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Construction and characterization of intestinal oligopeptide transporter PepT1-targeted polymeric micelles for enhanced intestinal absorption of poorly water-soluble agents.
- Source :
-
Journal of Chinese Pharmaceutical Sciences . Aug2019, Vol. 28 Issue 8, p561-570. 10p. - Publication Year :
- 2019
-
Abstract
- To overcome the main barrier of intestinal epithelium for the oral absorption of poorly water-soluble drugs and further improve their oral absorption, Gly-Sar, the substrate of the oligopeptide transporter PepT1 widely distributed in the small intestine, conjugated poly(ethylene glycol)-block-poly(D,L-lactide) (Gly-Sar-PEG-b-PLA) was designed and synthesized, and PepT1-targeted polymeric micelles were prepared and characterized. The structure of the synthesized Gly-Sar-PEG-b-PLA was confirmed by use of TLC and 1H-NMR. The average molecular weight measured by GPC was 5954 g/mol with PDI of 1.34. The DiI-loaded polymeric micelles from Gly-Sar-PEG-b-PLA with drug loading content of 0.076% were characterized to exhibit 40.36 nm in diameter with PDI of 0.294, and well-defined spherical shape observed by TEM. Furthermore, the PepT1-targeted polymeric micelles profoundly enhanced intestinal absorption of poorly water-soluble drug. Therefore, the designed PepT1-targeted polymeric micelles might have a promising potential for oral delivery of water-insoluble drugs. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 10031057
- Volume :
- 28
- Issue :
- 8
- Database :
- Academic Search Index
- Journal :
- Journal of Chinese Pharmaceutical Sciences
- Publication Type :
- Academic Journal
- Accession number :
- 138426881
- Full Text :
- https://doi.org/10.5246/jcps.2019.08.054