Preparation Of Nano Curcumin And Curcumin-PLGA Particle By Supercritical CO₂Antisolvent Technology

Curcumin is a phenolic pigments, with good biological activity. It hasthe function of antioxidant, anti-inflammatory, anti-tumor, anti-HIV, andanti-bacterial. However, due to poor stability and poor water solubility, thebioavailability of curcumin is very low, which is difficult to be fullyabsorbed. In this paper, curcumin was made into nanoparticles andmicrocapsules to improve its bioavailability.Supercritical carbon dioxideanti-solvent method attracted widespread attention in the preparation ofnanoparticles with the advantage of mild conditions, low residual solventsin product, and so on. In this research, supercritical carbon dioxideanti-solvent was used to prepare curcumin nanoparticles, and PolyLactic-co-Glycolic Acid (PLGA) is used as the carrier to preparecurcumin-PLGA nanocapsules.The main findings are as follows:(1) Supercritical carbon dioxide anti-solvent assisted by ultrasonicwas used to prepare curcumin nanoparticles. The effect of temperature,pressure, solution flow rate, concentration, ultrasonic power on particlesize was studied. Experimental results show that, the particle sizedecreases with increasing pressure, increases with increasing temperature,decreases with increasing flow rate increases, increases with increasingconcentration, and decreases with increasing ultrasonic power. The yield ofparticles increases with increasing pressure, decreases with increasingtemperature, increases with increasing concentration, and decreases withincreasing ultrasonic power. The water solubility and dispersity ofcurcumin are improved with nano-size.(2) Supercritical carbon dioxide anti-solvent assisted by ultrasonicwas used to prepare curcumin-PLGA nanocapsules. The effect of temperature, pressure, concentration, core material ratio, solution flow rate,ultrasonic power on the curcumin-PLGA microcapsules particle size, yield,drug loading and embedding rate was studied. The experimental resultsshowed that: the particle size increases with increasing temperature,increases with increasing concentration, increases with increasing massratio of PLGA to curcumin, decreases with increasing flow rate, anddecreases with increasing ultrasonic power. The particle yield increaseswith increasing concentration, increases with increasing mass ratio ofPLGA and curcumin, and decreases with increasing ultrasonic power. Drugloading and embedding rate increases with increasing concentration. Theincrease of mass ratio of PLGA and curcumin lead to decrease of drugloading, increase of embedding rate. Curcumin-PLGA nanocapsules withhigh embedding rate release in vitro better.(3) A new method of supercritical carbon dioxide anti-solvent assistedby ultrasonic was used to prepare curcumin-PLGA nanocapsules. Theeffect of concentration, core material ratio, solution flow rate, ultrasonicpower, residence time on the curcumin-PLGA microcapsules particle size,yield, drug loading and embedding rate was studied. Experimental resultsshow that: the particle yield is between60%and80%, which increasesabout100%. The yield of particles increases with increasing concentration,increases increasing mass ratio of PLGA to curcumin, decreases and thenincreases with increasing ultrasonic power, increases with increasingresidence time, increases with increasing molar ratio of carbon dioxide tosolution. Particle size increases with increasing residence time, decreaseswith increasing molar ratio of carbon dioxide to solution.(4) A improved method of supercritical carbon dioxide anti-solventassisted by ultrasonic was used to prepare curcumin-PLGA nanocapsules.Curcumin particles are separated out first, then PLGA is added to embed.Response surface optimization is used to study the effect of mass ratio ofPLGA to curcumin, flow rate, and ultrasonic power on yield andembedding rate. The results show that mass ratio of PLGA to curcumin influence the most on yield and embedding rate, the flow rate influence theleast. When the mass ratio of PLGA and curcumin is2.29/1, flow rate is3.5ml/min, ultrasonic power is120W, the yield reaches a maximum of58.03%. When the the mass ratio of PLGA and curcumin is3/1, flow rateis1.8ml/min, ultrasonic power is180W, embedding rate reaches amaximum of93.89%.