1.Department of Pharmacy, The First Hospital of Lanzhou University, Lanzhou 730000, China; 2.College of Pharmacy , Lanzhou University, Lanzhou 730000 ,China
OBJECTIVE To prepare diazepam solid lipid nanoparticles, evaluate the pharmacy characters and study the pharmacokinetics after intranasal administration. METHODS Diazepam solid lipid nanoparticles were prepared by high temperature emulsification-low temperature solidification method. The entrapment efficiency, particle size distrubtion, Zeta potential and morphology were measured. After administrating solid lipid nanoparticles in intranasal routes or diazepam parenteral solution via intravenous, the blood samples were collected from the femoral artery. Drug concentration in plasma were analyzed by HPLC method. The concentration-time curves were obtained, and pharmacokinetic parameters were obtained by DAS 1.0. RESULTS The morphology of diazepam solid lipid nanoparticles obtained were appoximately spherical. The average particle size was (104.4±0.56 nm. The Zeta potential was (-18.50±0.98 mV. Encapsulating efficiency was(98.8±3%. After intranasal aministration of diazepam solid lipid nanoparticles, tmax was 11 min, ρmax was (0.33±0.01 μg·mL-1, and the absolute bioavailability was 67.01%. CONCLUSION The rapid absorption and high absolute bioavailability were obtained after nasal administration of diazepam solid lipid nanoparticle. It is a promising approach for the treatment of status epilepticus.
M Li;WEI Yu-hui;DUN Ho-gng;WU Qin-yun;ZHNG Jin-qing;WU Xin-n.
Preparation of Diazepam Solid Lipid Nanoparticles and Its Pharmacokinetics after Intranasal Administration in Rats[J]. Chinese Pharmaceutical Journal, 2011, 46(1): 44-47
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