Preparation And In Vitro Drug-release Behavior Of Neferine Nanoparticles

OBJECTIVETo prepare neferine PLGA nanoparticles (NEF-PLGA- NP), and develop detecting methods to study its in vitro release characteristics.METHODSNEF-PLGA-NP were prepared by modified self-emulsification solvent diffusion method with poly (lactic-co-glycolic) acid (PLGA) as carrier material and acetone-ethanol as mixed organic solvent, polyvinyl alcohol (PVA) as surfactant. According to the entrapment efficiency and drug loading, the single factor examination was first applied to choose the main factors of preparation of NEF-PLGA-NP. Then the optimum preparation formulation of the NEF-PLGA-NP is achieved by employing the orthogonal design. According to the results of the single factor examination and the optimum formulation was checked by experiment. The entrapment efficiency and drug loading of neferine about the NEF-PLGA-NP was detected by high performance liquid chromatography, the morphology of nanoparticles were observed by transmission electric macroscope (TEM), ZETASIZER1000 apparatus was used to measure size distribution and zata electric potential. The method of dynamic membrane dialysis was used to study in vitro release characteristics of NEF-PLGA-NP.RESULTSAfter single factor and orthogonal design experiments, the optimum preparation formulation of NEF-PLGA-NP was as follows:the concentration of PLGA was 20 mg·mL-1, the dosage of NEF was 3.3mg, the ratio of water phase and organic phase was 8:1, the concentration of PVA was 1.0%. The average encapsulation efficiency of resultant nanoparticles was 70.35%, the mean particle size was 213.5nm, and the average zeta potential was-21.0mV. Particle morphology observed by transmission electron microscopy shows that NEF-PLGA-NP have spherical shape, smooth surface, uniform size, good dispersion, and no adhesion between the nanoparticles.The in vitro release profiles of NEF stuff could be described by first order dynamic model and could be expressed by the following equation: Ln (100-Q)=-0.2615t+4.3977 (r=0.9964). The in vitro release behavior of NEF-PLGA-NP investigated in phosphate buffer saline (pH7.4) could be described by Ritger-Peppas equation and could be expressed by the following equation:LnQ=0.2639Lnt+3.2176 (r=0.9931).Release test in vitro showed the nanoparticles have slow-release efrect.CONCLUSIONThe optical formulation method presented here was simple with relative high encapsulation efficiency, large drug loading, and relative concentration of particle size distribution, better shape. In vitro release test showed that the preparation has in sustained effect. It's for the NEF-PLGA-NP delivery system development and application of the theoretical foundation.