TITLE:
In Vivo Pharmacokinetic and Hemocompatible Evaluation of Lyophilization Induced Nifedipine Solid-Lipid Nanoparticle
AUTHORS:
Ranjan Kumar Barman, Yasunori Iwao, Md. Rafiqul Islam, Yuka Funakoshi, Shuji Noguchi, Mir Imam Ibne Wahed, Shigeru Itai
KEYWORDS:
Nifedipine, Solid-Lipid Nanoparticles, Lyophilization, Pharmacokinetics, Hemocompatibility
JOURNAL NAME:
Pharmacology & Pharmacy,
Vol.5 No.5,
May
13,
2014
ABSTRACT: Nifedipine-solid-lipid
nanoparticles lyophilized with trehalose (NI-SLN-Tre) were prepared by the high
pressure homogenization of a roll mixture consisting of NI and hydrogenated
soybean phosphatidylcholine and dipalmitoylphosphatidylglycerol, and in vivo pharmacokinetic properties and
their hemocompatibility were determined and compared with those of a NI-SLN
suspension. The resulting pharmacokinetic data demonstrated that although no
significant differences were observed between the time of peak concentration
(Tmax), peak plasma
concentration (Cmax), and
the area under the curve (AUC0→∞)
values of both administrated samples, NI tended to be absorbed to a much
greater extent from the lyophilized NI-SLN-Tre suspensions because of the
enhanced solvation of NI-SLN in gastrointestinal fluid, derived from
formation of hydrogen bonds between the polar head groups of the lipids and the
O-H groups of trehalose. Furthermore, the results of a hemolysis assay
revealed that the NI-SLN and NI-SLN-Tre suspensions showed good hemocompatibility
properties with hemolysis values of less than 5%. Taken together, the results
of this study demonstrate that NI-SLN-Tre exhibits suitable pharmacokinetic
properties and good biocompatibility.