Jump to main content
Jump to site search

Issue 89, 2017
Previous Article Next Article

An injectable in situ lipid phase transition system for sustained delivery of dabigatran etexilate with low burst release

Author affiliations

Abstract

Controlling initial burst release remains one of the greatest challenges in developing in situ-forming parenteral depot formulations. Here an injectable lipid phase transition system (LPTS) was fabricated to provide sustained release of dabigatran exilate (DABE) with low burst release. LPTS was prepared in a low-viscosity injectable state by simple mixing of sorbitan monooleate and phospholipids with ethanol. After subcutaneous injection, the liquid LPTS underwent a phase transition in situ and formed a semi-solid mesophase, creating a drug-release depot. The physicochemical properties of DABE–LPTS were investigated using rheological techniques. Release profiles in vitro indicated that DABE–LPTS has suitable controlled release properties. Pharmacokinetic studies showed that DABE–LPTS significantly reduced the initial burst release after subcutaneous injection in rats. Pharmacodynamic studies showed that single administration of DABE–LPTS exerted anticoagulant effects in rats lasting 1 week. DABE–LPTS showed good biocompatibility in vitro and in vivo. Thus, the LPTS-based depot system shows promise for sustained DABE delivery with low burst release.

Graphical abstract: An injectable in situ lipid phase transition system for sustained delivery of dabigatran etexilate with low burst release

Back to tab navigation

Supplementary files

Article information


Submitted
18 Sep 2017
Accepted
07 Dec 2017
First published
15 Dec 2017

This article is Open Access

RSC Adv., 2017,7, 56594-56601
Article type
Paper

An injectable in situ lipid phase transition system for sustained delivery of dabigatran etexilate with low burst release

X. Zhang, M. Hu, G. Wei, M. Jia, T. Gong and J. Liu, RSC Adv., 2017, 7, 56594
DOI: 10.1039/C7RA10375A

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Material from this article can be used in other publications provided that the correct acknowledgement is given with the reproduced material.

Reproduced material should be attributed as follows:

  • For reproduction of material from NJC:
    [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the Centre National de la Recherche Scientifique (CNRS) and the RSC.
  • For reproduction of material from PCCP:
    [Original citation] - Published by the PCCP Owner Societies.
  • For reproduction of material from PPS:
    [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the European Society for Photobiology, the European Photochemistry Association, and RSC.
  • For reproduction of material from all other RSC journals:
    [Original citation] - Published by The Royal Society of Chemistry.

Information about reproducing material from RSC articles with different licences is available on our Permission Requests page.


Social activity

Search articles by author

Spotlight

Advertisements