Objective To determine the inhibitory effect of emodin-containing shape memory gastric retention composite membrane on the proliferation of SGC-7901 gastric cancer cells in vitro,and evaluate the efficacy of gastric retention and bioavailability of composite membrane.Methods The optimal ratio of polylactic acid(PLA)to poly-propylide carboxate(PPC)was based on floating time,shape recovery and cumulative release rate of emodin in the composite membrane.CCK-8 method and cell scratch test were used to evaluate the inhibitory effect of composite membrane on the proliferation of gastric cancer cells.The pharmacokinetics of the best composite membrane PLA/PPC(6/4)@SD in rats were studied by HPLC.The gastric retention of solid dispersion(SD)and PLA/PPC(6/4)@SD in mice was analyzed by in vivo imaging.Results The optimal ratio of PLA to PPC in the composite membrane was 6:4,its continuous floating time was longer than 12 h,the deformation recovery of the composite membrane reached 79％at 37 ℃,and the drug release rate was up to 57.36％after 24 h.The in vitro experiments showed that emodin-containing composite membrane had obvious inhibition on SGC-7901 gastric cancer cells.The pharmacokinetic experiment showed PLA/PPC(6/4)@SD effectively improved the bioavailability of emodin in rats,and the bioavailability increased by 375％as compared with emodin(EMO)and 166％as compared with SD group.The gastric retention time of PLA/PPC(6/4)@SD group could reach 12 h.Conclusion The prepared emodin-containing shape memory gastric retention membrane can prolong the retention time of emodin in the stomach,improve the bioavailability of emodin,and effectively inhibit SGC-7901 gastric cancer cells,serving as an adjuvant treatment of gastric cancer.
关键词
形状记忆聚合物/大黄素/胃癌/活体成像
Key words
shape memory polymer/emodin/gastric cancer/in vivo imaging
维普
万方数据