Study About Synthesis And Properties Of New Cyclodextrin Derivatives

Objective Using inclusion drug molecules of cyclodextrin, new cyclodextrin metal-organic framework(CD-MOF) were synthesized. Furthermore, CD-MOFs as inclusion materials are used to include the drug molecules, in order to improve the inclusion rate and enhance their solubility.Methods New cyclodextrin based metal-organic frameworks were synthesized by the solvothermal method and characterized by X-ray single crystal diffraction?Infrared spectroscopy(IR), Elemental analysis and X-ray powder diffraction; New cyclodextrin metal-organic frameworks were used to include and load drug molecules, which was studied by NMR?IR?DSC?HPLC. The release properties of inclusion and lading compounds were explored by the turning basket method; The invitro cytotoxicity were researched by the method of CCK-8.Results Three new cyclodextrin metal-organic frameworks were successfully isolated; The drug molecules can be included and loaded into CD-MOFs; The results of releasing experiments show that CD-MOFs possess obvious sustained release effects; The results of solubility experiments show the solubility of inclusion were increased; The results of invitro cytotoxicity show that CD-MOFs can reduce the drug toxicity significantly and the corresponding IC50 value was obtained.Conclusion In this paper, three new CD-MOFs were synthesized successfully by using different reaction solvent, and formula as follows: K(C42H72O35)·11H2O(CD-MOF-1) Na(C42H72O35)·11H2O(CD-MOF-2);(NaOH))4(C42H72O35)2·H2O(CD-MOF-3). The technology optimization about ferulic acid(FA) inclusion complex is studied by using CD-MOF-1 as including materials, and the optimal technology was as follows: the mol ratio for 1:3(drug to CD-MOF-1), 1.0 h dropping time, inclusion temperature for 40? and 1.0 h inclusion time. The solubility of FA increases 15 times after the formation of inclusion complex; 5-FU and quercetin can be included into the CD-MOF-2 at the same time. 5-FU can be loaded into CD-MOF-3, the releasing results showed that drug could release smoothly within 200 min, and the accumulation release of 5-FU is 81.02%; The results of invitro cytotoxicity show that CD-MOF-1, CD-MOF-2 and CD-MOF-3 are non-toxic drug carrier, IC50 value for 5- FU-CD-MOF-3 was 0.145 ug/mL, which indicates the load of drug toxicity is reduced significantly.