Study On Curcumin Eudragit E100 Nanoparticles

Objective The new and active compounds were spring up at the contemporary study on pharmacology, but there is a little of them can be used in the clinical. And the most important reason is their inherent nature of the poor stability and weak solubility. The technique of nanometer medicine has been proved can raise the solubility of insolubility compound and enhance its stability as the compound encapsulated by the nanomaterial. The aim of our study was to develop a novel curcumin-loaded Eudragit E100 nanopaticles(Cur-E100-NPs) system and to evaluate its value of utilization in improving the water solubility and bioavailability by oral administration.Methods Cur-E100-NPs were prepared by nanoprecipitation technique, with Eudragit E100 as the carrier material, alcohol as the organic solvent, poloxamer 188 as the surfactant, m cur、m E100、v water:v oil et al as the investigation factor. The orthogonal design was applied to the optimization of the formulation based on the encapsulation efficiency. A high performance liquid chromatography(HPLC) method was developed for the determination of CUR in the CUR-E100-NPs. The particle size distribution, dissolution rate and the stability of the preparation were determined. The stability of the sample about the encapsulation efficiency was investigated. A HPLC method was developed and applied for the determination of the pharmacokinetics of CUR of Curcumin suspension(CUR-SUS) formulations and CUR-E100-NPs in rat plasma.Results The optimized formulation by orthogonal design was consisted of CUR 5 mg, Eudragit E100 50 mg, ethanol 2 m L, 1% Poloxamer 188 10 m L. The encapsulation efficiency and drug loading were approximately 50.52% and 5.11%, respectively. The CUR-E100-NPs carried a particle size of 130.7 nm. The drug-loaded nanoparticles were spherical observed by the transmission electric microscope(TEM). The release study in vitro showed that the cumulative release value of the CUR-E100-NPs was 74.40% in simulated intestinal fluid, while was 44.33% in simulated gastric fluid in 12 h. A sensitive and selective method using HPLC has been developed and validated to determine the CUR in rat plasma. The method showed good reproducibility with intra-day and inter-day precision, as well as accuracy with inter-and intra-assay accuracy. The pharmacokinetics study indicated that the major pharmacokinetic parameters was significant different after administration the CUR-E100-NPs and the CUR-SUS. The AUC0→t of CUR-E100-NPs was 12.46 times more than CUR-SUS.Conclusions CUR-E100-NPs prepared by nanoprecipitation method that is reliable had high encapsulation efficiency and good stability. The dissolution and the bioavailability of the CUR from the CUR-E100-NPs obviously were improved compared to the reference formulations that were proved by the in vitro and in vivo expriments. This paper supported the theory foundation for the development and application of CUR-loaded nanoparticle drug delivery system.