Chelvi T P, Jain S K, Ralhan R
Department of Biochemistry, All India Institute of Medical Sciences, New Delhi.
Oncol Res. 1995;7(7-8):393-8.
Targeted drug delivery systems combining thermosensitive liposome-entrapped anticancer drugs and hyperthermia have been tried for targeting drugs to tumors. These heat-sensitive liposomes are prepared from synthetic lipids. Herein we report the use of thermosensitive liposomes composed of natural lipids, viz., egg phosphatidyl choline, cholesterol, and ethanol, having phase transition temperature of 42.7 degrees C for targeted drug delivery. The antitumor effect of melphalan encapsulated in thermosensitive small unilamellar liposomes administered in combination with hyperthermia was studied in C57B1/6 mice bearing B16F10 melanoma. The in vivo efficacy of liposome-encapsulated melphalan in combination with hyperthermia as measured by reduction in tumor volume and increased survival time was greater than that of an equivalent concentration of free melphalan with or without heating. These results suggest that the combination of drug-loaded natural lipid-derived thermosensitive liposomes with local hyperthermia at the tumor site could be useful in enhancing drug delivery to tumors and improving its therapeutic efficacy in treatment of solid tumors.
将热敏脂质体包裹的抗癌药物与热疗相结合的靶向给药系统已被尝试用于将药物靶向输送至肿瘤部位。这些热敏脂质体由合成脂质制备而成。在此，我们报道了使用由天然脂质（即鸡蛋磷脂酰胆碱、胆固醇和乙醇）组成的热敏脂质体进行靶向给药，其相变温度为42.7摄氏度。在携带B16F10黑色素瘤的C57B1/6小鼠中，研究了包裹在热敏小单层脂质体中的美法仑与热疗联合给药的抗肿瘤效果。通过肿瘤体积减小和存活时间延长来衡量，脂质体包裹的美法仑与热疗联合使用的体内疗效大于同等浓度的游离美法仑在加热或不加热情况下的疗效。这些结果表明，载药的天然脂质来源的热敏脂质体与肿瘤部位的局部热疗相结合，可能有助于增强药物向肿瘤的递送，并提高其在实体瘤治疗中的疗效。
