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Eur J Pharm Sci. 2014 Oct 15;63:187-98. doi: 10.1016/j.ejps.2014.07.007. Epub 2014 Jul 22.

The efficacy of nimodipine drug delivery using mPEG-PLA micelles and mPEG-PLA/TPGS mixed micelles.

Author information

  • 1Department of Pharmacy, Guangdong Pharmaceutical University, Higher Education Mega Center, Guangzhou 510006, China.
  • 2Department of Pharmacy, Guangdong Women and Children Hospital, Guangzhou 510006, China.
  • 3Department of Pharmacy, Guangdong General Hospital, Guangdong Academy of Medical Sciences, 106 Zhongshan Second Road, Guangzhou 510080, China.
  • 4Department of Pharmacy, The Third Affiliated Hospital, Sun Yat-Sen University, Guangzhou 510006, China. Electronic address: zhangym@tom.com.
  • 5Department of Pharmacy, Guangdong Pharmaceutical University, Higher Education Mega Center, Guangzhou 510006, China. Electronic address: gzyangfan@hotmail.com.

Abstract

OBJECTIVE:

In order to develop and compare mPEG-PLA micelles and mPEG-PLA/TPGS mixed micelles, with the intention to develop a highly efficient formulation for nimodipine (NIM), NIM-loaded micelles and mixed micelles were made and their pharmacokinetics were studied.

METHODS:

Single factor experiments and orthogonal experiments were designed to optimize the final preparation process, characterizations and drug release behaviors were studied. Pharmacokinetics of NIM micelles, NIM mixed micelles were researched and were compared to NIM solution.

RESULTS:

Micelles and mixed micelles were prepared by solvent evaporation method, with relatively high drug loading efficiency and within nano-particle size range. The CMC value of mPEG-PLA was lower than that of mPEG-PLA/TPGS. The results of FTIR and TEM confirmed the spherical core-shell structure of micelles as well as mixed micelles, and the encapsulation of NIM inside the cores. In vitro release showed that micelles and mixed micelles had sustained release effect in the forms of passive diffusion and dissolution process, respectively. Following intraperitoneal administration (5mg/kg), micelles and mixed micelles were absorbed faster than solution, and with larger MRT(0-t), smaller CLz and larger AUC(0-t) as compared to that of solution, which showed micelles and mixed micelles had higher retention, slower elimination and higher bioavailability. This experiment also showed that mixed micelles released NIM more stably than micelles. By evaluate the bioequivalence, NIM micelles and NIM mixed micelles were testified non-bioequivalent to NIM solution.

CONCLUSION:

Micelles and mixed micelles could sustain the NIM concentrations more efficiently in plasma as compared to solution. Mixed micelles were the best ones since they had high loading content and released more stably. Thus, apprehending micelles and mixed micelles were suited as poor aqueous solubility drug carriers, and mixed micelles were better due to their high loading content and more stable release.

Copyright © 2014 Elsevier B.V. All rights reserved.

KEYWORDS:

Micelles; Mixed micelles; Nimodipine; Pharmacokinetics; Sustained release

PMID:
25063034
[PubMed - in process]
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