title: Sulfatide-containing lipid perfluorooctylbromide nanoparticles as paclitaxel vehicles targeting breast carcinoma.
abstract: Targeted nanoparticle (NP) delivery vehicles are emerging technologies, the full potential of which has yet to be realized. Sulfatide is known to bind to extracellular matrix glycoproteins that are highly expressed in breast tumors. In this study, we report for the first time the combination of sulfatide and lipid perfluorooctylbromide NPs as a targeted breast cancer delivery vehicle for paclitaxel (PTX). PTX-sulfatide-containing lipid perfluorooctylbromide NPs (PTX-SNPs) were prepared using the emulsion/solvent evaporation method. PTX-SNPs exhibited a spherical shape, small particle size, high encapsulation efficiency, and a biphasic release in phosphate-buffered solution. The cytotoxicity study and cell apoptosis assay revealed that blank sulfatide-containing lipid perfluorooctylbromide NPs (SNPs) had no cytotoxicity, whereas PTX-SNPs had greater EMT6 cytotoxicity levels than PTX-lipid perfluorooctylbromide NPs (PTX-NPs) and free PTX. An in vitro cellular uptake study revealed that SNPs can deliver greater amounts of drug with more efficient and immediate access to intracellular targets. In vivo biodistribution measured using high-performance liquid chromatography confirmed that the PTX-SNPs can target breast tumor tissues to increase the accumulation of PTX in these tissues. The in vivo tumor inhibition ability of PTX-SNPs was remarkably higher than PTX-NPs and free PTX. Furthermore, toxicity studies suggested that the blank SNPs had no systemic toxicity. All results suggested that SNPs may serve as efficient PTX delivery vehicles targeting breast carcinoma.
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou, People's Republic of China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Li
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou, People's Republic of China.
authors.forename: Fei
authors.initials: F
authors.lastname: Qin
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou, People's Republic of China.
authors.forename: Li
authors.initials: L
authors.lastname: Yang
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou, People's Republic of China.
authors.forename: Liqian
authors.initials: L
authors.lastname: Mo
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou, People's Republic of China.
authors.forename: Lei
authors.initials: L
authors.lastname: Li
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou, People's Republic of China.
authors.forename: Lianbing
authors.initials: L
authors.lastname: Hou
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry* / Q000494:pharmacology; D005260:Female; D005466:Fluorocarbons / Q000737:chemistry / Q000494:pharmacology; D006842:Hydrocarbons, Brominated; D008325:Mammary Neoplasms, Experimental / Q000378:metabolism* / Q000473:pathology; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000737:chemistry*; D017239:Paclitaxel / Q000737:chemistry* / Q000494:pharmacology; D013433:Sulfoglycosphingolipids / Q000737:chemistry* / Q000494:pharmacology; D014018:Tissue Distribution
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D005466:Fluorocarbons; D006842:Hydrocarbons, Brominated; D013433:Sulfoglycosphingolipids; D017239:Paclitaxel; C003072:perflubron
keywords: antitumor efficacy; drug delivery; paclitaxel; perfluorooctylbromide nanoparticles; targeting