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苦杏仁苷作为癌症治疗方法的有效性和安全性的体外及体内评估

In Vitro and In Vivo Evaluation of the Effectiveness and Safety of Amygdalin as a Cancer Therapy.

作者信息

El-Ela Fatma I Abo, Gamal Amr, Elbanna Hossny Awad, ElBanna Ahmed H, Salem Heba F, Tulbah Alaa S

机构信息

Department of Pharmacology, Faculty of Veterinary Medicine, Beni-Suef University, Beni-Suef 62511, Egypt.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62511, Egypt.

出版信息

Pharmaceuticals (Basel). 2022 Oct 22;15(11):1306. doi: 10.3390/ph15111306.

Abstract

Cancer is one of the most important causes of death worldwide. Several studies have shown the efficacy of apricot kernel seed as a cancer therapy due to the presence of amygdalin. These studies have demonstrated amygdalin's cytotoxicity, antioxidant activity, and apoptosis in vitro using human cancer cell lines. However, no studies have demonstrated their cancer activity in vivo. The aim of this study is to develop an amygdalin-loaded niosomes (ALN) gel formulation as a drug delivery system in order to investigate the selectivity, efficacy, and toxicity of amygdalin as a cancer therapy in vivo using the 7,12-dimethylbenz (a) anthracene (DMBA) carcinoma rat model. Based on pre-formulation studies, the ALN formulation composed of Tween 60: cholesterol: dihexadecyl phosphate in a molar ratio of 1:2:0.1 was chosen as an optimum formulation because it has a percent of EE of 66.52% with a particle size of 269.3 nm and a reflux of 3.54 µg.cm.h. The ALN gel formulation was integrated into carbopol gel to be evaluated in vivo. Compared to DMBA control, treatment with ALN gel showed a reduction in the carcinoma volume and in the hyperplasia of the epidermis with no signs of edema. In conclusion, the ALN gel formulation could be an efficient cancer therapy.

摘要

癌症是全球最重要的死因之一。多项研究表明,由于苦杏仁苷的存在,杏仁核种子作为一种癌症治疗方法具有疗效。这些研究使用人类癌细胞系在体外证明了苦杏仁苷的细胞毒性、抗氧化活性和凋亡作用。然而,尚无研究在体内证明其抗癌活性。本研究的目的是开发一种载有苦杏仁苷的非离子表面活性剂囊泡(ALN)凝胶制剂作为药物递送系统,以便使用7,12-二甲基苯并(a)蒽(DMBA)诱导的大鼠癌模型在体内研究苦杏仁苷作为癌症治疗的选择性、疗效和毒性。基于处方前研究,选择由吐温60:胆固醇:磷酸二己酯按1:2:0.1的摩尔比组成的ALN制剂作为最佳制剂,因为它的包封率为66.52%,粒径为269.3 nm,回流率为3.54 µg.cm.h。将ALN凝胶制剂整合到卡波姆凝胶中进行体内评估。与DMBA对照组相比,用ALN凝胶治疗显示癌体积减小,表皮增生减少,且无水肿迹象。总之,ALN凝胶制剂可能是一种有效的癌症治疗方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e766/9697812/9f07c32e9b34/pharmaceuticals-15-01306-g004.jpg

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