血卟啉衍生物脂质体瘤内注射给药在荷瘤鼠体组织中的药物分布

的：研究血卟啉衍生物不同剂型及不同给药方法对血卟啉衍生物在肿瘤及各种组织中分布的影响。方法：采用反相蒸发法制备大单层血卟啉衍生物脂质体，经荷瘤小鼠瘤体内给药，结合对照，不同时间，血、肝、脾、肿瘤及皮肤组织采样，荧光法测定各种组织中血卟啉衍生物（HPD）的浓度。结果：脂质体药物包裹率为52.6% ，72 h内药物渗漏率小于7.6％。两种剂型、两种方式给药后各个时间段的瘤体内药物浓度，L-HPD i.t.组明显高于L-HPD i.p.组和HPD i.t.组，皮肤中HPD浓度则明显降低；此结果在给药12～24 h内，L-HPD和游离HPD瘤内给药比较时更为明显。结论：与L-HPD i.p.和HPD i.t.比较，L-HPD经i.t.给药可显著提高肿瘤组织内HPD浓度，同时降低了皮肤中HPD含量。

Distribution of HPD in tissues and tumor in mice b y intratumor injection of liposome-HPD

To investigate the effect of different dosage forms of hematoporphyrin derivatives (HPD) as well as different ways of administration on the distribution of HPD in tumor and tissues. Methods: Large unilamilar vesicle L HPD was prepared using reverse phase vaporization method. The L HPD was administered to mice with tumor by i.t. or i.p. injections.The concentrations of HPD in tumor and tissues were determined by a fluorometric method at various times after injection. Results: The average diameter of L HPD particles was 100 200 nm. HPD encapsulated ratio was 52.6%. Leakage rate was within 7.6% in 72 hours. At all times after injection the concentration of HPD in tumor by i.t. injection of L HPD were higher than by i.p. injection of L HPD, as well as by i.t. injection of free HPD, whereas the level of HPD in skin was lowest after i.t. injection of L HPD. Conclusion: The results suggested that, in comparison with i.p. injection of L HPD and i.t.injection of free HPD, the concentration of HPD in tumor was the highest after i.t. injection of L HPD,hence the last one should be a favorable method for PDT.