Doxorubicin-loaded galactose-conjugated poly(d,l-lactide-co-glycolide) nanoparticles as hepatocyte-targeting drug carrier

Abstract

The objective of this work is to produce doxorubicin-loaded galactose-conjugated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) to be specifically recognised by human hepatoma cellular carcinoma (Hep G2) cells and assess NPs cytotoxicity. Doxorubicin-unloaded and doxorubicin-loaded galactose-conjugated PLGA NPs were prepared using an emulsion method and characterised for morphology, size, drug release behaviour, Hep G2 recognition and cell cytotoxicity. The produced doxorubicin-loaded PLGA-galactose-conjugate nanoparticles (PLGA-GAL NPs) are spherical in shape with a size of 365 ± 74 nm, a drug encapsulation efficiency of 69% and released in a biphasic pattern with higher release rates at pH 5. In vitro cell studies confirmed the specific interaction between the receptors of Hep G2 and the PLGA-GAL NPs. Cell cytotoxicity tests showed that unloaded NPs are non-toxic and that doxorubicin-loaded NPs caused a cellular viability decrease of around 80%, therefore representing a promising approach to improve liver-specific drug delivery.

Keywords:

• Galactosylated PLGA
• liver-specific nanoparticles
• Hep G2 cells
• asialoglycoprotein receptor (ASPGR)
• doxorubicin delivery

Acknowledgement

The authors would like to acknowledge Dr. António Lopes (ITQB, UNL) for the transfer of knowledge related with the interpretation of DLS.

Disclosure statement

The authors report no declaration of interest.

Funding information

This work was supported by Fundação para a Ciência e a Tecnologia, Portugal, [PTDC/EQU-EPR/119631/2010, PEst-C/EQB/LA0006/2013, Ph.D. grant SFRH/BD/48773/2008].