Bufalin-Loaded CaP/DPPE-PEG-EGF Nanospheres: Preparation, Cellular Uptake, Distribution, and Anti-Tumor Effects

Bufalin has significant antitumor effects on various kinds of tumors. However, bufalin's clinical utility is severely limited because of its side effects, toxicity, and fast metabolism. We made bufalin-loaded, targeted nanospheres with the aim of overcoming bufalin's limitations. Epidermal growth factor (EGF)-modified nanospheres with encapsulated bufalin showed increased toxicity in colorectal cancer cells, inhibition of cell proliferation, and induction of apoptosis relative to the non-EGF-modified nanospheres. The average particle size of the nanospheres was 171 nm and the encapsulation efficiency was 83.2%. In vitro release data showed that bufalin loaded in calcium phosphate/DPPE-PEG-EGF hybrid porous nanospheres was released more slowly from dialysis membranes than free bufalin. According to our results, EGF-modified nanospheres containing bufalin show improved anti-tumor effects on colon cancer in nude mice, but without severe side effects.