PLA-PEG-PLA dendritic polymer

Abstract

The invention discloses a PLA-PEG-PLA dendritic polymer as well as a preparation method and an application thereof. The preparation method is simple, because of special molecular structures of hydrophobic chain segments of the dendritic polymer, winding degree of the chain segments in a micelle core is higher than the winding degree of a line type polymer, and medicaments which are embedded in the product are not easy to dissolve out, so that stability of the drug loaded micelle is improved; quantity of end groups of the dendritic structure is higher than the quantity of end groups of the linear polymer, so that the modification effects aiming at end groups are more obvious than the effects of the linear polymer; the structure of the micelle formed by the dendritic polymer is tight, the particle size is small, EPR effects are easy to perform, and the polymer has good targeting ability for tumor tissue of tumor. The dendritic polymer can be used as a drug carrier and applied to preparation of medicinal preparation.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a PLA-PEG-PLA dendritic polymer, a preparation method and an application thereof. Background technique [0002] Polymer micelle is a nano-drug controlled release system developed in recent years mainly for insoluble drugs. The polymer micelle drug delivery system can significantly improve the solubility of the drug; reduce the toxic and side effects of the drug, thereby increasing the therapeutic dose; the drug is encapsulated in the core to avoid drug degradation and inactivation; the micelle particle size is very small, usually below 100nm, It can avoid the phagocytosis of the reticuloendothelial system (RES), prolong the systemic circulation time, and achieve passive targeting of tumors by enhancing the penetration effect (EPR effect), thereby improving the therapeutic effect. So far, the most important materials for forming micelles are still amphiphilic block co...

AI Technical Summary

Problems solved by technology

For example, patent 201010001047 discloses a method of adding amino acid to the micellar solution to improve the stability of the micelles, but it is not known whether the amino acid component as an auxiliary additive can still maintain the stability of the micelles after being diluted with blood after entering the body , so the effect of in vivo use is not clear; the added amino acid, as a non-inert component, also has uncertainty about whether it will affect the efficacy of the drug

In addition, some studies have suggested that embedding paclitaxel and docetaxel in block copolymer micelles can significantly improve the stability of the micelles. currently unknown

[0007] In summary, the development of micellar preparations is facing great difficulties. On the one hand, the selection of polymer excipients that have been clinically proven safe for drug delivery systems is extremely limited, and the development of a new type of polymer excipients is undoubtedly at great risk

Secondly, the efficacy of various micellar preparations that have been reported is difficult to significantly improve compared with traditional preparations. For example, Genexol PM, a paclitaxel micelle developed by South Korea’s Samyang Corporation, has completed phase III clinical trials in the United States, but its efficacy is not obvious. Has not yet received FDA marketing approval

Third, the micellar excipients that have been reported so far have poor versatility. Usually, one excipient can only form micelles for one or two active ingredients of drugs, which affects its popularization and application.

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