Preparation And In Vivo Distribution Of Dendritic Macromolecule-Loaded Resveratrol Nanoliposomes

Objectives The stability and distribution of resveratrol nanoliposomes were investigated.Methods 1 3.0G,4.0G,5.0G polyamide-amine dendritic macromolecule nano-carriers were synthesized by divergence method,and acetylate it.Carrier characterization:¹H-NMR,IR and laser particle size analyzer;2 Resveratrol liposomes were prepared by reverse evaporation,and the carrier algebra,reaction time and pH were controled.In addition,the optimum preparation conditions were determined by carrying dosage and encapsulation rate,and the particle size was determined.3 The accelerated centrifugal method and long-term stability experiment were performed;4 The pharmacokinetics and tissue distribution of resveratrol liposomes after intravenous injection were investigated by using resveratrol standard products as the control.The pharmacokinetic parameters were calculated by DAS 2.0 program,and both Re and Te were calculated.Results 1 ¹H-NMR:PAMAM absorbed at 3.219³.245 ppm and 2.702².777 ppm,respectively.PAMAM-Ac absorbed at 1.866 ppm;IR:PAMAM and PAMAM-Ac were absorbed at 1645.50 cm^-1 and 1558.25 cm^-1,respectively;2 The PAMAM particle size was?8.00±1.30?nm and the PAMAM-Ac particle size was?8.07±0.71?nm,the characterization results showed that the Nano-carrier PAMAM and PAMAM-Ac were synthesized successfully.3 The optimum preparation conditions of resveratrol liposomes were as follows:4.0G PAMAM were used as the carrier,under the condition of pH=7,25?,shocked more than 60 h,the measured particle size was?167.3±21.7?nm,the average dosage was 79.21 mg/mL,and the encapsulation rate was 73.65%.4 The stability parameter?K_E?was less than 0.15,and the drug had no obvious precipitation precipitation;5 The distribution of resveratrol liposomes in rats was in accordance with the non-compartment model,the main pharmacokinetic parameters were as follows:AUC_?0-??=?45.50±5.95?mg/L·h,T1/2z=?0.98±0.15?h,MRT?0-t?=?1.42±0.19?h,Clz=?0.71±0.09?L/h/kg,According to the pharmacokinetic parameters,the Re of the Res liposome in the liver and kidney tissues were 2.156 and 2.739,respectively,and the Rte were 1.119 and 1.425,respectively.The results were all greater than 1,indicating that Res nanoliposomes have liver and kidney targeting in vivo.Conclusions Resveratrol liposomes with good stability were synthesized,which increased the targeting of liver and kidney,prolonged the metabolic time of resveratrol in vivo.In a word,resveratrol liposomes improved the bioavailability in vivo compared with resveratrol standard products.Figure 22;Table 12;Reference 111...</sub>