Home > News > Small: the advantages of self-assembled nanoparticles of docetaxel dimer precursor bridged by diselenide Bond: small role, big responsibility

Small: the advantages of self-assembled nanoparticles of docetaxel dimer precursor bridged by diselenide Bond: small role, big responsibility

wallpapers News 2020-12-18

cancer is a serious threat to human health life. Chemotherapy is one of the most effective means to treat cancer at present. It is also called the three major means of cancer treatment together with surgery radiotherapy. However at this stage chemotherapy has the problems of low delivery efficiency poor targeting which leads to poor clinical effect serious side effects. For example docetaxel is widely used in the treatment of non-small cell lung cancer breast cancer. However the clinical targeting delivery of docetaxel injection (docetaxel) is low can cause serious side effects * such as fluid retention bone marrow suppression allergic reactions. In addition due to the low water solubility of docetaxel in order to meet the requirements of clinical medication Taxotere uses Tween-80 ethanol as solubilizers which will cause serious side effects related to excipients. Taxotere also has the problem of poor stability the preparation needs to be used now need to be used within 6 hours. These problems greatly limit its clinical application. Therefore it is very important to design a drug delivery system with high efficiency low toxicity in chemotherapy drug delivery.

have many strategies to improve drug delivery efficiency such as precursor drug strategy nano drug delivery system. Prodrug strategy can effectively improve the adverse properties of chemotherapeutic drugs including low solubility poor stability toxic side effects. Nano drug delivery system can significantly improve the pharmacokinetic properties of drugs prolong the internal circulation time of chemotherapy drugs increase the accumulation of drugs in tumor sites. However prodrugs are easy to be eliminated in vivo while traditional nano drug delivery systems have the problems of low drug loading poor stability excipient related toxicity. Combined with these two strategies we developed a small molecule prodrug self-assembled nano drug delivery system. As small molecule prodrugs can be used as drug carriers release active mother drugs small molecule prodrugs self-assembled nano drug delivery system has shown the advantages of high drug loading good stability low toxicity so on which has become a hot spot in the research of chemotherapy drug delivery in recent years.

small molecule prodrugs self-assembled nano drug delivery systems usually use carbon chain or fatty acid chain to modify drugs to introduce "structural defects" to balance the intermolecular force during assembly. The loading capacity of the self-assembled nanoparticles can reach 50%. Dimer prodrug is the coupling of two molecules of drugs which can further improve the drug loading. However the structure of dimer prodrug coupled with two molecules of drugs is more rigid the intermolecular force is stronger which hinders its self-assembly affects its assembly stability. Therefore how to improve the self-assembly ability of dimer prodrugs is the key to construct ultra-high drug loading nanoformulations.

Sun Jin research group of boundless innovation college of Shenyang Pharmaceutical University designed docetaxel dimer prodrugs with selenium bond as chemical bridge. It was found that compared with disulfide bond carbon bond selenium bond has a bond angle of nearly 90 ° dihedral angle. In the self-assembly process of prodrugs diselenium bond can effectively increase the spatial flexibility of prodrugs significantly enhance the self-assembly ability of prodrugs improve the stability of self-assembled nanoparticles in vivo circulation time tumor accumulation. In vivo in vitro studies show that the diselenium bond has double sensitivity to redox can intelligently release the mother drug in tumor microenvironment. At the same time the diselenium bond can disturb the redox equilibrium of tumor cells increase the level of oxidation state further promote the apoptosis of tumor cells. Docetaxel dimer prodrug bridged by selenium showed good antitumor effect in both in situ ectopic tumor bearing mice models effectively alleviated the systemic toxicity of docetaxel. Relevant research results are published in small an international well-known journal in the field of nanotechnology( DOI:10.1002/smll.202005039 )。


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