Novel drug-loaded microsphere and preparation method thereof

Abstract

The invention relates to a novel drug-loaded microsphere and a preparation method thereof. The preparation method comprises the following steps: pre-mixing a polyvinyl alcohol aqueous solution with hydroxyapatite particles, adding concentrated hydrochloric acid as a catalyst, adding a cross-linking agent glutaraldehyde to obtain a reaction solution, carrying out a pre-reaction for 3-30 seconds, dropwise adding a pre-reaction solution into a mixed oil phase containing liquid paraffin and sorbitan fatty acid ester before the pre-reaction solution is coagulated, stirring and reacting in an oil bath at 50-60 DEG C for at least 3 hours, and then filtering, washing and drying the reacted mixture to obtain the drug-loaded microspheres. The method provided by the invention is beneficial to batch production, the drug-loaded microspheres prepared by the method have high drug loading capacity and encapsulation efficiency and good slow release effect, and the hydroxyapatite particles are embeddedinto the polyvinyl alcohol after polymerization reaction, so that the drug-loaded microspheres have a certain developing function.

Description

technical field [0001] The invention relates to a drug-loadable microsphere and a preparation method thereof. Background technique [0002] Microspheres can be used as drug-loading carriers in medicine, or as interventional embolic materials. Common drug-loading microsphere materials include polyvinyl alcohol microspheres, gelatin microspheres, sodium alginate microspheres, polylactic acid microspheres, and albumin microspheres. ball and so on. For example, liver cancer can be treated with interventional methods in clinical treatment, and the interventional material is embolic microspheres. The microspheres have two functions: first, the microspheres block the blood vessels in the tumor target blood vessels, blocking the nutrient source of the tumor cells. Second, the microspheres can be loaded with drugs, and the released drugs can play a role in curbing tumor growth. The title of the patent is "A Preparation Method of Polyvinyl Alcohol / Hydroxyapatite Composite Microsphe...

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Problems solved by technology

[0010] Among the methods of the above-mentioned prior art, the electrostatic spray method is not suitable for temperature-sensitive, heat-labile protein polypeptide microspheres, and it is also difficult to control the particle size of the microsphere particles

The emulsification cross-linking method takes a long time in the preparation of microspheres, is easily affected by the environment and is not suitable for the large-scale preparation of microspheres, and the cross-linking agent has certain toxicity

The phase separation method needs to use a large amount of organic solvents in the preparation process, but these solvents are difficult to remove from the microspheres and bring certain toxicity, so this method is easily affected by the addition of coagulants and solvent residues

The solvent evaporation method is affected by temperature. If the temperature is too low, the microsphere formation time will be prolonged and the encapsulation efficiency will be reduced; The burst release is severe, and the particle size of the microspheres will become larger

[0011] There are many problems in the existing technology, such as the particle size of the prepared microspheres cannot be adjusted, the production process is complicated and easily affected by the environment, and it is not convenient for mass production, there are restrictions on the loading of temperature-sensitive drugs, the development effect is not good, and the microspheres are loaded with drugs. The rate is not high, the sustained release effect is not ideal, etc.

Therefore, the current microspheres mainly have the problems of complex and unstable production process and low drug loading capacity.

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