Pharmaceutics Research Projects Laboratory, Department of Pharmaceutical Sciences, Dr. H. S. Gour Vishwavidyalaya, Sagar (Madhya Pradesh), India.
J Drug Target. 2011 May;19(4):251-7. doi: 10.3109/1061186X.2010.492525. Epub 2010 Jun 14.
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.
本研究旨在开发并探索硫酸软骨素偶联脂质体（CS-LP）在实体瘤靶向治疗中的应用。采用薄膜水化法制备脂质体，并通过硫酸软骨素进行偶联。通过红外光谱对其进行确认。对各种参数进行了表征，如囊泡形状和表面形态、粒径和粒径分布、Zeta 电位、包封效率和体外释放模式。未偶联脂质体（256nm）的囊泡粒径小于 CS-LP（310nm）。体外药物释放结果显示，未偶联脂质体制剂在 24 小时结束时的释放率为 44.2%，而偶联制剂的释放率为 38.3%。通过荧光显微镜观察 MDA-MB-231 乳腺癌细胞系对 CS-LP 和未偶联脂质体的摄取情况，结果表明，硫酸软骨素的偶联依赖于脂质体的识别和更高的摄取。脂质体的偶联显著增强了药物在肿瘤中的摄取，这反映在 CS-LP 给药后从肿瘤中回收的剂量百分比更高，与未偶联脂质体或游离药物相比，提示它们可作为实体瘤靶向治疗的载体。
