Preparation And Antitumor Application Of Baicalin Self-loaded Nano Delivery System

Objectives To prepare baicalin(BAI)self-loading drug nano delivery system to achieve synergistic anti-tumor effect,by loading emodin(EMO)or doxorubicin(DOX).Methods SA-SS-BAI polymer was prepared by linking sodium alginate(SA)and BAI with cystamine(CYS)as linking arm.SA-SS-BAI NPs were prepared and characterized by particle size,Zeta potential and scanning electron microscopy.The critical micelle concentration(CMC)was determined by pyrene fluorescence probe method.EMO/SA-SSBAI NPs and DOX/SA-SS-BAI NPs were obtained by wrapping EMO and DOX respectively;drug loading and encapsulation efficiency were determined by HPLC;the stimulus response experiment verifies the dual response;in vitro release experiments evaluated the release of drug-loaded nanoparticles under different conditions;cell uptake experiment investigated the uptake ability of Hep G2 cells to nanostructures;MTT was used to investigate the in vitro antitumor activities of the two drug-loaded nanoparticles.Finally,H22 tumor-bearing mice were used to verify the anti-tumor ability of DOX/SA-SS-BAI NPs.Results The CMC and particle size of prodrug nanoparticles with different degrees of substitution were determined,and the optimal prodrug nanoparticles were selected to be about 149 nm;hemolysis experiments proved that SA-SS-BAI NPs met the requirements of injection preparations.Drug loading of EMO/SA-SS-BAI NPs was(15.72±0.38)%,encapsulation efficiency was(54.31±3.11)%,and particle size about 219 nm;drug loading of DOX/SA-SS-BAI NPs was(16.22±0.06)%,encapsulation efficiency was(64.34±0.25)%,and particle size about 158 nm;stimuli responsiveness confirms p H/reduction dual response of two drug loaded nanoparticles;in vitro release showed that the two drug-loaded nanoparticles had the fastest release rate under the dual conditions of acid and high concentration of GSH.Cell uptake proved that nanostructures were more easily absorbed by cells;MTT experiment showed that the two drug-loaded nanoparticles had obvious anticancer effect.Animal experiments showed that DOX/SA-SS-BAI NPs had good anti-tumor ability.Conclusions SA-SS-BAI polymer and EMO/SA-SS-BAI NPs and DOX/SA-SS-BAI NPs were successfully prepared.Baicalin self-loaded nanoparticles had high drug loading,dual response,and good anti-tumor ability and synergistic effect.Figure 37;Table 23;Reference 102...