V. Mantareva et al., SI(IV)-METHOXYETHYLENE-GLYCOL-NAPHTHALOCYANINE - SYNTHESIS AND PHARMACOKINETIC AND PHOTOSENSITIZING PROPERTIES IN DIFFERENT TUMOR-MODELS, Journal of photochemistry and photobiology.B, Biology, 40(3), 1997, pp. 258-262
A Si(IV)-naphthalocyanine bearing two methoxyethylenglycol axial ligan
ds to the centrally coordinated metal ion (SiNc) was prepared by chemi
cal synthesis and assayed for the phototherapeutic activity after admi
nistration in a Cremophor formulation to C57BI/6 mice bearing a subcut
aneously transplanted Lewis lung carcinoma or B16 pigmented melanoma.
Pharmacokinetic studies indicate that the maximal accumulation in the
tumour occurs at 24 h after intraperitoneal injection of 0.5 mg kg(-1)
of SiNc, although the naphthalocyanine concentration in the Lewis lun
g carcinoma (0.70 mu g g(-1)) is significantly larger than that in the
B16 pigmented melanoma (0.15 mu g g(-1)). This results in a higher se
lectivity of tumour targeting in the case of the lung carcinoma. Fhoto
dynamic therapy (782 nm, 370 mW cm(-2), 360 J cm(-2)) at 24 h after Si
Nc injection causes an efficient tumour response for Lewis lung carcin
oma (50% lower tumour diameter on day 19 post-treatment as compared to
untreated controls) while the pigmented melanoma shows only a minor r
esponse regarding the rate of tumour growth. (C) 1997 Elsevier Science
S.A.