结肠靶向.pptVIP

口服结肠靶向给药系统简介;概念;;时间依赖型OCDDS; pH依赖型OCDDS; 由于结肠中内容物较多，水分较少， 肠道蠕动会直接对药物产生压力， 药 物因不能耐受结肠蠕动产生的压力而崩解溶出，这是压力控制型OCDDS 的设计思路。;新型口服结肠靶向给药系统;结肠靶向给药治疗的优点：;结肠靶向给药治疗的优点：;A novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting;图1 FR 介导的内吞作用过程;Methods: Ternary phase diagrams were constructed in order to obtain the most efficient self-emulsification region, and the formulation of curcumin-loaded SMEDDS was optimized by a simplex lattice experiment design. Then, three lipophilic folate derivatives (folate-polyethylene glycol-distearoylphosphatidylethanolamine, folate-polyethylene glycol-cholesteryl hemisuccinate, and folate-polyethylene glycol-cholesterol) used as a surfactant were added to curcumin-loaded SMEDDS formulations. An in situ colon perfusion method in rats was used to optimize the formulation of FSMEDDS. Curcumin-loaded FSMEDDS was then filled into colon-targeted capsules and the in vitro release was investigated. Cytotoxicity studies and cellular uptake studies was used in this research.;Results: The optimal formulation of FSMEDDS obtained with the established in situ colon perfusion method in rats was comprised of 57.5% Cremophor? EL, 32.5% Transcutol? HP, 10% Capryol? 90, and a small amount of folate-polyethylene glycol-cholesteryl hemisuccinate(the weight ratio of folate materials to Cremophor EL was 1:100). The in vitro release results indicated that the obtained formulation of curcumin could reach the colon efficiently and release the drug immediately. Cellular uptake studies analyzed with fluorescence microscopy and flow cytometry indicated that the FSMEDDS formulation could efficiently bind with the folate receptors on the surface of positive folate receptors cell lines. In addition, FSMEDDS showed greater cytotoxicity than SMEDDS in the above two cells.;Conclusion: FSMEDDS-filled colon-targeted capsules are a potential carrier for colon delivery of curcumin.;