Preparation of protamine-hyaluronic acid coated core-shell nanoparticles for enhanced solubility, permeability, and oral bioavailability of decoquinate.

Autor: Wei W; National Engineering Research Center for Process Development of Active Pharmaceutical Ingredients, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, PR China., Lu M; National Engineering Research Center for Process Development of Active Pharmaceutical Ingredients, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, PR China., Xu W; National Engineering Research Center for Process Development of Active Pharmaceutical Ingredients, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, PR China., Polyakov NE; Institute of Chemical Kinetics and Combustion, Novosibirsk 630090, Russia; Institute of Solid State Chemistry and Mechanochemistry, Novosibirsk, Russia., Dushkin AV; National Engineering Research Center for Process Development of Active Pharmaceutical Ingredients, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, PR China; Institute of Solid State Chemistry and Mechanochemistry, Novosibirsk, Russia. Electronic address: drivergood@mail.ru., Su WK; National Engineering Research Center for Process Development of Active Pharmaceutical Ingredients, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, PR China; Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, PR China. Electronic address: pharmlab@zjut.edu.cn.
Jazyk: angličtina
Zdroj: International journal of biological macromolecules [Int J Biol Macromol] 2022 Oct 01; Vol. 218, pp. 346-355. Date of Electronic Publication: 2022 Jul 22.
DOI: 10.1016/j.ijbiomac.2022.07.152
Abstrakt: Decoquinate (DQ) has low oral bioavailability owing to its poor water solubility. In this study, a DQ solid dispersion (DQ-SD) was fabricated using mechanochemical technology to encapsulate DQ and improve its oral bioavailability. DQ-SD is easily generated via self-assembly in the aqueous phase to form micelles consisting of disodium glycyrrhizinate (Na 2 GA) nanoparticles with a protamine (PRM) and anionic hyaluronic acid (HA) layers. The spherical DQ nanoparticles with an average diameter of 114.95 nm were obtained in an aqueous phase with a critical micelle concentration of 0.157 mg/mL, zeta potential of -38.38 mV, polydispersity index of 0.200, and drug loading of 5.66 %. The dissolution rate and cumulative release of DQ-SD were higher than those of pure DQ. Furthermore, the bioavailability of DQ-SD was approximately 6.3 times higher than that of pure DQ. Pharmacokinetic and biodistribution studies indicated that DQ-SD possessed a significantly higher concentration in the blood and preferential liver tissue accumulation, than that of pure DQ. The developed DQ-SD exhibited considerable potential for developing old DQ for a new application as a hematogenous parasite drug and provides a reference for developing more efficient delivery systems for hydrophobic bioactive agents.
Competing Interests: Declaration of competing interest There are no conflicts of interest to declare.
(Copyright © 2022. Published by Elsevier B.V.)
Databáze: MEDLINE
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