Lung-targeting delivery of dexamethasone acetate loaded solid lipid nanoparticles.
The objective of the present study was to develop a novel solid lipid nanoparticle (SLN) for the lung-targeting delivery of dexamethasone acetate (DXM) by intravenous administration. DXM loaded SLN colloidal suspensions were prepared by the high pressure homogenization method. The mean particle size, drug loading capacity and drug entrapment efficiency (EE%) of SLNs were investigated. In vitro drug release was also determined. The biodistribution and lung-targeting efficiency of DXM-SLNs and DXM-solutions (DXM-sol) in mice after intravenous administration were studied using reversed-phase high-performance liquid chromatography (HPLC). The results (expressed as mean +/- SD) showed that the DXM-SLNs had an average diameter of 552 +/- 6.5 nm with a drug loading capacity of 8.79 +/- 0.04% and an entrapment efficiency of 92.1 +/- 0.41%. The in vitro drug release profile showed that the initial burst release of DXM from DXM-SLNs was about 68% during the first 2 h, and then the remaining drug was released gradually over the following 48 hours. The biodistribution of DXM-SLNs in mice was significantly different from that of DXM-sol. The concentration of DXM in the lung reached a maximum level at 0.5 h post DXM-SLNs injection. A 17.8-fold larger area under the curve of DXM-SLNs was achieved compared to that of DXM-sol. These results indicate that SLN may be promising lung-targeting drug carrier for lipophilic drugs such as DXM.
Xiang
Qing-yu
QY
Key Laboratory of Drug Targeting of Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, P.R. China.
Wang
Min-ting
MT
Chen
Fu
F
Gong
Tao
T
Jian
Yan-lin
YL
Zhang
Zhi-rong
ZR
Huang
Yuan
Y
D000818:Animals; D003692:Delayed-Action Preparations; D003907:Dexamethasone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D008055:Lipids / Q000008:administration & dosage*; D008168:Lung / Q000378:metabolism*; D051379:Mice; D053758:Nanoparticles; D012995:Solubility; D014018:Tissue Distribution
D003692:Delayed-Action Preparations; D008055:Lipids; D003907:Dexamethasone; C018038:dexamethasone acetate