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


METHODS
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.


RESULTS
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).


CONCLUSIONS
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.
Zhou
Zhao-xiong
ZX
Department of Vascular Surgery, Shanghai Renji Hospital, Affiliated with the Shanghai Jiaotong University School of Medicine, Shanghai, China.
Zhang
Bai-gen
BG
Zhang
Hao
H
Huang
Xiao-zhong
XZ
Hu
Ya-li
YL
Sun
Li
L
Wang
Xiao-min
XM
Zhang
Ji-wei
JW
D017209:Apoptosis / Q000187:drug effects; D002465:Cell Movement / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D003907:Dexamethasone / Q000008:administration & dosage / Q000031:analogs & derivatives*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D005466:Fluorocarbons / Q000737:chemistry*; D006801:Humans; D009131:Muscle, Smooth, Vascular / Q000166:cytology / Q000187:drug effects; D032389:Myocytes, Smooth Muscle / Q000187:drug effects / Q000378:metabolism; D053758:Nanoparticles; D010316:Particle Size; D014469:Umbilical Arteries / Q000166:cytology / Q000378:metabolism
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005466:Fluorocarbons; C004180:dexamethasone 21-phosphate; D003907:Dexamethasone; C018038:dexamethasone acetate