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Uncharged amphiphilic chitosan nano drug carrier and preparation method and application thereof

A technology of chitosan nano and chitosan derivatives, which is applied in drug combination, antineoplastic drugs, powder delivery, etc. It can solve the problems of unfavorable controlled release, poor stability, difficult application, etc., and achieve slow drug release and easy operation , the effect of controllable output

Inactive Publication Date: 2012-01-11
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the patent (Chinese patent: CN1883708) is only limited to: grafting C8-C22 fatty acids on chitosan chains with a molecular weight of 1.5-51KDa
Low-molecular-weight chitosan degrades quickly, and the prepared drug carrier has a phenomenon of burst release of the drug, which is not conducive to the controlled release of the experimental drug for a long time
Since the fatty acid used in its patent is a flexible straight chain, the stability of the polymer micelles is poor after dilution. Therefore, in order to improve its stability, it is necessary to chemically modify the surface of the nanomicelles with bifunctional small molecules. Intermolecular chemical bond bridging on the surface of polymeric micelles to improve the stability of polymeric micelles
Moreover, existing studies have shown that since chitosan itself needs to be dissolved under acidic (pH<6.5) conditions, and the pH value of blood is neutral under human physiological conditions, only the lipophilicity of chitosan can be pulled. Amphiphilic drug carrier materials prepared by small molecules are difficult to be applied clinically due to precipitation under neutral conditions

Method used

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  • Uncharged amphiphilic chitosan nano drug carrier and preparation method and application thereof
  • Uncharged amphiphilic chitosan nano drug carrier and preparation method and application thereof
  • Uncharged amphiphilic chitosan nano drug carrier and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] 1) At room temperature, 4g chitosan (24KDa) was dissolved in 200mL hydrochloric acid aqueous solution, then the pH of the solution was adjusted to 5.6 with 1N NaOH to form a transparent 2% (w / v) chitosan solution.

[0033] 2) Get a certain amount of deoxybile acid, make the ratio of the amount of substance of deoxybile acid to the amount of substance of glucosamine residue in chitosan be 0.1: 1, join it in the DMSO solution of 100mL, then add deoxybile acid EDC and NHS were added into the solution in equal amounts, and the ratio of EDC to deoxybile acid was kept constant at 1.2:1. Deoxybile acid, EDC and NHS were reacted at room temperature at 1000rpm for 30min.

[0034] 3) A mixed solution of lithocholic acid, EDC and NHS reacted in 100 mL of DMSO for 30 min was slowly added dropwise to a 2% (w / v) chitosan solution within 30 min, and reacted for 24 h at a stirring speed of 1000 rpm.

[0035] 4) The above 300mL reaction mixture solution was added into 200mL methanol, a...

Embodiment 2

[0044] Except that the mol ratio of deoxyacid and glucosamine residue in chitosan is 0.2: 1, other conditions are the same as specific example 1.

[0045] The FTIR characterization spectrum of the synthetic product of the first step of grafting deoxybile acid under this condition is shown in figure 1 -c.

[0046] The FTIR characterization spectrum of the synthetic product of the second step grafted glyceryl trimethylammonium chloride under this condition is shown in figure 2 -c.

[0047] The particle size intensity distribution diagram and TEM morphology characterization diagram of the nanoparticles prepared under this condition are shown in image 3 (Z-average=201.0±3.0 nm, PDI=0.151).

[0048] The drug-loading capacity and drug-loading efficiency of the materials prepared under this condition were 17.3% and 88%, respectively.

[0049] The release curve of the drug-loaded nanoparticles prepared under the condition of pH=7.4 is shown in Figure 4 b.

Embodiment 3

[0051] Except that the molar ratio of deoxybile acid to glucosamine residue in chitosan is 0.3:1, other conditions are the same as in specific example 1.

[0052] The FTIR characterization spectrum of the synthetic product of the first step of grafting deoxybile acid under this condition is shown in figure 1 -d.

[0053] The drug-loading capacity and drug-loading efficiency of materials prepared under this condition to load PTX were 18.3% and 91.5%, respectively.

[0054] The release curves of the drug-loaded nanoparticles prepared under the conditions of pH=6.0 and pH=7.4 are shown in Figure 5 .

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Abstract

The invention relates to an uncharged amphiphilic chitosan nano drug carrier and a preparation method and application thereof. The preparation method is characterized in that lipophilic micromolecular deoxidized bile acid and hydrophilic micromolecular glycide are respectively grafted on chitosan molecules, thus obtaining a degradable amphiphilic chitosan material with good biocompatibility; in a wide pH solution, the amphiphilic chitosan material can quickly form a nano micelle which has a grain size of 150-300nm and is uniformly distributed through the principle of molecular self assembly under ultrasound conditions; and the inner lipophilic structure of the nano micelle is beneficial to improvement of the solubility of fat-soluble drugs in the aqueous solution, thus being expected to improve the in-vivo bioavailability of the drugs. The method has the advantages of simple requirements for instruments and equipment, simple and controllable preparation process and easy realization of large scale, so that the method is suitable for preparing nano carrier release systems of antitumor drugs with high price and poor water solubility and bioavailability such as paclitaxel, doxorubicin, camptothecin, vincaleucoblastine and the like. As a new dosage form of the antitumor drugs, the drug carrier has wide market prospects and potential clinical tumor treatment values.

Description

technical field [0001] The present invention relates to the preparation of lipophilic drug nano-carriers and the loading of drugs, specifically a method of preparing nano-particles with hydrophilic surface and internal lipophilicity through molecular self-assembly under ultrasonic conditions combined with dialysis and loading oily anti-tumor drugs inside Methods in the oleophilic core. Background technique [0002] Amphiphilic polymers composed of hydrophilic and lipophilic segments form nanomicelles in aqueous solution through the principle of molecular self-assembly. Because the surface of the micelles is hydrophilic and the interior is lipophilic, this type of micelles has many advantages in the field of drug delivery and controlled release, such as improving the solubility of lipophilic drugs in the solution and avoiding the effect of easily degraded drugs. Degradation occurs during the process of targeting, improving the bioavailability of drugs, prolonging the circula...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K9/14A61K31/337C08B37/08A61P35/00
Inventor 马小军周火飞刘袖洞
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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