| 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 ?2.69?2.79.In the PAMAM-Res,?9.18 and ?6.11?7.40 are the absorption peaks of hydrogen on the hydroxyl group and benzene ring.In the LA-PAMAM-Res,?5.32 and ?5.91?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 ?g/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... |
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