Design and characterization of a novel amphiphilic chitosan nanocapsule-based thermo-gelling biogel with sustained in vivo release of the hydrophilic anti-epilepsy drug ethosuximide
Journal article, 2012

Thermo-gelling injectable nanogels, with no burst release of loaded drug, were prepared by a simple route by combining self assembled nanocapsules of amphiphilically modified chitosan with glycerophosphate di-sodium salt and glycerol. The potential as a depot drug delivery system was demonstrated in vivo through the therapeutic effect of ethosuximide (ESM) loaded nanogels, suppressing spike wave discharges (SWDs) in Long Evan rat model. Simultaneously clearance of gels from the site of administration was monitored non-invasively using MRI. The gel structure was characterized using TEM and SEM, confirming the gels to be an assembly of nanocapsules and using two-photon microscopy to visualize the network structure. In vitro drug release studies using ESM revealed that the nanogels exhibited extended, mostly Fickian release. Finally, all investigated formulations displayed excellent cytotoxicity data determined by MTT assay using human retinal pigmented epithelium cells. All presented properties are highly desirable for injectable depot gels for drug delivery.

Thermo responsive

Drug delivery

Amphiphilic chitosan

Nano capsules

In vivo

Author

Meng-Hsuan Hsiao

National Chiao Tung University

Mikael Larsson

Chalmers, Chemical and Biological Engineering, Pharmaceutical Technology

SuMo Biomaterials

Anette Larsson

SuMo Biomaterials

Chalmers, Chemical and Biological Engineering, Pharmaceutical Technology

Hanne Evenbratt

Chalmers, Chemical and Biological Engineering, Pharmaceutical Technology

Ying-Yu Chen

University of Southern California

You-Yin Chen

National Yang-Ming University Taiwan

D. M. Liu

National Chiao Tung University

Journal of Controlled Release

0168-3659 (ISSN)

Vol. 161 3 942-948

Areas of Advance

Nanoscience and Nanotechnology (SO 2010-2017, EI 2018-)

Materials Science

Subject Categories

Pharmaceutical Sciences

Other Basic Medicine

Chemical Sciences

DOI

10.1016/j.jconrel.2012.05.038

More information

Latest update

8/18/2020