| Immunosuppressant inhibitory effect of drugs on the body’s immune response, can inhibit the proliferation and function of cells in the immune response (T and B cells macrophages) can reduce the antibody immune response. Immunosuppressant is mainly used in organ transplant anti-rejection and autoimmune disease. In this thesis, is used cyclosporine A as drug model, used natural polysaccharide sodium alginate and chitosan as the main carrier material, the use of pulsed electric field process preparation contained cyclosporine A calcium alginate/chitosan microspheres. Preparation of drug-loaded microspheres was studied in detail, preliminary experiments in vitro release of the microspheres. Get the following conclusions:1.In order to prepare the ocular topical administration to the requirements of the small particle size of drug-loaded microsphere formulation of microsphere preparation process were studied and optimized. Add the oil and surfactant in the raw material liquid formulations used to increase the solubility of cyclosporin A and reduce the surface tension of the feed solution, it is a good preparation of small particle size of drug-loaded microspheres. Add appropriate concentrations of surfactants and NaCI in Gelation to reduce the surface tension of the gel bath, is conducive to the formation of a better form of drug-loaded microspheres. The impact of these additives is not on the stability of cyclosporin A in a short period of time.2.According to the formation principle of microemulsion and the ternary phase diagram, to determine the MCT as a suitable oil to improve the solubility of cyclosporin A in the aqueous phase, then add the appropriate amount of surfactants to reduce the interfacial tension between oil phase and water phase, to determine the composition and proportion of the raw material liquid.3.Determine the optimal preparation process of drug-loaded microspheres:0.8wt%of sodium alginate solution,6.5wt%of the Tween20,1:1.5oil-water volume ratio and65mg dosage of cyclosporin A in the raw material liquid.4wt%of CaCl2,2%NaCl0.4wt%of1631and0.6wt%of the PEG600in the gelation. In this process conditions, the particle size of microspheres to accord with the local administration of eye requirements and uniform distribution, and to ensure a high level of cyclosporine A encapsulation efficiency with good reliability and repeatability. 4.Preliminary study on the experiment in vitro release of the drug-loaded microspheres, investigate under different conditions of the drug cumulative release rate changes over time.Through the detection of drug concentration obtain conclusion of the microspheres to prolong drug action. |