Folate-modified chondroitin sulfate-deoxycholic acid polymer and its synthesis method and application

A technology of chondroitin sulfate and deoxycholic acid, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, drug combinations, etc., to achieve low toxicity and side effects, excellent biocompatibility, and round shape Effect

Active Publication Date: 2018-08-28
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Folate-modified chondroitin sulfate-deoxycholic acid polymer and its synthesis method and application
  • Folate-modified chondroitin sulfate-deoxycholic acid polymer and its synthesis method and application
  • Folate-modified chondroitin sulfate-deoxycholic acid polymer and its synthesis method and application

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Embodiment 1

[0052] Embodiment 1: the synthesis of chondroitin sulfate-deoxycholic acid polymer

[0053] (1) Synthesis of chondroitin sulfate-adipate dihydrazide: Weigh 0.5g chondroitin sulfate and dissolve it in 150mL distilled water, stir to make it fully swell and dissolve, then add 5.0g adipic acid dihydrazide to the solution in turn Hydrazide, 1.6g 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 0.23g N-hydroxysuccinimide, adjust the pH value of the reaction system to 6.8 with sodium hydroxide , reacted at room temperature for 24 hours, dialyzed with distilled water for three days, and freeze-dried to obtain the intermediate product chondroitin sulfate-adipate dihydrazide.

[0054] (2) Weigh 80 mg of deoxycholic acid and dissolve it in 5 mL of N,N-dimethylformamide, and sequentially add 1-(3-dimethylaminopropyl)-3- Ethylcarbodiimide hydrochloride, N-hydroxysuccinimide equivalent to 2 times the molar amount of deoxycholic acid, stirred at room temperature for 30 minute...

Embodiment 2

[0057] Embodiment 2: Synthesis of folic acid-modified chondroitin sulfate-deoxycholic acid polymer

[0058] (1) Synthesis of chondroitin sulfate-adipate dihydrazide: Weigh 0.5g chondroitin sulfate and dissolve it in 150mL distilled water, stir to make it fully swell and dissolve, then add 5.0g adipic acid dihydrazide to the solution in turn Hydrazide, 1.6g 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 0.23g N-hydroxysuccinimide, adjust the pH value of the reaction system to 6.8 with sodium hydroxide , reacted at room temperature for 24 hours, dialyzed with distilled water for three days, and freeze-dried to obtain the intermediate product chondroitin sulfate-adipate dihydrazide.

[0059] (2) Weigh 80 mg of deoxycholic acid and dissolve it in 5 mL of N,N-dimethylformamide, and sequentially add 1-(3-dimethylaminopropyl)-3- Ethylcarbodiimide hydrochloride, N-hydroxysuccinimide equivalent to 2 times the molar amount of deoxycholic acid, stirred at room temperatu...

Embodiment 3

[0064] Example 3: Preparation of folic acid-modified chondroitin sulfate-deoxycholic acid polymer nanomicelles loaded with docetaxel

[0065] 50 mg of folic acid-modified chondroitin sulfate-deoxycholic acid (prepared in Example 2) was ultrasonically dispersed in 10 mL of deionized water for later use; another 15 mg of docetaxel was dissolved in 2 mL of methanol, and slowly added dropwise under strong stirring Add the above-mentioned folic acid-modified chondroitin sulfate-deoxycholic acid polymer aqueous solution, continue to stir vigorously at room temperature overnight (8-12), then use probe-type ultrasonic treatment at 120W power three times, each time for 2min, pulse on for 2s and stop. For 4s, the temperature was kept at 4°C to 8°C, then the solution was transferred to a dialysis bag and dialyzed against water for 24 hours, and then the resulting solution was centrifuged at 4000r / min for 20min to remove unencapsulated drugs. The supernatant is then passed through a 0.8 μ...

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Abstract

The invention discloses a folate-modified chondroitin sulfate-deoxycholic acid polymer as well as a synthesis method and application thereof. With chondroitin sulfate as a water-soluble skeleton material, a water-soluble skeleton is subjected to hydrophobic transformation with deoxycholic acid and folic acid through adipic dihydrazide as a connecting arm, so as to prepare a folate-mediated nano-carrier material with folate receptor and CD44(+) receptor tumor cell dual-targeting ability. The folate-modified chondroitin sulfate-deoxycholic acid polymer disclosed by the invention has good biocompatibility, non-immunogenicity and biodegradability. The prepared tumor dual-targeting drug-loaded nano-micelle is round in appearance, good in stability, high in encapsulation efficiency and high in drug loading capacity, and has excellent slow-release property and good application prospect; the target concentration of the drug can be enhanced; the tumor-killing treatment effect is enhanced; the non-specific toxic or side effect is reduced.

Description

technical field [0001] The invention relates to a nanopolymer self-assembled micelle material and its application, in particular to a folic acid-modified chondroitin sulfate-deoxycholic acid polymer and its synthesis method and application, belonging to the fields of biomedical materials and nanomedicine preparations. Background technique [0002] In recent years, the incidence and mortality of tumors have shown an obvious upward trend, and it has become a disease that seriously threatens human health, with the characteristics of high mortality and poor prognosis. At present, chemotherapy is still one of the main methods of tumor treatment. The commonly used chemotherapeutic drugs in clinical practice are mainly cytotoxic drugs. Strong cytotoxicity, and then cause serious toxic side effects. Therefore, the development of suitable preparations to improve the solubility of poorly soluble chemotherapeutic drugs and increase their targeted therapy to reduce the potential risks ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K47/22A61K47/36A61K47/34A61K31/337A61K31/12A61P35/00C08B37/08
CPCA61K9/1075A61K9/19A61K31/12A61K31/337A61K47/22A61K47/34A61K47/36C08B37/0069A61K2300/00
Inventor 翟光喜刘梦锐
Owner SHANDONG UNIV
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