title: PEGylated non-ionic surfactant vesicles as drug delivery systems for Gambogenic acid.
abstract: Gambogenic acid (GNA), a popular Chinese traditional medicine, has its limitations of coming into use due to its low aqueous solubility and poor bioavailability. In this study, therefore, the PEGylated non-ionic surfactant vesicles drug delivery systems were prepared from biocompatible non-ionic surfactant of Span60, cholesterol and dicetyl phosphate (DCP) by the improved ethanol injection method, and were modified with a polyethylene glycol monostearate15 (PEG15-SA). PEG15-SA, as a biocompatible, non-toxic and non-immunogenic hydrophilic segment, was grafted onto the surface of colloidal niosomes carries to reduce the uptake by the reticuloendothelial system (RES), prolonging the circulation time and attaining higher entrapment efficiency. To our knowledge, this work is the first to report that PEG15-SA was applied to coating of niosomes for encapsulation of GNA. The optimized PEG-GNA-NISVs (P-GNA-NISVs) were characterized in terms of mean vesicles size, polydispersity index (PDI), Zeta potential and entrapment efficiency of the P-GNA-NISVs. The results showed that the mean diameter, PDI, Zeta potential, and the entrapment efficiency of the P-GNA-NISVs were 70.1 nm, 0.166, -44.3 mV and 87.74%, respectively. Furthermore, the release studies of GNA from PEGylated niosomes in vitro and the pharmacokinetics in vivo exhibited a prolonged release profile as studied over 24 h. In conclusion, the result suggests that P-GNA-NISVs prepared in this way not only have higher encapsulation capacity, more colloidal stability but also offer an approach that the PEGylated niosomes is a promising carrier for anticancer GNA.
authors.affiliation: The Pharmacokinetics Lab, Anhui University of Chinese Medicine , Hefei 230038 , China.
authors.forename: Tongyuan
authors.initials: T
authors.lastname: Lin
authors.forename: Qingying
authors.initials: Q
authors.lastname: Fang
authors.forename: Daiyin
authors.initials: D
authors.lastname: Peng
authors.forename: Xia
authors.initials: X
authors.lastname: Huang
authors.forename: Tingting
authors.initials: T
authors.lastname: Zhu
authors.forename: Qing
authors.initials: Q
authors.lastname: Luo
authors.forename: Kai
authors.initials: K
authors.lastname: Zhou
authors.forename: Weidong
authors.initials: W
authors.lastname: Chen
mesh_terms: D000818:Animals; D001682:Biological Availability; D002784:Cholesterol / Q000737:chemistry; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D004355:Drug Stability; D005260:Female; D006601:Hexoses / Q000737:chemistry; D008081:Liposomes; D008297:Male; D008516:Medicine, Chinese Traditional; D012157:Mononuclear Phagocyte System / Q000378:metabolism; D010755:Organophosphates / Q000737:chemistry; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D051381:Rats; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*; D013729:Terpenes / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D014966:Xanthenes; D044004:Xanthones / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D006601:Hexoses; D008081:Liposomes; D010755:Organophosphates; D013501:Surface-Active Agents; D013729:Terpenes; D014966:Xanthenes; D044004:Xanthones; C002290:dicetylphosphate; D011092:Polyethylene Glycols; C009314:polyethylene glycol monostearate; C045863:neo-gambogic acid; D002784:Cholesterol; C009298:sorbitan monostearate