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Preparation and characterization of intestinal transporter -targeted polymeric micelles.
- Source :
-
Journal of Chinese Pharmaceutical Sciences . Jul2018, Vol. 27 Issue 7, p490-497. 8p. - Publication Year :
- 2018
-
Abstract
- The intestinal epithelium is the main barrier to the oral delivery of poorly water-soluble drugs. Based on the specific transporters expressed on the apical membrane of the intestinal epithelium, novel polymer micelles targeting to the organic cation transporter 2 (OCTN2) were constructed by combining carnitine conjugated poly(2 -ethyl-2-oxazoline)-poly(D,L-lactide) (Car-PEOz-PLA) with monomethoxy poly(ethylene glycol)-poly(D,L-lactide) (mPEG-PLA). The structure of the synthesized Car-PEOz-PLA was confirmed by ¹H NMR, TLC and ammonium reineckate precipitation reaction, and the number-average molecular weight determined by GPC was 7260 g/mol with a low PDI of 1.44. Coumarin 6-loaded carnitine modified polymeric micelles prepared by film hydration method were characterized to have a nano-scaled size of about 31 nm in diameter, uniform spherical morphology, high drug loading content of 0.098%±0.03% and encapsulation efficiency of 92.67%±2.80%. Moreover, the carnitine-modified micelles exhibited the similar in vitro release behavior in SGF and SIF, and evidently enhanced intestinal absorption of poorly water-soluble agent. Therefore, the designed OCTN2-targeted micelles might have a promising potential for oral delivery of poorly water-soluble drugs. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 10031057
- Volume :
- 27
- Issue :
- 7
- Database :
- Academic Search Index
- Journal :
- Journal of Chinese Pharmaceutical Sciences
- Publication Type :
- Academic Journal
- Accession number :
- 131958429
- Full Text :
- https://doi.org/10.5246/jcps.2018.07.050