LIPOSOME-DELIVERED SI(IV)-NAPHTHALOCYANINE AS A PHOTODYNAMIC SENSITIZER FOR EXPERIMENTAL-TUMORS - PHARMACOKINETIC AND PHOTOTHERAPEUTIC STUDIES
LIPOSOME-DELIVERED SI(IV)-NAPHTHALOCYANINE AS A PHOTODYNAMIC SENSITIZER FOR EXPERIMENTAL-TUMORS - PHARMACOKINETIC AND PHOTOTHERAPEUTIC STUDIES
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DOI：
10.1038/bjc.1990.418
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发表时间：
1990-12-01
影响因子：
8.8
通讯作者：
RODGERS, MAJ
中科院分区：
文献类型：
--
作者：
CUOMO, V;JORI, G;RODGERS, MAJ
The pharmacokinetic behaviour and phototherapeutic effectiveness of bis(di-isobutyloctadecylsiloxy)-2,3-naphthalocyanatosilicon (iso-BOSiNc) incorporated into dipalmitoyl-phosphatidylcholine (DPPC) liposomes have been studied in Balb/c mice bearing an MS-2 fibrosarcoma. We found that iso-BOSiNc i.v.-injected at a dose of 0.5 mg kg-1 b.w. is preferentially transported by serum lipoproteins; in particular, the photosensitiser is associated with LDL (57.8% of total recovery in the serum) and HDL (35.7%) while minor amounts are associated to VLDL (2.63%) and other serum proteins (3.89%), Iso-BOSiNc concentrations greater than 1 .mu.g g-1 of tissue are recovered from the tumour at 12-48 h after administration while the ratio of iso-BOSiNc concentration in tumour and peritumoral tissue is greater than 10. Upon increasing the injected dose, the additional iso-BOSiNc is almost exclusively bound by HDL, which leads to large uptake of the photosensitiser by liver and spleen. The efficiency of iso-BOSiNc as a photodynamic agent was measured upon irradiation with a different dose-rate for a total light dose of 450 J cm-2. The extent of tumour necrotic area is linearly dependent on the irradiation dose-rate up to 100 mW cm-2. In all there is substantial evidence that iso-BOSiNc delivered in a liposomal dispersion is a highly effective photosensitizer for PDT of tumours.
