Preparation And Properties Of Resveratrol Nano-drugs Grafted With Lactobionic Acid Modified Polyamido-amine

Objectives To prepare resveratrol nano-drug grafted with polyamide-amine dendrimer modified by lactose acid and its in vitro performance study.Methods 1 The third-generation polyamide-amine dendrimer carrier was synthesized by the divergent method.LA-PAMAM-Res nano-drug were prepared by partially carboxylating the terminal amino group of the carrier（G3.0 PAMAM-COOH）,and then grafting resveratrol（PAMAM-Res）and amidation reaction to bind lactobionic acid.And it was prepared by physical encapsulation of resveratrol to prepare LA-PAMAM-Res/Res nano-drug.2 Infrared spectroscopy（FTIR）method and nuclear magnetic resonance hydrogen spectroscopy（¹H-NMR）method were used for structural characterization.The laser particle size analysis method examines the particle size and dispersion coefficient of the carrier and nano-drugs.Then the ultrasonic method destroys the structure of the nanodrugs to detect its drug loading.3 Experiments to determine the in vitro drug release performance of nano-drugs by dialysis.The UV-spectrophotometric method was used to detect the hemolysis rate of the carrier and nano-drugs.The MTT method was used to investigate the cytotoxicity of the carrier and nanomedicine.Results 1 In the FTIR detection results,G3.0 PAMAM is the characteristic absorption peak of amide bond at 1 638.69 cm^-1 and 1 560.78 cm^-1.G3.0 PAMAM-COOH shows-OH bending vibration absorption peak at 954.68 cm^-1 is also a characteristic absorption peak of carboxyl group.The PAMAM-Res has a characteristic absorption peak of trans-C=C-at 964.85 cm^-1.And the LA-PAMAM-Res shows a characteristic absorption peak of-C-O-Casymmetrical extension in the galactose ring at 1 139.99 cm^-1.In the search results of ¹HNMR,the G3.0 PAMAM showed a methylene proton peak of-CONHCH2-at δ2.69～2.79.In the PAMAM-Res,δ9.18 and δ6.11～7.40 are the absorption peaks of hydrogen on the hydroxyl group and benzene ring.In the LA-PAMAM-Res,δ5.32 and δ5.91～5.96 are characteristic absorption peaks of lactobionic acid.The above results prove that the LAPAMAM-Res is successfully prepared.2 The particle size of LA-PAMAM-Res and LAPAMAM-Res/Res are（126.3±3.4）nm and（251±15.7）nm,and the drug loading is（7.2±0.9）% and（18.4±1.1）%.The encapsulation rate of LA-PAMAM-Res/Res was（75.1±2.2）%,which proved that LA-PAMAM-Res/Res was successfully encapsulated.3 The cumulative drug release in vitro of LA-PAMAM-Res and LA-PAMAM-Res/Res is（23.83±0.43）% and（35.28±0.72）%,and the hemolysis rate of nano-drugs is high,medium and low When the concentration is lower than 5%,it has biological safety.Carrier G3.0 PAMAM and G3.0 PAMAM-COOH,nano-drugs LA-PAMAM-Res and LA-PAMAMRes/Res,drug Res at 50 μg/m L liver cancer A549 cell survival rates were（58.75±4.18）%,（89.98±3.24）%,（63.76±4.11）%,（59.68±2.06）% and（55.46±3.98）%,demonstrating that terminal carboxylation reduces the carrier’s cytotoxicity,while nanomedicine still has the drug’s anticancer activity.Conclusions Prepared LA-PAMAM-Res and LA-PAMAM-Res/Res nano-drugs with uniform particle size,slow drug release,good biocompatibility,low cytotoxicity and anticancer activity,and LA-PAMAM-Res/Res nano-drug further increases the resveratrol loading.Figure 17;Table 10;Reference 117...