El-Bakry Rana, Mahmoud Dina M, Eskander Attia Mary, Gamal Fouad Amr, H Mohammed Nada, Belal Amany, Miski Samar F, Khalid Aref Albezrah Nisreen, Abduljabbar Maram H, Mahmoud Tamer M
Department of Pharmacology and Toxicology, EL Saleheya EL Gadida University, EL Saleheya El Gadida, Sharkia, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy, El Saleheya El Gadida University, El Saleheya El Gadida, Sharkia, Egypt; Department of Pharmaceutics, Faculty of Pharmacy, Nahda University, Beni-Suef, Egypt.
Int J Pharm. 2024 Nov 15;665:124684. doi: 10.1016/j.ijpharm.2024.124684. Epub 2024 Sep 11.
Anastrazole (ASZ) is an effective aromatase inhibitor that is used for breast cancer treatment. Nevertheless, ASZ's effectiveness is diminished due to its low water solubility, unregulated release, absence of targeting, and inadequate patient compliance. The goal of the research was to create a hydrogel formulation of ASZ-loaded invasomes (ALI) to enhance the solubility, permeability, targeting, and efficacy of ASZ while also sustaining its release for treatment of breast cancer. The optimized ALI formulation was determined to be 3%w/v phospholipid, 0.15%w/v cholesterol, 3%v/v ethanol, and 1 %v/v cineole based on the results of the pre-formulation study. After conducting in vitro characterization of the optimum formulation, it was combined with carbopol for in vivo examination of its anti-tumor efficacy in a rat model of 7, 12-dimethylbenzanthracene. Compared to free ASZ, ALI hydrogel increased its penetration by 10.67 times and prolonged its release by 64.02%. Compared to the control positive group, ALI hydrogel reduced tumor volume by 99.19% and mortality by 10.93%. The anti-tumor effect of the ALI hydrogel was demonstrated by its ability to accumulate more ASZ in tumors and reduce hypercellular tumors. Overall, transdermal ALI hydrogel shows potential as a promising approach for treating breast cancer.
阿那曲唑（ASZ）是一种用于乳腺癌治疗的有效芳香酶抑制剂。然而，由于其低水溶性、释放不受控、缺乏靶向性以及患者依从性不足，ASZ的有效性有所降低。该研究的目的是制备一种负载阿那曲唑的侵入体水凝胶制剂（ALI），以提高ASZ的溶解度、渗透性、靶向性和疗效，同时维持其释放以治疗乳腺癌。根据处方前研究的结果，确定优化后的ALI制剂为3%w/v磷脂、0.15%w/v胆固醇、3%v/v乙醇和1%v/v桉叶油素。在对最佳制剂进行体外表征后，将其与卡波姆混合，用于在7,12-二甲基苯并蒽大鼠模型中体内检测其抗肿瘤疗效。与游离ASZ相比，ALI水凝胶使其渗透率提高了10.67倍，释放时间延长了64.02%。与对照阳性组相比，ALI水凝胶使肿瘤体积减少了99.19%，死亡率降低了10.93%。ALI水凝胶的抗肿瘤作用通过其在肿瘤中积累更多ASZ并减少高细胞性肿瘤的能力得到证明。总体而言，经皮ALI水凝胶显示出作为一种有前景的乳腺癌治疗方法的潜力。
