Supermolecular assembly for targeted conduction of anticancer taxol prodrug and preparation method thereof

A technology of supramolecular assembly and targeted delivery, which can be applied in the direction of antineoplastic drugs, drug combinations, and pharmaceutical formulations, and can solve the problems of great impact on physical condition and quality of life, severe side effects of paclitaxel, toxicity, and neurotoxicity. Achieve similar anticancer activity, reduce toxic and side effects, and simple preparation process

Inactive Publication Date: 2014-11-05
NANKAI UNIV
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Problems solved by technology

However, paclitaxel has serious side effects and is insoluble in water. Clinically, it can only be dissolved with the aid of polyoxyethylene castor oil, citric acid and absolute ethanol, and ...

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  • Supermolecular assembly for targeted conduction of anticancer taxol prodrug and preparation method thereof
  • Supermolecular assembly for targeted conduction of anticancer taxol prodrug and preparation method thereof
  • Supermolecular assembly for targeted conduction of anticancer taxol prodrug and preparation method thereof

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Embodiment

[0029] A supramolecular assembly for targeted delivery of paclitaxel prodrug, which is a binary supramolecular assembly synthesized based on permethylated cyclodextrin modified hyaluronic acid and porphyrin modified paclitaxel prodrug, in which permethylated cyclodextrin The molecular formula of refined hyaluronic acid is (C 14 h 21 NO 11 ) 409 (C 78 h 135 N 3 o 44 ) 64 , an average of 64 fully methylated cyclodextrin units are modified on one polymer chain, and the chemical formula of porphyrin-modified paclitaxel is C 92 h 79 N 5 o 15 ; The binary supramolecular assembly uses strong non-covalent interaction between fully methylated cyclodextrin and porphyrin and amphiphilic interaction between molecules to form a hydrophobic porphyrin with a hydrophilic hyaluronic acid as the shell. The paclitaxel prodrug is modified as a supramolecular nanoparticle with the inner core, and the particle size of the nanoparticle is 30-40 nm.

[0030] The preparation method of the ...

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Abstract

The invention discloses a supermolecular assembly for targeted conduction of anticancer taxol prodrug. The supermolecular assembly is a binary supermolecular assembly which is synthesized from full-methylated cyclodextrin modified hyaluronic acid and porphyrin modified taxol prodrug, the binary supermolecular assembly is formed into supermolecular nano particles which take hydrophilic hyaluronic acid as shells and hydrophobic porphyrin modified taxol prodrug as kernels based on the strong non-covalent interaction of full-methylated cyclodextrin and porphyrin and the amphiphilic action of molecules, and the particle size of the nano particles is 30-40nm. The supermolecular assembly has the advantages that the supermolecular assembly is simple in synthesis route, low in production cost, relatively high in yield and applicable to amplified synthesis and practical production and application; due to endocytosis which takes an overexpressed hyaluronic acid receptor on the surface of a malignant cell as a medium, the supermolecular assembly (HATXP) is introduced into cancer cells in a targeted manner, protection on normal cells and targeted selective killing of cancer cells are achieved, the anticancer activity is remarkable, and the toxic and side effects are remarkably reduced.

Description

technical field [0001] The invention relates to the technical field of targeted delivery of anticancer drugs, in particular to a supramolecular assembly and a preparation method for targeted delivery of paclitaxel prodrugs. Background technique [0002] Today, cancer has become the second major disease threatening human health, second only to cardiovascular and cerebrovascular diseases. The high mortality rate of cancer, the high recurrence rate after treatment, and the pain caused to patients make cancer known as "terminally ill". In order to fight against this disease, human beings have invented various treatment methods, mainly including surgery, radiotherapy and chemotherapy, among which paclitaxel (Taxol) is a broad-spectrum anti-cancer chemotherapy drug widely used in clinical practice, especially for breast cancer and ovarian cancer have good curative effect. In addition, paclitaxel can also act synergistically with a variety of anticancer drugs without cross-resis...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/36A61K9/51A61K31/337A61P35/00
Inventor 刘育杨洋张瀛溟
Owner NANKAI UNIV
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