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


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.


CONCLUSIONS
The PZQ-loaded HCO-SLN could be a promising formulation to enhance the pharmacological activity of PZQ.
Xie
Shuyu
S
Department of Preventive Veterinary Medicine, College of Veterinary Medicine, China Agricultural University, 2 Yuanmingyuan Road West, Beijing 100193, PR China.
Pan
Baoliang
B
Wang
Ming
M
Zhu
Luyan
L
Wang
Fenghua
F
Dong
Zhao
Z
Wang
Xiaofang
X
Zhou
WenZhong
W
D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage* / Q000097:blood*; D001682:Biological Availability; D002368:Castor Oil / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D008055:Lipids / Q000737:chemistry; D008297:Male; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D011223:Praziquantel / Q000008:administration & dosage* / Q000097:blood*
D000871:Anthelmintics; D004337:Drug Carriers; D008055:Lipids; D011223:Praziquantel; D002368:Castor Oil