Optimization Of Formulation And Preparation Procedure Of Nanoparticles

As a new dosage form, Nanoparticles is a promising drug delivery system. It has the exploring potential and utility value. Compared with other conventional dosage forms, Nanoparticles can overcome many disadvantages. Nanoparticles has extensive medical prosepects on the aspects the transport of the gene、antineoplastic、 antiviral due to its advantages such as passive targeting,noncytotoxicity, immunogenicity,high gene transfer and so on.However, Nanoparticles has some disadvantages,the future studies should be focusd on the following aspects:(1) discover and synthetize the new macromolecular materials with non-toxic, well biocompatibility and biodegradablity;(2)modify the surface of nanoparticles which can improve passive targeting, controllability, stability, entrapment efficiency and the drug loading of the nanoparticles;(3)research the function mechanism and monitor the carrier material in vitro and vivo;(4)optimize prescription and preparation technology in order to industrial-scale production of nanoparticles.The topic prepare different kinds of nanoparticles by two methods with Tilmicosin as the model drug,Inspect and optimize its prescription and preparation technology.The nanoparticles were prepared by evaporating ethanol solution containing Eudragit L100, and the tilmicosin was used as model drug. To study the formulation and procedure of prepare Eudragit L100nanoparticles loaded with tilmicosin, and observe the encapsulation efficiency and release behavior in vitro.First of all, the effective method of detecting encapsulation efficiencies mainly studied in this experiment. The nanoparticles and free drugs were separated by sephadex filtration, dialysis bag method and ultrafiltration, and ultimately determine the dialysis bag method as encapsulation efficiency measurement methods; secondly, to investigate the single factor of parameters of technic process and formulation of nanoparticles, general range of technic factors and prescription factors of influence of the nanoparticles quality were studied by single-factor test, and the optimal condition were definited by orthogonal experiment.Finaly, the encapsulation efficiency and release test were determined by using dialysis bag. The obtained nanoparticles were spherical with a solid dense structure. They have average particle size of (45.6±4.8) nm with uniformed distribution. The encapsulation efficiency was higher than95%, and drug loading coefficient was (20.64±0.36)%. The release of tilmicosin-NPs distinctly depended on the pH conditions, and decreased the release efficiency values. By using the means of evaporating ethanol solution, The resulting nanoparticle with higher encapsulation efficiency is promising in decreasing the release efficiency.Investigate the prescription and preparation technology of solid lipid nanoparticles with Tilmicosin as the model drug by W/O microemulsion method.First,screening the prescription by making Pseudo-ternary phase diagram in order to make sure the prescription and the best ratio, ensure the critical point of the micro emulsion by staining method and conductimetric method. Preparation technology was screened by single factor experiment and then make sure the optimum technological conditions。Then the topic studied the methods to improve the encapsulation efficiency and drug loading capacity of the SLN with mixed lipid as the carrier material, simultaneously, to solve the dumping effect when released in the vitro。study the shape, stability and release degree in vitro of the solid lipid nanoparticles by the two methods. The mean grain size should be about200nm,and the encapsulation efficiency should be more than85%of the solid lipid nanoparticles by micro-emulsion method.They should have non significant change placed3months on the condition of4℃. This solid lipid nanoparticles should has the good effect of sustained-release.