A preparation method for delivering 5-fluorouracil microspheres

Abstract

The invention discloses a method for preparing 5-fluorouracil delivery microspheres, wherein the method includes the steps of modification of butanedioic anhydride, preparation of sodium alginate microspheres, preparation of sodium alginate-chitosan microspheres, and preparation of sodium alginate-chitosan-carrageenan microspheres. The beneficial effects comprise that the surface of the sodium alginate microspheres is coated with two polysaccharide layers, an LBL structure is formed, surface voids of the prepared core-shell type multilayer microspheres are reduced, delivery active ingredientscan reach colons through an acidic gastric juice, and a certain effect of targeted therapy is achieved; the sodium alginate-chitosan-carrageenan microsphere system shows extremely high sensitivity ina colonic weakly alkaline environment with the pH of about 7.4, has the swelling ratio in 30 minutes reaching 20 or more and has good targeting swelling selectivity at colon positions; with the selectivity, the sodium alginate-chitosan-carrageenan microspheres are expected as a special preparation colon targeted drug delivery carrier and have high market prospect.

Description

technical field [0001] The invention relates to the field of preparation of microspheres for delivery media, in particular to a preparation method for delivery of 5-fluorouracil microspheres. [0002] technical background [0003] Oral preparations are currently the most common and effective treatment approach, but for some preparations, oral preparations have many disadvantages, such as the active ingredients of these preparations will be decomposed in the acidic gastric juice or enzyme fluid medium in the body, thus losing the therapeutic effect. In recent years, there has been a significant increase in the medical field of research on controlled-release delivery systems aimed at improving therapy, reducing side effects, and increasing the desired therapeutic effect of formulations. Many literatures have been published using corresponding materials and methods to prepare controlled-release delivery systems, but unfortunately, most of the methods use harmful raw materials, t...

AI Technical Summary

Problems solved by technology

[0005] There are many methods about the microsphere technology of sodium alginate loaded with active ingredients. The existing technology, such as the Chinese invention patent with the authorized public number CN102885710 B, discloses a sodium alginate / chitosan / collagen compound loaded with active ingredients. Microspheres and their preparation method. The inventive method uses collagen, sodium alginate, and chitosan as carrier materials to prepare microspheres loaded with various cosmetic active ingredients. The surface of the microspheres is smooth and round, with good monodispersity and particle size distribution. Uniformity and other advantages, but the lysozyme swollen with sodium alginate / chitosan / collagen composite microspheres in the inventive method is an aqueous solution of butanediol and hyaluronic acid, which has strict requirements on the pH value of the lysozyme, which limits The scope of application is widened, and a variety of divalent cations such as Co 2+ , Zn 2 + , Mn 2+ , Ni 2+ , will affect the active ingredients of cosmetics, and its preparation process is relatively cumbersome, the process is not easy to control, and it is difficult to apply on a large scale