title: Formulation and evaluation of celastrol-loaded liposomes.
abstract: The main purpose of this study was to evaluate the intestinal absorption and the antineoplastic effect of the poorly water-soluble drug celastrol when liposomes were used as oral drug delivery system. Liposomes were prepared by the ethanol-injection method. An optimized liposome formulation composed of phospholipid, cholesterol and Tween-80 resulted in favorable encapsulation efficiency at 98.06 ± 0.94%. Homogeneous and stable particle size of 89.6 ± 7.3 nm and zeta potential of -(87.7 ± 5.8) mV were determined by laser particle size analyzer. Subsequently, the four-site perfusion rat intestinal model revealed that celastrol-loaded liposomes had improved effective permeability compared to the free drug in four intestinal segments (p < 0.05). Moreover, celastrol-loaded liposomes could also inhibit the tumor growth in C57BL/6 mice. These results suggest that liposomes could be a promising perioral carrier for celastrol.
authors.affiliation: Key Laboratory of Delivery Systems of Chinese Meteria Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing 210028, Jiangsu, China. jxiaobin2005@hotmail.com
authors.forename: Jie
authors.initials: J
authors.lastname: Song
authors.forename: Feng
authors.initials: F
authors.lastname: Shi
authors.forename: Zhenhai
authors.initials: Z
authors.lastname: Zhang
authors.forename: Fenxia
authors.initials: F
authors.lastname: Zhu
authors.forename: Jing
authors.initials: J
authors.lastname: Xue
authors.forename: Xiaobin
authors.initials: X
authors.lastname: Tan
authors.forename: Luyong
authors.initials: L
authors.lastname: Zhang
authors.forename: Xiaobin
authors.initials: X
authors.lastname: Jia
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000494:pharmacology; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy* / Q000473:pathology; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems / Q000379:methods*; D007408:Intestinal Absorption / Q000187:drug effects; D007422:Intestines / Q000187:drug effects; D008081:Liposomes / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry; D008297:Male; D008516:Medicine, Chinese Traditional; D051379:Mice; D008810:Mice, Inbred C57BL; D053978:Pentacyclic Triterpenes; D010477:Perfusion / Q000379:methods; D051381:Rats; D017207:Rats, Sprague-Dawley; D014315:Triterpenes / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D008081:Liposomes; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; C050414:celastrol