Radiomodulatory effect of liposome encapsulated AK-2123 on tumor in mice exposed to hepatocarcinogen

Abstract

An attempt was made to evaluate the whole body gamma-radiation effect on tumor in the presence of free and liposome encapsulated AK-2123, a hypoxic cell radiosensitizer that has widely been used in combination with a number of cancer therapies such as thermotherapy, chemotherapy and radiotherapy. Entrapment efficiency of AK-2123 into liposome was determined by LASER Raman spectroscopy. Cancer induction in mice was carried out by repeated exposure of N-nitrosodiethylamine (DEN) in combination with partial hepatectomy. Parameters such as marker enzymes activities (GGT and AChE), rates of nucleic acid synthesis, viability modification factor and the histology of liver tissues monitored, supported the induction of cancer in liver. In addition, the effect of free as well as liposome encapsulated AK-2123 on haemopoietic parameters were also studied. It was observed that AK-2123 after incorporation into liposome afforded more efficient radiomodulatory effects than that of free AK-2123 as determined by the above-mentioned parameters. Neither free AK-2123 nor liposome encapsulated AK-2123 showed any detectable toxic effects on the mice. Thus, it is seen that treatment of cancer with a combination of radiation, a radiomodifier and a drug delivery system, opens a wide scope for exploitation for the improvement of existing cancer therapies.

Differential cytotoxicity and sonosensitization by sanazole: effect of cell type and acoustic parameters

“…In spite of these conclusions, we still cannot rule out a role for increased internalization of the drug, at least at PRFs lower than 5 Hz, as a consequence of increased membrane permeability (sonoporation) [15]. It is also worth mentioning that the presence of sanazole during sonication did not result in increased free radical formation even at higher intensities as measured by electron paramagnetic resonance (EPR) spin-trapping spectroscopy, and the acoustic irradiation did not change the molecular structure of sanazole as indicated by spectrophotometric analysis [34,35].…”

Ultrasound assisted synthesis of pyrazolo[1,5-a]pyrimidine-antipyrine hybrids and their anti-inflammatory and anti-cancer activities

“…In particular, test compound 6a produced the lowest metabolism of MTT by these cells (Figure 4), followed by test compounds 8b, 13a. This assay is commonly used to monitor cell viability and proliferation and hence can also be used for assessing cytotoxicity [36,42]. Figure 4.…”

Sanazole directed targeting of silver nanoparticle drug complex to tumor mass: A preclinical investigation in murine model

“…[9] Sanazole [AK 2123 or N-(2-methlyoxyethyl) -3-(3"-nitro-1"triazoyl) acetamide], a nitrotriazole hypoxic cell sensitizer [ Figure 1] that has widely been used in combination with a number of cancer therapies such as thermotherapy, chemotherapy, and radiotherapy. [10] Sanazole (AK) induces apoptosis in murine fibrosarcoma cells and enhances the level of caspase-3 enzyme and internucleosomal fragmentation. [5] Sanazole has been found to accumulate in hypoxic cells of tumors and this property has facilitated its utility for tumor imaging.…”