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A kind of vinca alkaloid drug carrier and preparation method thereof

A vinca alkaloid and carrier technology, which can be used in drug combinations, pharmaceutical formulations, antitumor drugs, etc., can solve problems such as unsatisfactory drug loading and unstable drug encapsulation efficiency.

Inactive Publication Date: 2016-03-02
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although liposomes, polymer nanoparticles and nanomicelles have been reported, the instability of liposomes and nanomicelles and the unsatisfactory encapsulation efficiency and drug loading of polymer nanoparticles to drugs are still unsatisfactory. can be effectively resolved

Method used

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  • A kind of vinca alkaloid drug carrier and preparation method thereof
  • A kind of vinca alkaloid drug carrier and preparation method thereof
  • A kind of vinca alkaloid drug carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0022] Example 1 (preparation of vinca alkaloid drug carrier):

[0023] 1. Preparation of functional monomer N-acryloyl-L-tryptophan

[0024] Weigh 4.90g (0.024mol) of L-tryptophan (L-Trp) and 1.92g (0.048mol) of sodium hydroxide, dissolve in 40mL of water, and when the mixed solution becomes clear and transparent, place it on ice below 0°C in a salt bath. Under magnetic stirring, 2.00 mL (0.025 mol) of acryloyl chloride was added dropwise with a pipette. After the dropwise addition, it was stirred at room temperature for 24 h to make the reaction complete. Adjust the pH to 2 with concentrated hydrochloric acid to completely precipitate the reaction product. Suction filtration, washing with water to neutrality, and vacuum drying at 50°C for 24 hours yielded 3.25 g of white powdery solid, the functional monomer N-acryloyl-L-tryptophan (A-Trp), with a yield of 52.4%.

[0025] 2. Preparation of vinca alkaloid drug carrier

[0026] In a 50ml Erlenmeyer flask, add 1.8mmol func...

example 2

[0033] Example 2: (preparation of vinca alkaloid sustained-release medicine)

[0034] Weigh 5 mg of the vinca alkaloid drug carrier obtained in Preparation Example 1, place it in a 5 mL centrifuge tube, add 2 mL of vincristine solution with a concentration of 0.6 mmol / mL, place it in a shaker at room temperature and shake for 8 hours in the dark. Centrifuge at 10,000rmp for 15min with a high-speed centrifuge. Pipette the supernatant and measure the concentration of vincristine in it by ultraviolet spectroscopy, collect the precipitate, freeze-dry to obtain vincristine sulfate drug-loaded nanoparticles, and the drug loading and encapsulation efficiency are 8.55% and 65.99% respectively.

example 3

[0035] Example 3: (preparation of vinca alkaloid sustained-release medicine)

[0036] Weigh 5 mg of the vinca alkaloid drug carrier obtained in Preparation Example 1, put it into a 5 mL centrifuge tube, add 2 mL of vinblastine solution with a concentration of 0.6 mmol / mL, place it in a shaker at room temperature and shake for 8 hours in the dark. Centrifuge at 10,000rmp for 15min with a high-speed centrifuge. The supernatant was taken out and the concentration of vinblastine was determined by ultraviolet spectroscopy, and the precipitate was collected and freeze-dried to obtain vinblastine sulfate drug-loaded nanoparticles. The drug-loading capacity and encapsulation efficiency were 7.04% and 48.49%, respectively.

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Abstract

The invention relates to a catharanthus roseus alkaloidal drug carrier which is a copolymer of which the constitutional repeating unit is shown in the formula (1) in the description. The molar ratio of a functional monomer, namely N-acryloyl-L-tryptophan, to a crosslinking monomer, namely ethylene glycol dimethyl acrylate, is 67 / 33 in the copolymer, and the copolymer is prepared through water bath polymerization of the functional monomer and the crosslinking monomer. The drug carrier has the advantages that the biocompatibility is good, the drug loading capacity is large, and the drug is difficult to leak and release abruptly.

Description

technical field [0001] The present invention relates to a medical preparation, which is characterized by the organic polymer compound used. Background technique [0002] Vinblastine, vincristine, and vinorelbine are currently clinically used antineoplastic drugs. Due to the existence of therapeutic barriers, that is, the non-selective killing of normal cells and tumor cells, it often brings unacceptable side effects to patients, such as neurotoxicity, bone marrow suppression, leukopenia, anemia, etc., which limits its clinical application. use. In order to improve the clinical efficacy of vinca alkaloids and reduce their adverse reactions, new drug delivery systems such as liposomes, micelles, microemulsions, and microspheres have emerged in recent years. Although the emergence of new carriers has improved the clinical application of chemotherapy drugs to a certain extent, there are still problems such as easy leakage of drugs, short action time and biological safety of ca...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F220/60C08F222/14A61K47/48A61K47/34A61K31/475A61P35/00
Inventor 朱全红殷勇冠李敏婷朱泳妍
Owner SOUTHERN MEDICAL UNIVERSITY
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