Zoology and Entomology Department, Faculty of Science, Al-Azhar University, Youssef Abbas St. off Mostafa Elnhhas, 6th District, Nasr City, Cairo, 11751, Egypt.
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Al-Azhar University, Youssef Abbas St. off Mostafa Elnhhas, 6th District, Nasr City, Cairo, 11751, Egypt.
Sci Rep. 2022 Aug 2;12(1):13213. doi: 10.1038/s41598-022-17391-w.
Bee venom (B.V.) is a toxin produced naturally by honey bees with several toxic and therapeutic efficacies. It is used in the treatment of different cancer kinds like renal, hepatic, and prostate cancer. Due to its protein nature, it is degraded in the upper gastrointestinal tract. Colon-targeted drug delivery systems represent a useful tool to protect B.V. from degradation and can be administered orally instead of I.V. infusion and traditional bee stinging. In the present study, B.V. loaded enteric-coated cross-linked microspheres were prepared by emulsion cross-linking method. Percentage yield, entrapment efficiency %, swelling degree, and in-vitro release are evaluated for prepared microspheres. Free B.V., optimized microspheres formula (F3), and doxorubicin cytotoxic effects were tested by MTT assay. Results concluded that free B.V. was more effective against the growth of human prostate adenocarcinoma (PC3) cells followed by optimized microspheres than doxorubicin. But both free B.V. and doxorubicin have a cytotoxic effect on normal oral epithelial cells (OEC). According to flow cytometric analysis, the optimized microsphere formula induced apoptosis and reduced necrosis percent at IC concentration. Furthermore, microspheres did not affect the viability of OEC. These results revealed that microspheres have a degree of specificity for malignant cells. Therefore, it seems that this targeted formulation could be a good candidate for future clinical trials for cancer therapy.
蜂毒（B.V.）是由蜜蜂自然产生的一种毒素，具有多种毒性和治疗功效。它被用于治疗不同类型的癌症，如肾、肝和前列腺癌。由于其蛋白质性质，它在上消化道中被降解。结肠靶向药物递送系统是一种有用的工具，可以保护 B.V.免受降解，并可以口服给药，而不是静脉输注和传统的蜜蜂蜇伤。在本研究中，通过乳化交联法制备了载蜂毒的肠溶交联微球。评价了所得微球的产率、包封效率%、溶胀度和体外释放度。通过 MTT 法测试了游离 B.V.、优化的微球配方（F3）和阿霉素的细胞毒性作用。结果表明，游离 B.V.对人前列腺腺癌（PC3）细胞的生长抑制作用强于优化的微球，强于阿霉素。但游离 B.V.和阿霉素对正常口腔上皮细胞（OEC）均有细胞毒性作用。根据流式细胞术分析，优化的微球配方在 IC 浓度下诱导细胞凋亡并降低坏死率。此外，微球不影响 OEC 的活力。这些结果表明微球对恶性细胞具有一定的特异性。因此，这种靶向制剂似乎是癌症治疗未来临床试验的一个很好的候选药物。
