Formulation, characterization and pharmacokinetics of praziquantel-loaded hydrogenated castor oil solid lipid nanoparticles

被引:47
作者
Xie, Shuyu [1 ]
Pan, Baoliang [1 ]
Wang, Ming [1 ]
Zhu, Luyan [1 ]
Wang, Fenghua [1 ]
Dong, Zhao [1 ]
Wang, Xiaofang [1 ]
Zhou, WenZhong [1 ]
机构
[1] China Agr Univ, Dept Vet Prevent Med, Coll Vet Med, Beijing, Peoples R China
关键词
bioavailability; pharmacokinetics; praziquantel; solid lipid; nanoparticles; systemic circulation; SCHISTOSOMA-MANSONI; ORAL BIOAVAILABILITY; DRUG-DELIVERY; IN-VITRO; SOLUBLE DRUGS; IMPROVEMENT; RESISTANCE; CIMETIDINE; TOXICITY; CARRIERS;
D O I
10.2217/NNM.10.42
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
The purpose of this study was to formulate praziquantel (PZQ)-loaded hydrogenated castor oil (HCO) solid lipid nanoparticles (SLN) to enhance the bioavailability and prolong the systemic circulation of the drug. Materials & methods: PZQ was encapsulated into HCO nanoparticles by a hot homogenization and ultrasonication method. The physicochemical characteristics of SLN were investigated by optical microscope, scanning electron microscopy and photon correlation spectroscopy. Pharmacokinetics were studied after oral, subcutaneous and intramuscular administration in mice. Results: The diameter, polydispersivity index, zeta potential, encapsulation efficiency and loading capacity of the nanoparticles were 344.0 +/- 15.1 nm, 0.31 +/- 0.08, -16.7 +/- 0.5 mV, 62.17 +/- 6.53% and 12.43 +/- 1.31%, respectively. In vitro release of PZQ-loaded HCO-SLN exhibited an initial burst release followed by a sustained release. SLN increased the bioavailability of PZQ by 14.9-, 16.1- and 2.6-fold, and extended the mean residence time of the drug from 7.6, 6.6 and 8.2 to 95.9, 151.6 and 48.2 h after oral, subcutaneous and intramuscular administration, respectively. Conclusion: The PZQ-loaded HCO-SLN could be a promising formulation to enhance the pharmacological activity of PZQ.
引用
收藏
页码:693 / 701
页数:9
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