Abstract
To develop injectable formulation and improve the stability of curcumin (Cur), Cur was encapsulated into monomethyl poly (ethylene glycol)-poly (ε-caprolactone)-poly (trimethylene carbonate) (MPEG-P(CL-co-TMC)) micelles through a single-step solid dispersion method. The obtained Cur micelles had a small particle size of 27.6 ± 0.7 nm with polydisperse index (PDI) of 0.11 ± 0.05, drug loading of 14.07 ± 0.94%, and encapsulation efficiency of 96.08 ± 3.23%. Both free Cur and Cur micelles efficiently suppressed growth of CT26 colon carcinoma cells in vitro. The results of in vitro anticancer studies confirmed that apoptosis induction and cellular uptake on CT26 cells had completely increased in Cur micelles compared with free Cur. Besides, Cur micelles were more effective in suppressing the tumor growth of subcutaneous CT26 colon in vivo, and the mechanisms included the inhibition of tumor proliferation and angiogenesis and increased apoptosis of tumor cells. Furthermore, few side effects were found in Cur micelles. Overall, our findings suggested that Cur micelles could be a stabilized aqueous formulation for intravenous application with improved antitumor activity, which may be a potential treatment strategy for colon cancer in the future.
Highlights
Cancer is one of the most severe diseases with increasing morbidity and mortality every year around the world
Copolymer was successfully synthesized by ring-opening polymerization of ε-CL and trimethylene carbonate (TMC) initiated by MPEG using stannous octoate as catalyst
The number-average molecular weights (Mn) of MPEG-P(CL-co-TMC) copolymer caculated by 1H-NMR was 4292 (2000-1836-456)
Summary
Cancer is one of the most severe diseases with increasing morbidity and mortality every year around the world. The natural herbal Cur is less toxic than other chemotherapeutic agents in the treatment of cancer. Micelles have attracted increasing attentions in drug delivery and cancer treatment as nanocarriers. Polymeric micelles can improve aqueous formulations of hydrophobic drugs, prolong their circulation time in vivo, enhance the cellular uptake, and passively target at tumor regions by the enhanced permeability and retention (EPR) effect[19,20]. Cur-loaded monomethyl poly (ethylene glycol)-poly (ε-caprolactone) (MPEG-PCL) micelles were developed in laboratory. In order to enhance the water solubility and make it avaliable for injection, Cur loaded into a promising monomethyl poly (ethylene glycol)-poly (ε-caprolactone)-poly (trimethylene carbonate) (MPEG-P(CL-co-TMC)) micelles. The cytotoxicity of Cur micelles in vitro and the anti-tumor activity in a mouse model of colon cancer were investigated in our article
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