The Preparation And Preliminary Quality Evaluation Of Chitosan-coated Cur Liposomes

Curcumin (CUR) is a multi-hydroxy compound extracted from Curcuma Genusplants, with a variety of pharmacologically active anti-tumor, anti-inflammatory,anti-HIV, anti-oxidation, lowering blood pressure, etc., and a wide spectrum of cancer,drug side effects, has important implications for cancer treatment. However, due to lowwater solubility, oxidation, low bioavailability, clinical application is limited. Liposomes(LP) is closed in a similar biofilms vesicle bilayer structure composed of phospholipidsand cholesterol. Ordinary LP be modified to improve its stability, increased targeting oftumor cells and cytotoxicity. Chitosan (CS) is a non-toxic natural polysaccharide polymercompound having excellent biocompatibility and biodegradability.In order to improve the oral bioavailability of CUR, the subject preparedchitosan-coated curcumin liposomes (CCLP), and research from the following four parts:The first part examines the CCLP preparation methods and the physical andchemical properties. This experiment adopts film dispersion method to prepare CLP, withCS to cladding CLP, CCLP is prepared. Glucan gel column method for determining theenvelopment efficiency (EE%) of CCLP, the EE%was (71.42±2.14)%. Theexperimental results demonstrate the average particle size and zeta potential were550.1nm and+12.7mV. The physicochemical properties of the optimal formulation of CCLPwere investigated by Transmission electron microscope(TEM).The second part adopts the dynamic dialysis method to examines the CCLP indifferent release media in vitro, The behaviors of CCLP in various release media (0.1mol/L HCl and pH6.8PBS) were all fits the Weibull model. The release behaviors ofCCLP in different media were similar. Release behavior between CCLP and CUR presence significant differences, the vitro dissolution behavior was changed.In the third part, the intestinal permeability of CCLP was studied using in situ singlepass perfusion model. The ultraviolet spectrophotometry method was used to investigatethe absorption and determine the concentration of analyze the data. The result showedthat the absorption rate constant (Ka) and Effective permeability (Peff) of CCLP are betterthan free CUR.The fourth part of the experiment is pharmacokinetic. After oral administration ofCCLP, the concentrations of CUR at different time in rats were determined by HPLC andthe pharmacokinetic parameters were computed. Compared to the free CUR, thebioavailability of CCLP in rats was increased remarkably after oral administration ofCCLP.