshan University, No.438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Yanping
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Applying Chemistry Key Lab of Hebei Province, Yanshan University, No.438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Qianqian
authors.initials: Q
authors.lastname: Wang
authors.affiliation: Applying Chemistry Key Lab of Hebei Province, Yanshan University, No.438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Shanshan
authors.initials: S
authors.lastname: Xing
authors.affiliation: Applying Chemistry Key Lab of Hebei Province, Yanshan University, No.438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Lei
authors.initials: L
authors.lastname: Li
authors.affiliation: Applying Chemistry Key Lab of Hebei Province, Yanshan University, No.438 Hebei Street, Qinhuangdao 066004, China.
authors.forename: Longgang
authors.initials: L
authors.lastname: Wang
authors.affiliation: The First Hospital of Qinhuangdao, No. 258 Cultural Road, Qinhuangdao 066000, China.
authors.forename: Lanxiang
authors.initials: L
authors.lastname: Liu
authors.affiliation: Applying Chemistry Key Lab of Hebei Province, Yanshan University, No.438 Hebei Street, Qinhuangdao 066004, China. Electronic address: dwgao@ysu.edu.cn.
authors.forename: Dawei
authors.initials: D
authors.lastname: Gao
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D048271:Chitosan / Q000737:chemistry / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008081:Liposomes; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology; D023041:Xenograft Model Antitumor Assays; D000097245:Ursolic Acid
chemical_list: D000970:Antineoplastic Agents; D048271:Chitosan; D008081:Liposomes; D014315:Triterpenes; D000097245:Ursolic Acid
keywords: Antitumor; Chitosan; Liposomes; Ursolic acid; pH-responsive release