Research On Preparation And Properties Of Curcumin-loaded PLA/PLGA Nanoparticles

Curcumin, a polyphenolic compound extracted from turmeric rhizome of the gingerfamily plant, has a wide range of pharmacological activity such as anti-tumor,anti-inflammatory, antibacterial, antiviral, anti-oxidation, cholesterol and so on, especially incancer prevention and treatment the role is particularly prominent and worthy of being studied.However, the popularization and application of curcumin is severely limited by its poorwater solubility, poor stability and low bioavailability. In order to solve these problems,researchers have manipulated curcumin into different drug delivery systems, such asmicrospheres, liposomes and nanoparticles. Featured with multiple methods for preparing,plentiful materials for choosing and good stability, nanoparticles are generally used to drugnanocarriers.This paper was designed to prepare curcumin-loaded nanoparticles using polylactic acid(PLA) and poly(lactic-co-glycolic acid)(PLGA) as carrier materials, which havegood biocompatibility and biodegradability, the study includes:(1) Curcumin-loaded PLAnanoparticles were prepared by emulsion solvent evaporation method with encapsulationefficiency and drug loading as the evaluation. The experimental prescriptions and preparationwere optimized based on single factor such as emulsifier concentration of TPGS, aqueous toorganic phase, PLA concentration, drug concentration, ultrasonic time and the timing ofvolatile organic solvents.(2) The preparation process of curcumin-loaded PLA nanoparticleswas optimized by orthogonal experimental method. The nanoparticles were determinated onsurface morphology, particle size, zeta potential, thermal performance and release properties,while studying the drug loading mode of nanoparticles and the law of drug release.(3)Curcumin-loaded PLGA nanoparticles were prepared by emulsion solvent evaporationmethod. We investigated the emulsifier concentration of TPGS, aqueous to organic phase,PLGA concentration, drug concentration, the concentration of PLGA and drug in organicphase (fixed the concentration ratio of them) and stirring speed on the encapsulationefficiency and drug loading.(4) The preparation process of curcumin-loaded PLGAnanoparticles was optimized by orthogonal experimental method. The nanoparticles weredeterminated on particle size, surface morphology, zeta potential, thermal performance andthe drug release in vitro, while studying the drug loading mode of nanoparticles., the law ofdrug release and the relationship of carrier materials and release properties.(5)Curcumin-loaded nanoparticles were prepared by emulsion solvent evaporation using theamphipathic copolymers as carrier materials, which get by PEG modified PLGA. We investigated the effects of technological factors on the preparation of nanoparticles.The results showed that: By the single factor experiment and the orthogonal experimentto optimize the preparation process, can obtain ideal of drug-loaded nanoparticles.The shapeof nanoparticles were spherical, regular and smooth surface, good dispersion; The averagesize of curcumin-loaded PLA nanoparticles was167.5nm, the zeta potential was-29.4mV, theencapsulation efficiency was89.52%, the drug loading was13.72%; The average size ofcurcumin-loaded PLGA nanoparticles was148.1nm, the zeta potential was-28.8mV, theencapsulation efficiency was94.75%, the drug loading was13.14%; The PEG content ofamphipathic copolymer is less, the encapsulation efficiency and drug loading of nanoparticlesare higher; The curcumin was dispersed in nanoparticles with molecular state; Experiment bydynamiac dialysis method in vitro shows that the drug-loaded nanoparticles have a goodsustained release efficacy. The release behavior of the drug-loaded nanoparticles was fitted toWeibull equation.