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A dendrimer-based anti-tumor nano-prodrug system and its preparation method

A polymer and dendritic technology, applied in the field of biomedicine and nanomedicine, can solve the problems of drug resistance of tumor cells, lagging disease progression, short half-life, etc., to achieve the effect of optimizing in vivo behavior, improving solubility, and reducing toxic and side effects

Inactive Publication Date: 2012-02-01
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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

Method used

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  • A dendrimer-based anti-tumor nano-prodrug system and its preparation method
  • A dendrimer-based anti-tumor nano-prodrug system and its preparation method
  • A dendrimer-based anti-tumor nano-prodrug system and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] 1. Synthesis of CAD:

[0042] Weigh 27mgCA (173.1mol), dissolve it in 1ml dioxane, add dropwise to 10ml aqueous solution of 30mgDOX (51.7mol) at room temperature, use 0.5N sodium hydroxide solution to maintain the pH of the whole process at 8.5- 8.7, continue to react for 10 minutes, adjust the pH value to about 7.4, put it in the refrigerator to cool to 4°C, adjust the pH to 2.5-3 with 1N HCl at 4°C, extract with ethyl acetate (50ml×2), collect the organic layer, Use saturated sodium chloride and anhydrous sodium sulfate to remove water, and distill under reduced pressure to obtain a bright red powdery solid. The purity of HPLC analysis product (Hypersil ODS C18 column (4.6 * 250mm, 5m), column temperature is 30 ℃, mobile phase is 3% ammonium carbonate aqueous solution (w / w) / methanol=1 / 2 (v / v), carries out The sample volume is 20l, and the flow rate is 1.0ml / min).

[0043] 2. Synthesis of RGDyC-PEG-G4 PAMAM:

[0044] Weigh 10.5mg of RGDyC (17.6mol), dissolve in 2.1m...

Embodiment 2

[0048] The same test method as in Example 1, fixed the molecular weight (5000Da) of G4 PAMAM and MAL-PEG-NHS, changed the feeding ratio of PEG / PAMAM, and prepared nano drug-loading systems with different degrees of PEG modification.

Embodiment 3

[0050] In the same test method as in Example 1, G4 PAMAM was fixed, and the molecular weight of MAL-PEG-NHS was changed to 1000Da, 2000Da, 3400kDa, 10000Da to prepare PEG-modified nano drug-loading systems with different molecular weights.

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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...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K31/704A61P35/00A61K47/59A61K47/60A61K47/64
Inventor 姜嫣嫣朱赛杰裴元英洪鸣凰
Owner FUDAN UNIV
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