Gel injection of sustained-released topology enzyme inhibitor and preparation method thereof

Abstract

The invention relates to a slow-release topoismerase inhibitor gel injection which contains an anticancer-effective amount of topoismerase inhibitor microspheres (or microsphere and topoismerase inhibitor micropowder), an amphiphilic block polymer composed of polyethylene glycol and polyester, a solvent and a certain amount of slow-release regulator. The amphiphilic block polymer aqueous solution is liquid at the room temperature and turns into a semisolid or solid biodegradable water-insoluble gel in vivo in warm-blooded animals, so that the topoismerase inhibitor encapsulated therein is sustainedly and locally released around the tumor and the microspheres can further control the slow release for a plurality of weeks to a plurality of months. After the intratumoral injection or peritumoral injection or post-operative intracavitary injection or arterial embolization, the slow-release topoismerase inhibitor gel injection can significantly reduce the general drug reaction and selectively enhance the curative effect of non-operative treatment such as chemotherapy and radiotherapy, and is used for the treatment of tumors of different stages. The topoismerase inhibitor is selected from camptothecin, topoteean, etoposide, teniposide, esorubicin, pirarubicin and valrubicin.

Description

(1) Technical field [0001] The invention relates to a sustained-release gel injection containing a topozyme inhibitor, which belongs to the technical field of medicines. Part or all of the topozyme inhibitor in the gel sustained-release injection is present in the sustained-release microspheres. The dual sustained release of the gel and the microspheres can prolong the release time of the topoenzyme inhibitor contained in the local tumor. Several weeks to several months. (2) Background technology [0002] There are many ways to treat solid tumors and many related studies have been reported. However, the survival conditions of most patients have not been significantly improved in the past few decades. Among various treatments, chemotherapy is still one of the commonly used options. Although conventional chemotherapy has been used for a long time, its therapeutic effect on solid tumors is uncertain. The fundamental problem is that traditional chemotherapy cannot achieve effective d...

AI Technical Summary

Problems solved by technology

Therefore, in most cases, the final sustained-release formulations are mostly solid shapes (eg, microspheres, tablets, or rods), which require a more complicated implantation process and are prone to tissue trauma and even tumor cell seeding or dissemination

In addition, organic solvents or high heat processes often lead to the degradation and denaturation of many anti-cancer active ingredients

[0005] Solid implants cannot effectively cover the irregular tumor cavity after tumor resection, so the residual tumor cells cannot be effectively removed after surgery, and postoperative recurrence cannot be effectively controlled