脂质体或低密度脂蛋白给药的锌（II）-酞菁作为肿瘤光动力剂。I. 药代动力学性质和光疗效率。
Liposome- or LDL-administered Zn (II)-phthalocyanine as a photodynamic agent for tumours. I. Pharmacokinetic properties and phototherapeutic efficiency.
作者信息
Reddi E, Zhou C, Biolo R, Menegaldo E, Jori G
机构信息
Department of Biology, University of Padova, Italy.
出版信息
Br J Cancer. 1990 Mar;61(3):407-11. doi: 10.1038/bjc.1990.89.
Abstract
The pharmacokinetics of Zn-phthalocyanine (Zn-Pc) in mice bearing a transplanted MS-2 fibrosarcoma has been studied using dipalmitoyl-phosphatidylcholine (DPPC) liposomes and low density lipoproteins (LDL) as drug delivery systems. LDL induce a higher Zn-Pc uptake by the tumour and improve the selectivity of tumour targeting as compared to DPPC liposomes. Experimental photodynamic therapy (PDT) of the MS-2 fibrosarcoma has been performed using liposome-delivered Zn-Pc and the efficiency of tumour necrosis has been measured following four different irradiation protocols. We found that Zn-Pc doses as low as 0.07-0.35 mg kg-1 are sufficient for inducing an efficient tumour response that is linearly dependent on the injected dose. The amount of Zn-Pc in the tumour decreases very slowly as a function of time, hence PDT gives satisfactory results even if performed at relatively long time intervals after administration.
摘要
以二棕榈酰磷脂酰胆碱（DPPC）脂质体和低密度脂蛋白（LDL）作为药物递送系统，研究了锌酞菁（Zn-Pc）在移植了MS-2纤维肉瘤的小鼠体内的药代动力学。与DPPC脂质体相比，LDL可诱导肿瘤对Zn-Pc的摄取增加，并提高肿瘤靶向的选择性。使用脂质体递送的Zn-Pc对MS-2纤维肉瘤进行了实验性光动力疗法（PDT），并在四种不同的照射方案后测量了肿瘤坏死的效率。我们发现，低至0.07-0.35 mg kg-1的Zn-Pc剂量足以诱导有效的肿瘤反应，该反应与注射剂量呈线性相关。肿瘤中Zn-Pc的量随时间下降非常缓慢，因此即使在给药后较长时间间隔进行PDT也能取得满意的结果。
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