Chondroitin sulfate functionalized liposomes for solid tumor targeting

Abstract

The present investigation was aimed to develop and explore the use of chondroitin sulfate–coupled liposomes (CS-LP) for solid tumor targeting. The liposomes were prepared by cast film method and coupled with chondroitin sulfate. The coupling was confirmed by infrared spectroscopy. They were further characterized for various parameters such as vesicle shape and surface morphology, size and size distribution, zeta potential, entrapment efficiency, and in vitro release pattern. The vesicle size of the uncoupled liposome (256 nm) was found to be less than that of CS-LP (310 nm). In vitro drug release exhibited a release of 44.2% from uncoupled liposomal formulation, compared to 38.3% as observed in coupled formulation at the end of 24 hr. The uptake of the CS-LP and uncoupled liposomes by MDA-MB-231 breast cancer cell lines was visualized using fluorescence microscopy that revealed the dependence of liposomes recognition and higher uptake on the coupling of chondroitin sulfate. Coupling of the liposomes significantly enhanced the tumor uptake of drug, which is reflected in the recovery of a higher percentage of the dose from tumor following administration of CS-LP in comparison to uncoupled liposomes or free drug, suggesting that they can be used as vectors for solid tumor targeting.

Keywords::

• Liposomes
• chondroitin sulfate
• solid tumors

Acknowledgement

We thank Biotech India Ltd New Delhi, for providing Etoposide as a gift sample. The authors are also thankful to sophisticated analytical instrument facility, AIIMS, New Delhi, for performing transmission electron microscopy (TEM) studies and the University Grants Commission (UGC) for providing financial assistance in the form of junior research fellowship to one of the authors (Rashmi Bagri).

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.