Abstract
Garcinia mangostana Linn extract (GME) is a natural product that has received considerable attention in cancer therapy, and has the potential to reduce side effects of chemotherapeutics and improve efficacy. We formulated GME-encapsulated ethyl cellulose (GME-EC) and a polymer blend of ethyl cellulose and methyl cellulose (GME-EC/MC) nanoparticles. We achieved high drug-loading and encapsulation efficiency using a solvent-displacement method with particle sizes around 250 nm. Cellular uptake and accumulation of GME was higher for GME-encapsulated nanoparticles compared to free GME. In vitro cytotoxicity analysis showed effective anticancer activity of GME-EC and GME-EC/MC nanoparticles in HeLa cells in a dose-dependent manner. GME-EC/MC nanoparticles showed approximately twofold-higher anticancer activity compared to GME-EC nanoparticles, likely due to their enhanced bioavailability. GME-encapsulated nanoparticles primarily entered HeLa cells by clathrin-mediated endocytosis and trafficked through the endolysosomal pathway. As far as we know, this is the first report on the cellular uptake and intracellular trafficking mechanism of drug-loaded cellulose-based nanoparticles. In summary, encapsulation of GME using cellulose-derivative nanoparticles-GME-EC and GME-EC/MC nanoparticles-successfully improved the bioavailability of GME in aqueous solution, enhanced cellular uptake, and displayed effective anticancer activity.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 3677-3686 |
| Number of pages | 10 |
| Journal | International journal of nanomedicine |
| Volume | 9 |
| Issue number | 1 |
| DOIs | |
| State | Published - Aug 6 2014 |
Keywords
- Cancer
- Cellulose
- Intracellular trafficking
- Nanoparticles
- Phytotherapy
ASJC Scopus subject areas
- Biophysics
- Bioengineering
- Biomaterials
- Pharmaceutical Science
- Drug Discovery
- Organic Chemistry