Anti-tumor nano prodrug system based on dendrimer and preparation method thereof

Abstract

The invention relates to a multi-function nano prodrug system based on a dendrimer, which belongs to the technical field of biomedicines and nano medical science. The nano system comprises four function parts: an outermost layer RGD (arginyl-glycocoll-aspartate) cyclic peptide as an active targeting head group (1), a polyethylene glycol (PEG) hydrophilic chain segment (2) connected with the targeting head group and the dendrimer, an anti-tumour drug (3) connected with the dendrimer by an acid sensitive chemical bond and a dendrimer kernel (4). The general formula of the nano system is RGD-PEG-Dendrimer-DOX (doxorubicine), wherein the macromolecule attribute of a dendrimer vector makes a vector system passively target to tumor tissues through an EPR (Enhanced Permeability and retention) effect; the RGD cyclic peptide makes the vector system actively target to the tumor tissues through the interaction of a ligand and a receptor and promotes the endocytosis of the tumor tissues; the acid sensitive chemical bond ensures that a drug-carrying system is stable in systemic circulation and releases active drugs after arriving tumor positions and entering an acid organelle to perform the function of cytotoxicity.

Description

technical field [0001] The invention belongs to the technical field of biomedicine and nanomedicine, and relates to an anti-tumor nano-prodrug system based on a dendritic polymer and its preparation method and application. Background technique [0002] Malignant tumors are serious diseases that threaten human health. According to the report of the World Health Organization, there are 10 million new cancer patients and 7.4 million cancer deaths (about 13% of all deaths) in the world every year, and more than 70% of cancer deaths occur in low-income and middle-income countries. By 2010, cancer will overtake heart disease as the number one killer in the world. Although human beings have made remarkable progress in the diagnosis and treatment of tumors in the past few decades, they still lag behind the exacerbation of the disease. At present, the clinically used antineoplastic drugs are generally small molecule drugs, and there are some serious defects in the application of sm...

AI Technical Summary

Problems solved by technology

Although human beings have made remarkable progress in the diagnosis and treatment of tumors in the past few decades, it still lags behind the exacerbation of the disease

At present, the clinically used antineoplastic drugs are generally small molecule drugs, and there are some serious defects in the application of small molecule drugs, such as lack of selectivity, while killing tumor cells, they also have relatively large toxic and side effects on normal cells; Fast, rapid elimination in vivo, resulting in a short half-life in the systemic circulation; tumor cells develop drug resistance after long-term use

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