Introduction: Liver cancer or hepatocellular carcinoma (HCC) is a major cause of death worldwide. Targeted delivery of drug to the carcinoma cell can be achieved by conjugation of ligand on the carrier system. Methods and materials: In this study, oxaliplatin-loaded hepatoma-targeted liposome were designed and prepared using galactosylated distearoylphosphatidylethanolamine. The liposomes were prepared by cast film method and coupled with lactobionic acid (LA-LP) using 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide as a coupling agent. The coupling was confirmed by infrared spectroscopy. They were further characterized for various parameters such as vesicle shape and surface morphology, size, entrapment efficiency and in vitro release pattern. Results and discussion: The vesicle size of the uncoupled liposome (256 nm) was found to be less than LA-LP (310 nm). The uptake of LA-LP and uncoupled liposomes by BEL7402 HCC cell lines was visualized using fluorescence microscopy that revealed the dependence of liposomal recognition and higher uptake of the LA-LP. Organ distribution studies provided evidence that coupling of lactobionic acid on liposomal surface significantly enhanced the tumor uptake of drug, which is reflected by recovery of higher percentage of drug from tumor as compared to uncoupled liposomes or free drug. Conclusion: These studies suggest them as effective vectors for HCC targeting.
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.
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