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Preparation method and application of fatty acid-trimethyl chitosan polymer modified by lactobionic acid

A technology of trimethyl chitosan and fatty acid, which is applied in the direction of powder transportation, etc., can solve the problems of lowering the curative effect of drugs and restricting safe use, etc., and achieve good biocompatibility, reduce toxic and side effects, and improve the effect of curative effect

Inactive Publication Date: 2013-01-09
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Insufficient uptake of self-polymers in the tumor site reduces the drug efficacy of the administered dose, and non-specific side effects related to normal tissues limit the safe use of the maximum administered dose

Method used

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  • Preparation method and application of fatty acid-trimethyl chitosan polymer modified by lactobionic acid
  • Preparation method and application of fatty acid-trimethyl chitosan polymer modified by lactobionic acid
  • Preparation method and application of fatty acid-trimethyl chitosan polymer modified by lactobionic acid

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Experimental program
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Embodiment 1

[0032] (1) Combine 2.0g chitosan, 4.8gNaI, 11.5mlCH 3 I. Add 11ml 15% NaOH and 80ml NMP into the round bottom flask and mix well; place the mixture in a 60°C magnetic stirrer and heat and stir for 45 minutes in a water bath; take out the mixture, add excess ethanol to it, fully precipitate, centrifuge, and discard Supernatant: Wash the precipitate 2-3 times with ethanol and ether. After washing, discard the supernatant. Add 40ml of 0.16mol / L NaCl solution to the precipitate to dissolve it; add ethanol after dissolution to precipitate it and centrifuge The supernatant was discarded afterwards; the precipitate was washed with excess ethanol, filtered with suction, and the solid obtained was placed in a vacuum drying oven at 40°C for 12 hours. The obtained solid was characterized by infrared and nuclear magnetic properties. figure 1 with figure 2 B.

[0033] (2) In a 100mL round-bottom flask, add 0.128g palmitic acid (PA) (stearic acid can also be used), 50ml of dry dichloromethane,...

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Abstract

The invention discloses a fatty acid-trimethyl chitosan polymer modified by a lactobionic acid, a preparation method and an application. The fatty acid-trimethyl chitosan polymer modified by the lactobionic acid is an active targeting nano micelle carrier material. A trimethyl chitosan with a good water-solubility is used as a carrier material, the hydrophobic modification is performed by a fatty acid, and then the surface modification is performed by the lactobionic acid to obtain a polymer micelle with the lactobionic acid which mediates tumor tissue target. Harmine is used as a model drug to prepare a drug-loaded nano-micelle in a rubbing and self-assembly mode. A test confirms that the drug loading capacity and encapsulated ratio of the drug-loaded nano-micelle are high, the slow-release property is achieved, cells are effectively taken in through a lactobionic acid receptor pathway, and distribution of drugs on the tumor tissue is increased, so that the curative effect is improved, the toxic and side effect is reduced, and targeted therapy is achieved. The fatty acid-trimethyl chitosan polymer modified by the lactobionic acid, the preparation method and the application provide an ideal novel drug carrier and a preparation form for antitumor drugs with slightly solubility.

Description

Technical field [0001] The invention relates to a lactobionic acid-modified fatty acid-trimethylchitosan polymer, a preparation method, and application as a carrier in preparing an antitumor drug receptor targeting nanomicelle preparation, belonging to the field of pharmaceutical preparations. Background technique [0002] At present, the clinical treatment of liver cancer lacks specificity and the curative effect is not ideal. More than 90% of the drugs are taken up by the body's normal tissues, and only 2% to 5% of the drugs reach the tumor package. In fact, the anti-tumor chemotherapy drugs used clinically all have a certain degree of toxic and side effects, and some serious side effects are the direct reasons for limiting the dosage and use of drugs. The main reason for the occurrence of these toxic and side effects is that chemotherapy drugs lack specificity to tumor sites, and produce non-specific toxicity when administered in large doses, and even cause serious damage to ...

Claims

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Application Information

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IPC IPC(8): C08B37/08A61K9/14A61K47/36
Inventor 张学农贝永燕陈维良朱爱军
Owner SUZHOU UNIV
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