Enhanced therapeutic potential of folic acid-tagged targeted liposomal quercetin (Lipo-Que) over Free-Que in Benzo [a] pyrene-induced lung cancer in mice

在苯并[a]芘诱导的小鼠肺癌中,叶酸标记的靶向脂质体槲皮素(Lipo-Que)比游离槲皮素(Free-Que)具有更强的治疗潜力。

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Abstract

AIMS: The anti-cancer potency of quercetin is limited by poor intestinal absorption and rapid metabolism clearance. This study was designed to analyze therapeutic efficacy of liposome nano-formulation of quercetin in experimental lung cancer when administered intravenously and compare it with a molecular drug, liposomal sorafenib. MATERIALS AND METHODS: The Lipo-Que and Lipo-Sorafenib were prepared by thin film formation method and administered to Benzo (a) Pyrene induced lung cancer mice. The mean survival time and other therapeutic effects in vivo were evaluated. Apoptosis induction in lung tissue ex vivo was quantified using Flow cytometry analysis. RESULTS: The Lipo-Que significantly prolonged the lifespan of cancer-induced mice (MST: 310.86 ± 0.58 days) compared to cancer control (210.18 ± 0.00 days) and Free-Que-treated mice. It significantly reduced the tumor foci and histopathologic changes in lungs and liver with complete elimination of liver metastasis. A highly significant reduction (p ≤ 0.001) in the hematopathology changes of cancer with early apoptosis induction (19.47 ± 0.00%) was observed in the Lipo-Que group, which signifies its non-inflammatory clearance of cancer cells. CONCLUSIONS: Lipo-Que exhibits superior therapeutic efficacy compared to Free-Que, highlighting its targeted delivery and action as a promising and safe alternative to conventional mode of quercetin therapy, opening avenues for further translational development.

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