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Preparation method of novel sulfhydrylated nanoparticles based on guar gum/cysteine conjugates

A cystine conjugate and nanoparticle technology, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, and drug combinations, etc. Continuous release and other issues, to achieve the effects of good water solubility and biodegradability, good application prospects, and a wide range of sources

Inactive Publication Date: 2016-07-13
GUANGZHOU CHUANGSAI BIOLOGICAL MEDICAL MATERIALS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Guar gum is a biodegradable biocompatible material. Guar gum molecules usually exist in a curly spherical structure, with mannose in the main chain, and a large number of hydroxyl groups are basically wrapped inside the molecule, and due to intramolecular hydrogen bonds effect, making its water solubility greatly reduced, unable to quickly swell and hydrate
Guar gum can form hydrogen bonds with mucosal proteins and has good bioadhesive properties, but this non-covalent bond-based adhesion cannot effectively overcome the clearance mechanism in the body and ensure the sustained release of drugs at designated sites

Method used

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  • Preparation method of novel sulfhydrylated nanoparticles based on guar gum/cysteine conjugates
  • Preparation method of novel sulfhydrylated nanoparticles based on guar gum/cysteine conjugates
  • Preparation method of novel sulfhydrylated nanoparticles based on guar gum/cysteine conjugates

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Effect test

Embodiment 1

[0025] Take guar gum as raw material (transparent guar gum, molecular weight 1.60~1.8 million), prepare the guar gum / cysteine ​​nanoparticles of mercaptolation, and its specific steps are as follows:

[0026] Step (a): Dissolve 0.5 g of guar gum in 100 mL of water, add 1 mL of 0.4 mol / L hydrochloric acid solution to dissolve, add 0.8 g of sodium periodate, stir at room temperature for 2 h, add 100 μL of ethylene glycol, and Stir for 1 hour, dialyze for 3 days, change the water 3 times a day, freeze-dry and store at 4°C;

[0027] Step (b): Mix 0.1g morpholineethanesulfonic acid and the formylated guar gum in 30mL of distilled water, add 0.25g of cysteine, adjust pH=5 with 0.4mol / L hydrochloric acid solution, and finally use Adjust to 50ml with distilled water, incubate at room temperature for 3h, add 2g of NaCNBH 3 , reacted at room temperature for 24 hours, and then dialyzed 6 times in a dark environment at 10°C, the first time was dialyzed with distilled water, the second ti...

Embodiment 2

[0031] Take guar gum as raw material (transparent guar gum, molecular weight 1.60~1.8 million), prepare the guar gum / cysteine ​​nanoparticles of mercaptolation, and its specific steps are as follows:

[0032] Step (a): Dissolve 1 g of guar gum in 140 mL of water, add 2 mL of 0.4 mol / L HCl to dissolve it, add 1.5 g of sodium periodate solution, stir at room temperature for 2 h, add 150 μL of ethylene glycol, and stir at room temperature 1h, dialysis for 3 days, change the water 3 times a day, freeze-dry and store at 4°C;

[0033] Step (b): Mix 0.2g morpholineethanesulfonic acid and formylated guar gum in 40mL of distilled water, add 0.5g of cysteine, adjust pH=5 with 0.4mol / L HCl, and finally adjust with distilled water for 50ml. Incubate at room temperature for 3h, add 2g of NaCNBH 3 , reacted at room temperature for 36 hours, and then dialyzed 6 times in a dark environment at 10°C, the first time was dialyzed with distilled water, the second time was dialyzed with 0.2mmol / L...

Embodiment 3

[0037] Take guar gum as raw material (transparent guar gum, molecular weight 1.60~1.8 million), prepare the guar gum / cysteine ​​nanoparticles of mercaptolation, and its specific steps are as follows:

[0038] Step (a): Dissolve 1.5g of guar gum in 140mL of water, add 0.5ml of 20% sulfuric acid solution by mass to dissolve it, add 2g of sodium periodate solution, stir at room temperature for 2h, add 200μL of ethylene glycol Alcohol, stirred at room temperature for 1 hour, dialyzed for 3 days, changed water 3 times a day, freeze-dried, and stored at 4°C;

[0039] Step (b): Mix 0.3g morpholineethanesulfonic acid and formylated guar gum in 40mL of distilled water evenly, add 0.5g of cysteine, adjust pH=5 with 0.4mol / L HCl, and finally adjust with distilled water for 50ml. Incubate at room temperature for 3h, add 4g of NaCNBH 3, reacted at room temperature for 48 hours. Then dialyze 6 times in a dark environment at 10°C, the first time with distilled water, the second time with ...

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Abstract

The invention relates to the field of biology, in particular to a preparation method of novel sulfhydrylated nanoparticles based on guar gum / cysteine conjugates.The novel sulfhydrylated nanoparticles based on the guar gum / cysteine conjugates are obtained through two-step modification, are about 800 nm in particle size and have excellent water solubility and biodegradability, and encapsulation efficiency is as high as 96.7 and drug loading capacity is as high as 8.79% when the novel sulfhydrylated nanoparticles are used for loading drugs.The novel sulfhydrylated nanoparticles are a long-acting medical product for protecting or treating lesions in gastrointestinal tracts, and are adhered to gastrointestinal tissues and can be kept for sufficient time on lesion sites and nearby parts to allow the lesions to be healed or treated when applied on the lesion sites and the nearby parts.

Description

technical field [0001] The invention relates to the technical field of biomedical materials, in particular, the invention discloses a preparation method of novel mercapto nanoparticles. Background technique [0002] Drug-loaded nanoparticles exhibit unique nano-effects in the mucosal drug delivery system, which can not only improve the targeting of drugs and change the kinetics of drugs, but also change the membrane transport mechanism by prolonging the residence time in the mucosa and increase drug delivery. The permeability of the membrane effectively overcomes biological barriers such as enzymes, and it is an excellent drug delivery route with great development prospects, especially as a drug delivery route for biomacromolecular drugs, which can effectively solve the problem of biomacromolecular drug loss in the body. Viability and short half-life issues. At present, the research on mucosal absorption of nanomedicine is limited to a small number of nanoparticle systems, ...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/36A61K47/18A61K31/122A61P1/00A61P1/04
CPCA61K9/19A61K31/122A61K47/183A61K47/36
Inventor 郭瑞刘玉秦作斌
Owner GUANGZHOU CHUANGSAI BIOLOGICAL MEDICAL MATERIALS CO LTD
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