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KGM (Konjac Glucomannan)-g (grafted)-AH (Alicyclic Amine) drug loaded nano micelle and preparation method

A technology of konjac glucomannan and glucomannan, which can be used in pharmaceutical formulations, anti-tumor drugs, drug combinations, etc., can solve the problem of less pH-sensitive micelles, and achieve reduced toxic and side effects, good biocompatibility, and better biocompatibility. Biodegradability, the effect of improving drug efficacy

Inactive Publication Date: 2017-03-22
HUBEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few reports on pH-sensitive micelles containing C=N double bonds prepared from KGM

Method used

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  • KGM (Konjac Glucomannan)-g (grafted)-AH (Alicyclic Amine) drug loaded nano micelle and preparation method
  • KGM (Konjac Glucomannan)-g (grafted)-AH (Alicyclic Amine) drug loaded nano micelle and preparation method
  • KGM (Konjac Glucomannan)-g (grafted)-AH (Alicyclic Amine) drug loaded nano micelle and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1: Preparation of Dialdehyde Konjac Glucomannan (DAK)

[0034] Weigh 3.00 g of KGM, disperse in 500 mL of double-distilled water under mechanical stirring, and then swell at room temperature for 12 h to obtain a KGM dispersion; weigh 2.40 g of sodium periodate and dissolve in 100 mL of double-distilled water, drop Add it to the KGM dispersion, react for 24 h at room temperature in the dark, remove the reaction bottle, concentrate under reduced pressure at 55 °C to about 300 mL, transfer it to a dialysis bag with a molecular weight cut-off of 3500, After dialysis for 7 days, the dialysate was freeze-dried to obtain white dialdehyde konjac glucomannan (DAK).

[0035] Such as figure 1 As shown in the infrared spectrum b, at 3429 cm -1 There is a -OH stretching vibration peak at 2938 cm -1 There is a C-H stretching vibration peak at 1733 cm -1 There is a carbonyl stretching vibration peak at , indicating that C=O is produced after KGM is oxidized by sodium peri...

Embodiment 2

[0036] Embodiment 2: the preparation of octylamine grafted KGM (KGM- g -AH 8 )

[0037] Weigh 0.3 g of DAK in 30 mL of double-distilled water and dissolve at 50 °C for 10 min; weigh 0.19 mL of octylamine and dissolve it in 100 mL of ethanol, mix the ethanol solution of octylamine with DAK aqueous solution, and dissolve in the presence of ethanol Reflux at the boiling point for 8 h, remove the reaction bottle, remove ethanol under reduced pressure at 30 °C, wash with ethyl acetate or chloroform three times, take the organic phase, remove the organic reagent under reduced pressure at about 30 °C, and finally dissolve it with 2 mL of ethanol, Transfer to a dialysis bag, dialyze in double distilled water for 2 days, change the water every 4 h, take out the dialyzed fluid, and freeze-dry to obtain brown grafted konjac glucomannan KGM- g -AH 8 .

[0038] Such as figure 1 As shown in the infrared spectrum of c, at 3317 cm -1 There is a -OH stretching vibration peak at 2969 cm ...

Embodiment 3

[0040] Embodiment 3: the preparation of dodecylamine grafted KGM (KGM- g -AH 12 )

[0041] KGM-g-AH 12 Preparation process: Weigh 0.3 g of DAK in 30 mL of double distilled water and dissolve at 50 °C for 10 min; weigh 0.22 g of dodecylamine and dissolve it in 100 mL of ethanol, mix the ethanol solution of dodecylamine with the DAK aqueous solution , reflux at the boiling point of ethanol for 10 h, remove the reaction bottle, remove ethanol under reduced pressure at 30 °C, wash with ethyl acetate three times, take the organic phase, remove the organic reagent under reduced pressure at about 30 °C, and finally, use 2 mL of Dissolved in ethanol, transferred to a dialysis bag, dialyzed in double distilled water for 2 days, changed the water every 4 h, took out the dialyzed fluid, and freeze-dried to obtain brown grafted konjac glucomannan KGM- g -AH 12 .

[0042] Such as figure 1 As shown in the infrared spectrum of d, at 3356 cm -1 There is a -OH stretching vibration pea...

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Abstract

The invention relates to synthesis of a KGM (Konjac Glucomannan)-g(grafted)-AH (Alicyclic Amine) material and preparation of drug loaded nano micelle thereof, and belongs to the technical field of biological materials and slow release. The synthesis of the KGM-g-AH material comprises the following steps: firstly carrying out oxidization ring opening on KGM by using periodate, thus obtaining DAK (Dialdehyde KGM); then enabling the DAK to react with alicyclic amine, thus obtaining amphipathic KGM-g-AH. A grafted copolymer can be assembled to form nano micelle through an ethanol injection method; the nano micelle has pH (Potential of Hydrogen) sensitivity; in a neutral environment of normal tissues and blood, the nano micelle is relatively stable; in a weak acid environment of tumor tissues, imine bonds of molecules of the nano micelle are in reversible breakage, loaded drugs can be rapidly released, and the loaded drugs can be gathered in tumor cells, so that site-specific delivery of the drugs on the tumor tissues is realized. The prepared KGM-g-AH drug-loaded nano micelle is stable in structure, simple to synthesise, high in drug loading capacity, good in biocompatibility and low in cytotoxicity, has pH sensitivity and has a wide application prospect in the field of drug controlled release.

Description

technical field [0001] The invention relates to the synthesis of a fatty amine-grafted konjac glucomannan material with pH sensitivity and the preparation of drug-loaded nano micelles, belonging to the technical field of biological materials and sustained release. Background technique [0002] With the development of the economy and the destruction of the ecological environment, the incidence of cancer is also increasing, threatening people's health. Chemotherapy is currently the most widely used cancer treatment method, which is very fast and effective for killing and inhibiting cancer cells, and has the advantages of holistic and comprehensive treatment, but there are also many problems, such as poor water solubility of drugs, and Afterwards, it has poor selectivity in vivo, multi-drug resistance, short circulation time, and low bioavailability (Expert opinion on drug delivery, 2012, 9:687-700). To solve these problems, micro- and nanoscale drug delivery systems such as v...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/12A61K47/36A61P35/00C08B37/02
CPCA61K9/1075A61K31/12A61K47/36C08B37/009
Inventor 匡映栾金玲肖满严文莉姜发堂
Owner HUBEI UNIV OF TECH
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