title: Hyaluronic acid-coated cationic nanostructured lipid carriers for oral vincristine sulfate delivery.
abstract: The goal of this research is to structure a hyaluronic acid modified nanostructured lipid carrier (HA-NLCs) for vincristine sulfate (VCR) delivery, and detect its efficiency to improve the oral bioavailability. Emulsion solvent evaporation method was used to prepare the HA-NLCs nanoparticles. The particle size, zeta potential and entrapment efficiency of VCR-NLCs and HA-NLCs were 187 ± 3.52 nm, -8.61 ± 1.29 mV, 33.12 ± 1.16% and 192 ± 4.41 nm, -32.82 ± 2.64 mV, 34.41 ± 2.21%, respectively. HA-NLCs could significantly improve the cellular uptake efficiency and cytotoxicity in MCF-7 cells than other VCR formulations. The expressions of apoptosis related protein Caspase-3, Caspase-9, Bax and Bcl-2 were estimated by western blot assay in MCF-7 cells, and HA-NLCs exhibited the strongest effect in promoting cell apoptosis. The pharmacokinetics of HA-NLCs was evaluated in Sprague-Dawley male rats and the relative oral bioavailability of HA-NLCs and VCR-NLCs was improved about 1.8-fold and two-fold compared with VCR solution, respectively. Therefore, these results indicated that HA-NLCs could significantly improve the oral bioavailability and was a promising vehicle for the oral delivery of VCR.
authors.affiliation: a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
authors.forename: Xuan
authors.initials: X
authors.lastname: Gao
authors.affiliation: a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
authors.forename: Jun
authors.initials: J
authors.lastname: Zhang
authors.affiliation: a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
authors.forename: Qiang
authors.initials: Q
authors.lastname: Xu
authors.affiliation: a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
authors.forename: Zun
authors.initials: Z
authors.lastname: Huang
authors.affiliation: a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
authors.forename: Yiyue
authors.initials: Y
authors.lastname: Wang
authors.affiliation: a School of Pharmacy, Shanghai Jiao Tong University , Shanghai , China.
authors.forename: Qi
authors.initials: Q
authors.lastname: Shen
mesh_terms: D000284:Administration, Oral; D000818:Animals; D051017:Apoptosis Regulatory Proteins / Q000378:metabolism; D001682:Biological Availability; D002412:Cations / Q000737:chemistry*; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry*; D004655:Emulsions / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D006820:Hyaluronic Acid / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry*; D061986:MCF-7 Cells; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D014750:Vincristine / Q000008:administration & dosage* / Q000737:chemistry* / Q000378:metabolism
chemical_list: D051017:Apoptosis Regulatory Proteins; D002412:Cations; D004337:Drug Carriers; D004655:Emulsions; D008055:Lipids; D014750:Vincristine; D006820:Hyaluronic Acid
keywords: Hyaluronic acid; cationic; nanostructured lipid carrier; oral bioavailability; vincristine sulfate