[In vitro and in vivo study of two kinds of long-circulating solid lipid nanoparticles containing paclitaxel].
OBJECTIVE
To prepare long-circulating solid lipid nanoparticles containing paclitaxel with stearic acid, and investigate the in vitro and in vivo characterization of nanoparticles.


METHODS
The method of "emulsion evaporation-solidification at low temperature" was used to prepare the stearic acid solid lipid nanoparticles containing paclitaxel. Its morphology was examined by transmission electron microscope. The HPLC method for determination of paclitaxel in nanoparticles or serum samples was established. The release of paclitaxel in vitro and the pharmacokinetics after i.v. bolus injection to mice were studied.


RESULTS
The mean diameter of Brij78-SLN and F68-SLN is (103.5 +/- 29.2) nm and (220 +/- 98) nm, respectively. The nanoparticles release paclitaxel slowly and linearly, within 24 h, Brij78-SLN and F68-SLN release 8% and 20% of total drug, respectively. Long-circulation nanoparticles was found to stay in the blood circulation, with T 1/2 beta 10.1 h of F68-SLN, and T 1/2 beta 4.88 h of Brij78-SLN more than one commercialized paclitaxel injection, T 1/2 beta 1.3 h.


CONCLUSIONS
Stearic acid might be a new drug carrier material in the future.
Chen
Da-bing
DB
Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.
Yang
Tian-zhi
TZ
Lu
Wang-liang
WL
Zhang
Qiang
Q
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D051379:Mice; D036103:Nanotechnology; D017239:Paclitaxel / Q000008:administration & dosage* / Q000493:pharmacokinetics; D010316:Particle Size; D010714:Phosphatidylethanolamines; D011092:Polyethylene Glycols; D011897:Random Allocation; D013229:Stearic Acids / Q000737:chemistry*
D000972:Antineoplastic Agents, Phytogenic; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D010714:Phosphatidylethanolamines; D013229:Stearic Acids; C107570:polyethylene glycol-distearoylphosphatidylethanolamine; D011092:Polyethylene Glycols; C031183:stearic acid; D017239:Paclitaxel