Study of level and selectivity of liposomal form of photosensitiser hydroxyaluminium tetra-3-phenylthiophthalocyanine accumulation on transplantable mice tumor models at different ways of transplantation

Objective Study of embryotoxicity, teratogenicity and reproductive toxicity of the new drug Lipophtalocyan in rats. Material and Methods Studies were conducted on 210 non-inbred female rats and 105 non-inbred male rats. The drug was administered daily via i. v. injection for 48 days (males) and for 15 days (females) in 2 total doses corresponding to the therapeutic dose (TD) for mice when converted to rats and 10 TD. Results and Conclusion When mating with intact female rats, no changes in sexual behavior were observed, but the index of the ability to fertilize and conceive decreased when compared to the values of the control group by 35–40% (TD index=60%) and by 75–80% (10 TD index=20%). The index of the ability to fertilize and conceive differed from the values of the control group by 90% (TD index=5%) and by 15% (10 TD index=80%). There were no differences in the indicator of embryotoxicity and teratogenicity in intact and drug-treated female rats, compared with the control group. Lipophtalocyan has a negative effect on the male and female reproductive function in rats and has an embryotoxic effect according to the index of the ability to fertilize and conceive, as well as the indices of preimplantation and post-implantation fetal death. The drug does not have a teratogenic effect, neither it affects the physical development of offspring or the rate of maturation of sensory-motor reflexes during feeding.

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“…Before use, the contents of the vial are rehydrated with water for injection to obtain the recommended concentration 0.25 mg/ ml [3,4].…”

Section: Study Medicationmentioning

confidence: 99%

“…In preclinical studies, it was found that Lipophtalocyan has a fairly high selectivity of accumulation in the tumor in relation to normal tissue due to encapsulation of PS in PEG liposomes. The advantages of this drug are high selectivity of exposure to tumor foci, low systemic toxicity, and high efficiency shown in vivo studies [3,4].…”

Section: Introductionmentioning

confidence: 99%

Study of Reproductive Toxicity of the Liposomal Photosensitizer Lipophthalocyan

et al. 2021

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Study of pharmacokinetics of liposomal photosensitiser based on hydroxyaluminium tetra-3-phenylthiophthalocyanine on mice

Будько

Deichman

Меерович

et al. 2019

BMP

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The present work is devoted to the study of pharmacokinetics of infrared photosensitizer (PS) based on hydroxyaluminium tetra‑3‑phenylthiophthalocyanine in a sterically stabilized liposomal form. The study was carried out on adult female mice. The PS was administered once intravenously at a dose of 6 mg / kg. Evaluation of the PS accumulation dynamics in the mice tissues and organs was performed at time intervals from 5 minutes to 7 days using spectral‑ﬂuorescent method. The maximum accumulation of the PS photoactive form was recorded in lungs (32 µg / g in the interval of 5–30 minutes after introduction), liver (20.8 µg / g in the interval of 4–24 hours after introduction) and spleen (28 µg / g 4 hours after introduction). At the same time, by the end of the observation period (7 days after administration), trace amounts of the PS photoactive form were still detected in the liver and the spleen at a calculated concentration of 0.5‑1 µg / g. The PS accumulated the least in muscles and skin. The ﬂuorescent signal from the PS accumulated in skin was detectable almost immediately, and its concentration remained at the same level (1.2‑1.5 µg / g) for up to 3 days of observation. In the muscles, the concentration of the PS reached 1.5 µg / g 15 minutes after administration, and then gradually decreased until 0.25 µg / g at 24 hours. Data on the pharmacokinetics of PS in blood, basic organs and tissues of animals were obtained, pharmacokinetic parameters were calculated. 7 days after the administration, the PS concentration in the skin and muscles was below the detection limit. The studies confrmed that PEGylation of the PS liposomal form slows down the process of its capture by reticulo‑endothelial system. It was shown that the PS circulates in blood and organs of mice for a long time and it completely distributes only when 4 hours pass after administration.

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Study of level and selectivity of liposomal form of photosensitiser hydroxyaluminium tetra-3-phenylthiophthalocyanine accumulation on transplantable mice tumor models at different ways of transplantation

Cited by 2 publications

References 6 publications

Study of Reproductive Toxicity of the Liposomal Photosensitizer Lipophthalocyan

Study of Reproductive Toxicity of the Liposomal Photosensitizer Lipophthalocyan

Study of pharmacokinetics of liposomal photosensitiser based on hydroxyaluminium tetra-3-phenylthiophthalocyanine on mice

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