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  • Drug packaging and delivery using perfluorocarbon nanoparticles for targeted inhibition of vascular smooth muscle cells.

Drug packaging and delivery using perfluorocarbon nanoparticles for targeted inhibition of vascular smooth muscle cells.

Acta pharmacologica Sinica (2009-11-06)
Zhao-xiong Zhou, Bai-gen Zhang, Hao Zhang, Xiao-zhong Huang, Ya-li Hu, Li Sun, Xiao-min Wang, Ji-wei Zhang
ABSTRACT

To investigate the in vitro release profile of drugs encapsulated within perfluorocarbon (PFC) nanoparticles (NPs) and their ability to inhibit the activity of vascular smooth muscle cells (SMCs). Dexamethasone phosphate (DxP) or dexamethasone acetate (DxA) was encapsulated into PFC nanoparticles using a high-pressure homogenous method. The morphology and size of the NPs were examined using scanning electron microscopy (SEM) and a laser particle size analyzer. Drug loading and in vitro release were assessed by high-performance liquid chromatography (HPLC). The impact of NP capsules on SMC proliferation, migration and apoptosis in vitro was assessed using cell counting kit-8, transwell cell migration and flow cytometry assays. The sizes of DxP-NPs and DxA-NPs were 224+/-6 nm and 236+/-9 nm, respectively. The encapsulation efficiency (EE) of DxP-NPs was 66.4%+/-1.0%, with an initial release rate of 77.2%, whereas the EE of DxA-NPs was 95.3%+/-1.3%, with an initial release rate of 23.6%. Both of the NP-coated drugs could be released over 7 d. Human umbilical artery SMCs were harvested and cultured for four to six passages. Compared to free DxP, SMCs treated with tissue factor (TF)-directed DxP-NPs showed significant differences in the inhibition of proliferation, migration and apoptosis (P<0.05). The results collectively suggest that PFC nanoparticles will be beneficial for targeted drug delivery because of the sustained drug release and effective inhibition of SMC proliferation and migration.

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Sigma-Aldrich
Dexamethasone 21-acetate, ≥99%
Dexamethasone acetate, European Pharmacopoeia (EP) Reference Standard