Abstract
The purpose of this study was to identify and explore the differences in pharmacokinetics between different nanoformulations. This was done by comparing the pharmacokinetics of methotrexate-loaded nanoparticles [poly(lactic-co-glycolic acid); size of 163.70 ± 10.25 nm] and nanoemulsions (olive oil and Labrasol; size of 173.77 ± 5.76 nm), which represent hard- and soft-type nanoformulations, respectively. In addition, the population pharmacokinetic modeling approach as a useful tool for the comparison of pharmacokinetics between nanoformulations was newly proposed through this study. Significant pharmacokinetic differences were identified between nanoformulations through the new population pharmacokinetic modeling approach. As a result, the formulation type was explored as a significant covariate. The clearance and bioavailability of methotrexate-loaded nanoemulsions tended to decrease by 99% and increase by 19%, respectively, compared to those of the nanoparticles. The exploration of significant pharmacokinetic differences between drug formulations and their correlations presented in this study provide new perspectives on the development of nanoformulations.
Highlights
Values were significantly lower in nanoparticles. These pharmacokinetic results suggest that use of methotrexate-loaded nanoparticles could result in significant improvements in blood pharmacokinetic profile and bioavailability compared to use of free drug
The pharmacokinetic differences between nanoparticles and nanoemulsions, which correspond to hard- and soft-type nanoformulations, were analyzed and compared
The pharmacokinetic differences between free methotrexate solution as a control group and methotrexate-loaded nanoformulations as the experimental groups were compared through population pharmacokinetic model analysis using NLME
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. The pharmacokinetic properties of general small-molecule chemicals and those enclosed in nanoformulations are very different. These pharmacokinetic differences may occur because the distribution characteristics of nanoformulations dominate those of smallmolecule chemicals in the body. The characteristics of nanoformulations are remarkable when the compounds are administered intravenously. In the case of orally administered nanoformulations, it is common to release small-molecule chemicals from nanoformulations so that these chemicals are absorbed in the gastrointestinal tract. A mechanism by which the nanoformulation itself is absorbed
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