Abstract:
Bee venom (B.V.) is a toxin produced naturally by honey bees with several toxic and therapeutic
efcacies. It is used in the treatment of diferent 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 efciency %, swelling degree, and in-vitro release are evaluated for prepared
microspheres. Free B.V., optimized microspheres formula (F3), and doxorubicin cytotoxic efects were
tested by MTT assay. Results concluded that free B.V. was more efective 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 efect on normal oral epithelial cells (OEC). According to
fow cytometric analysis, the optimized microsphere formula induced apoptosis and reduced necrosis
percent at IC50 concentration. Furthermore, microspheres did not afect the viability of OEC. These
results revealed that microspheres have a degree of specifcity for malignant cells. Therefore, it seems
that this targeted formulation could be a good candidate for future clinical trials for cancer therapy.
