title: Baicalin loaded in folate-PEG modified liposomes for enhanced stability and tumor targeting.
abstract: Bioavailability of baicalin (BAI), an example of traditional Chinese medicine, has been modified by loading into liposome. Several liposome systems of different composition i.e., lipid/cholesterol (L), long-circulating stealth liposome (L-PEG) and folate receptor (FR)-targeted liposome (L-FA) have been used as the drug carrier for BAI. The obtained liposomes were around 80 nm in diameter with proper zeta potentials about -25 mV and sufficient physical stability in 3 months. The entrapment efficiency and loading efficiency of BAI in the liposomes were 41.0-46.4% and 8.8-10.0%, respectively. The morphology details of BAI lipsosome systems i.e., formation of small unilamellar vesicles, have been determined by cryogenic transmission electron microscopy (cryo-TEM) and small angle X-ray scattering (SAXS). In vitro cytotoxicity of BAI liposomes against HeLa cells was evaluated by MTT assay. BAI loaded FR-targeted liposomes showed higher cytotoxicity and cellular uptake compared with non-targeted liposomes. The results suggested that L-FA-BAI could enhance anti-tumor efficiency and should be an effective FR-targeted carrier system for BAI delivery.
authors.affiliation: State Key Laboratory of Bioreactor Engineering & Shanghai Key Laboratory of Functional Materials Chemistry, East China University of Science and Technology, Shanghai 200237, PR China.
authors.forename: Yiyin
authors.initials: Y
authors.lastname: Chen
authors.affiliation: State Key Laboratory of Bioreactor Engineering & Shanghai Key Laboratory of Functional Materials Chemistry, East China University of Science and Technology, Shanghai 200237, PR China; NTT Institute of Hi-Technology (NIH), Nguyen Tat Thanh University, Ho Chi Minh City, Viet Nam.
authors.forename: Le Van
authors.initials: LV
authors.lastname: Minh
authors.affiliation: State Key Laboratory of Bioreactor Engineering & Shanghai Key Laboratory of Functional Materials Chemistry, East China University of Science and Technology, Shanghai 200237, PR China.
authors.forename: Jianwen
authors.initials: J
authors.lastname: Liu
authors.affiliation: Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, Heyrovsky Sq. 2, CZ-16206 Prague, Czech Republic.
authors.forename: Borislav
authors.initials: B
authors.lastname: Angelov
authors.affiliation: Laboratory for Soft Matter Electron Microscopy, Bayreuth Institute of Macromolecular Research (BIMF), University of Bayreuth, D-95440, Bayreuth, Germany.
authors.forename: Markus
authors.initials: M
authors.lastname: Drechsler
authors.affiliation: Helmholtz-Zentrum Geesthacht: Centre for Materials and Coast Research, Institute of Materials Research, Max-Planck-Str. 1, D-21502 Geesthacht, Germany.
authors.forename: Vasil M
authors.initials: VM
authors.lastname: Garamus
authors.affiliation: Helmholtz-Zentrum Geesthacht: Centre for Materials and Coast Research, Institute of Materials Research, Max-Planck-Str. 1, D-21502 Geesthacht, Germany.
authors.forename: Regine
authors.initials: R
authors.lastname: Willumeit-Römer
authors.affiliation: State Key Laboratory of Bioreactor Engineering & Shanghai Key Laboratory of Functional Materials Chemistry, East China University of Science and Technology, Shanghai 200237, PR China. Electronic address: aihuazou@ecust.edu.cn.
authors.forename: Aihua
authors.initials: A
authors.lastname: Zou
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D020285:Cryoelectron Microscopy; D065546:Drug Liberation; D004355:Drug Stability; D005260:Female; D005419:Flavonoids / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D058973:Folate Receptors, GPI-Anchored / Q000037:antagonists & inhibitors / Q000378:metabolism; D005492:Folic Acid / Q000031:analogs & derivatives* / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D008081:Liposomes / Q000737:chemistry* / Q000648:ultrastructure; D018613:Microscopy, Confocal; D046529:Microscopy, Electron, Transmission; D011092:Polyethylene Glycols / Q000737:chemistry*; D053838:Scattering, Small Angle; D002583:Uterine Cervical Neoplasms / Q000378:metabolism / Q000473:pathology; D014961:X-Ray Diffraction
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D005419:Flavonoids; D058973:Folate Receptors, GPI-Anchored; D008081:Liposomes; C552831:poly(ethylene glycol)-folate; C038044:baicalin; D011092:Polyethylene Glycols; D005492:Folic Acid
keywords: Baicalin; Cryo-TEM; Folate receptor; Liposomes; SAXS; Targeting drug delivery