2022, Vol. 26 ›› Issue (28): 4489-4493

Preparation and in vitro release of curcumin sustained-release microspheres

Li Xikai1, Meng Yongchun2, Fu Li1, Liu Qing1, Wang Xiao1, Gu Chengxu1, Huang Fei1   

Abstract: BACKGROUND: Curcumin can inhibit inflammation and promote axonal growth, but it has a short half-life and a fast clearance rate.  
OBJECTIVE:   To prepare curcumin sustained-release microspheres to release curcumin slowly and continuously.
METHODS: Curcumin sustained-release microspheres were synthesized by O/W emulsification volatilization method using polylactic acid-glycolic acid copolymer as raw material. The preset drug loading rates were 10% and 20%, respectively, and set as No. 1 and No. 2 microspheres. The curcumin sustained release microspheres were synthesized by O/W emulsification volatilization method using L-lactic acid-polycaprolactone copolymer as raw material. The preset drug loading rates were 10% and 20%, respectively, and the microspheres were set as No. 3 and No. 4. The surface morphology of the microspheres was observed by scanning electron microscopy, and the drug loading and encapsulation efficiency of the microspheres were determined by high performance liquid chromatography. Four groups of microspheres were immersed in PBS release solution containing 1% sodium dodecyl sulfate, and the sustained release of curcumin microspheres was detected under simulated physiological environment.   
RESULTS AND CONCLUSION: (1) Scanning electron microscopy showed that the particle size and morphology of No. 3 and No. 4 curcumin microspheres were better than those of No. 1 and No. 2 curcumin microspheres. (2) The encapsulation rate of No. 3 microspheres was higher than that of the other three groups (P < 0.05, P < 0.01), and there was no significant difference in the encapsulation rate of No. 1, 2 and 4 microspheres (P > 0.05). (3) The drug loading rates of No. 2, 3 and 4 microspheres were higher than that of No. 1 microsphere (P < 0.01), and the drug loading rates of No. 2 and 4 microspheres were higher than that of No. 3 microsphere (P < 0.01). (4) The in vitro release of No. 3 curcumin sustained-release microspheres lasted for 14 days, and the release of the other three kinds of microspheres lasted for 21 days. The cumulative release rate of No. 1 and No. 3 was higher than that of No. 2 and No. 4, and the curcumin release concentration of No. 3 was higher than that of No. 1. (5) The results showed that slow-release effect of the curcumin sustained-release microspheres with a preset loading rate of 10% prepared by L-lactic acid-polycaprolactone copolymer best meets the Zero order release requirements.
Key words: curcumin, curcumin sustained-release microspheres, polylactic acid, glycolic acid copolymer, L-polylactic acid, polycaprolactone, in vitro release