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Super-molecular hydrogel double-medicament carrier and preparation method as well as application thereof

A supramolecular hydrogel and hydrophobic drug technology, applied in the field of biomedical engineering materials, to achieve good shear thinning, lower concentration and temperature requirements, and improve bioavailability

Inactive Publication Date: 2011-11-23
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, the preparation and application of supramolecular hydrogel dual drug carriers loaded with both hydrophilic and hydrophobic drugs through the host-guest interaction of polymers and cyclodextrins has not been reported.

Method used

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  • Super-molecular hydrogel double-medicament carrier and preparation method as well as application thereof
  • Super-molecular hydrogel double-medicament carrier and preparation method as well as application thereof
  • Super-molecular hydrogel double-medicament carrier and preparation method as well as application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0035] Dry polyethylene glycol monomethyl ether (MPEG, molecular weight 2000) and indomethacin (IND) were dissolved in anhydrous dimethyl sulfoxide under stirring conditions of 300 rpm to obtain a solution ( 100 ml of dimethyl sulfoxide contains 10 g of polyethylene glycol monomethyl ether); add 1,3-dicyclohexylcarbodiimide (DCC) and 4-dimethylaminopyridine (DMAP) to the solution, 5 Stirring reaction at ℃ for 48 hours; the molar ratio of polyethylene glycol monomethyl ether, hydrophobic drug, 1,3-dicyclohexylcarbodiimide and 4-dimethylaminopyridine is 1:1.1:1.2:1.1 After the reaction is completed, the product is filtered, and the filtrate is precipitated with ether; the resulting precipitate is redissolved in water, filtered and dialyzed for 2 days using a dialysis bag with a molecular weight cut-off of 3000, and freeze-dried to obtain prodrug A (MPEG-IND).

Embodiment 2

[0037]Dry polyethylene glycol monomethyl ether (MPEG, molecular weight 10000) and indomethacin (IND) were dissolved in anhydrous dimethyl sulfoxide under stirring conditions of 900 rpm to obtain a solution ( 20 g of polyethylene glycol monomethyl ether per 100 ml of dimethyl sulfoxide); 1,3-dicyclohexylcarbodiimide (DCC) and 4-dimethylaminopyridine (DMAP) were added to the solution, 35 Stirring reaction at ℃ for 24 hours; the molar ratio of polyethylene glycol monomethyl ether, hydrophobic drug, 1,3-dicyclohexylcarbodiimide and 4-dimethylaminopyridine is 1:1.1:1.2:1.1 After the reaction is completed, the product is filtered, and the filtrate is precipitated with ether; the resulting precipitate is redissolved in water, filtered and dialyzed for 3 days using a dialysis bag with a molecular weight cut-off of 500, and freeze-dried to obtain the prodrug (MPEG-IND).

Embodiment 3

[0039] Under the condition of room temperature 25 DEG C, the obtained MPEG-IND of embodiment 1 is dissolved in the phosphate buffer solution that pH is 6 and is made into the prodrug solution that the mass percent concentration is 8%, and the folic acid solution that the mass percent concentration is 1.0% ( Folic acid is dissolved in the sodium bicarbonate solution of 0.1mol / L and obtains) mixes in equal volumes, then adds the α-cyclodextrin solution (α-cyclodextrin Dissolved in a phosphate buffer solution with a pH of 6), stirred at a speed of 60 rpm for 60 seconds, mixed evenly, and stood at 5°C for 12 hours to obtain a supramolecular hydrogel loaded with both hydrophilic and hydrophobic drugs Gum Dual Drug Carrier B.

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Abstract

The invention discloses a super-molecular hydrogel double-medicament carrier for simultaneously loading hydrophilic and hydrophobic medicaments and a preparation method as well as application thereof. The method comprises the following operating steps of: performing chemical modification on the hydrophobic medicament by using methoxypolyethylene glycol to synthesize a water-soluble macromolecularprodrug; physically mixing prodrug molecules with the hydrophilic medicament; further mixing the mixed solution with an alpha-cyclodextrin solution and stirring; and standing at room temperature to obtain the super-molecular hydrogel double-medicament carrier for simultaneously loading the hydrophilic and the hydrophobic medicaments. The carrier has the advantages of easiness in operation, adjustable gel strength and gelation time, forming at room temperature, no chemical crosslinking reaction or organic solvent, high bioavailability, sustainable and controllable release of the medicament andthe like, and is expected to be widely applied to the field of biomedical engineering materials.

Description

technical field [0001] The invention belongs to the field of biomedical engineering materials, in particular to a supramolecular hydrogel dual drug carrier capable of simultaneously loading hydrophilic and hydrophobic drugs, and a preparation method and application thereof. Background technique [0002] Combination therapy of two or more drugs is currently an effective method for clinically treating diseases and tissue defects. The key to the implementation of this technology is to control the dosage and cycle of each drug. As a commonly used class of drug carriers, hydrogels have the advantages of high loading capacity, protection of drugs from biodegradation and clearance, and sustainable release of drugs, and have been studied as dual drug carriers in recent years. For example, Konishi et al. loaded cisplatin and doxorubicin in glutaraldehyde-crosslinked gelatin matrix at the same time, and achieved the purpose of efficiently inhibiting tumor cells through the synergisti...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K45/06
Inventor 马栋张黎明
Owner SUN YAT SEN UNIV
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