Soncin M, Polo L, Reddi E, Jori G, Kenney M E, Cheng G, Rodgers M A
Department of Biology, University of Padova, Italy.
Cancer Lett. 1995 Feb 10;89(1):101-6. doi: 10.1016/0304-3835(95)90164-7.
The pharmacokinetic properties of the Ge(IV)-octabutoxy-phthalocyanines (GePc) with two axially ligated triethylsiloxy (GePcEt) or trihexyl-siloxy (GePcHex) chains were studied in BALB/C mice bearing a transplanted MS-2 fibrosarcoma. The GePcs were delivered to mice after incorporation into unilamellar liposomes of dipalmitoyl phosphatidylcholine (DPPC) or in an emulsion of Cremophor-EL. The Cremophor delivered GePcs were cleared from the blood circulation at a much slower rate than the liposome-delivered GePcs. At the same time, Cremophor induced a slower and reduced uptake of the GePcs in the liver and spleen while it greatly enhanced the uptake in the tumour as compared to liposomes. Maximum tumour uptake was observed at 24 h post-injection and was equivalent to 0.67 and 0.50 nmol/g, respectively, for the Cremophor delivered GePcHex and GePcEt. The corresponding values for the liposome-delivered drugs were approximately one fourth of that observed with Cremophor.
在携带移植性MS-2纤维肉瘤的BALB/C小鼠中，研究了带有两个轴向连接的三乙氧基硅氧基（GePcEt）或三己氧基硅氧基（GePcHex）链的四价锗-八丁氧基-酞菁（GePc）的药代动力学特性。将GePc掺入二棕榈酰磷脂酰胆碱（DPPC）的单层脂质体中或聚氧乙烯蓖麻油（Cremophor-EL）乳剂后给小鼠给药。与脂质体递送的GePc相比，聚氧乙烯蓖麻油递送的GePc从血液循环中清除的速度要慢得多。同时，聚氧乙烯蓖麻油诱导GePc在肝脏和脾脏中的摄取较慢且减少，而与脂质体相比，它大大增强了GePc在肿瘤中的摄取。注射后24小时观察到最大肿瘤摄取量，聚氧乙烯蓖麻油递送的GePcHex和GePcEt分别相当于0.67和0.50 nmol/g。脂质体递送药物的相应值约为聚氧乙烯蓖麻油观察值的四分之一。
