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A supramolecular assembly and preparation method for targeted delivery of paclitaxel anticancer prodrug

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

Inactive Publication Date: 2016-07-20
NANKAI UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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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 then administered intravenously. It has significant myelosuppression, cardiovascular and liver Toxicity and neurotoxicity have a great impact on the patient's physical condition and quality of life

Method used

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  • A supramolecular assembly and preparation method for targeted delivery of paclitaxel anticancer prodrug
  • A supramolecular assembly and preparation method for targeted delivery of paclitaxel anticancer prodrug
  • A supramolecular assembly and preparation method for targeted delivery of paclitaxel anticancer prodrug

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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 the strong non-covalent interaction between fully methylated cyclodextrin and porphyrin and the 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 a core, and the particle size of the nanoparticle is 30-40nm.

[0030] The preparation method of the s...

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Abstract

A supramolecular assembly for targeted delivery of paclitaxel prodrug, which is a binary supramolecular assembly synthesized based on fully methylated cyclodextrin modified hyaluronic acid and porphyrin modified paclitaxel prodrug, the binary supramolecular assembly Based on the strong non-covalent interaction between fully methylated cyclodextrin and porphyrin and the amphiphilic interaction between molecules, a superstructure with hydrophilic hyaluronic acid as the shell and hydrophobic porphyrin-modified paclitaxel prodrug as the core is formed. Molecular nanoparticles with a particle size of 30‑40 nm. The advantages of the present invention are: the supramolecular assembly has simple synthetic route, low production cost and high yield, and is suitable for scale-up synthesis and practical production application; Endocytosis brings the supramolecular assembly HATXP into cancer cells in a targeted manner, realizing the protection of normal cells and the targeted selective killing of cancer cells, with significant anticancer activity and significantly reduced toxic and side effects.

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-resist...

Claims

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Application Information

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