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Hyaluronic acid prodrug as well as preparation method thereof and application thereof in transdermal delivery

The technology of hyaluronic acid and prodrug is applied in the field of hyaluronic acid prodrug and its preparation, and can solve the problems such as the need to improve the biocompatibility of the carrier, the existence of skin irritation and allergy, the damage to the normal barrier function of the skin, and the like, To achieve the effect of improving percutaneous penetration, facilitating treatment and improving targeting

Active Publication Date: 2018-10-16
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at present, transdermal drug delivery still has disadvantages such as low penetration rate, impaired normal skin barrier function, skin irritation and allergy, carrier biocompatibility needs to be improved, and low drug utilization rate.

Method used

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  • Hyaluronic acid prodrug as well as preparation method thereof and application thereof in transdermal delivery
  • Hyaluronic acid prodrug as well as preparation method thereof and application thereof in transdermal delivery
  • Hyaluronic acid prodrug as well as preparation method thereof and application thereof in transdermal delivery

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1: Preparation of hyaluronic acid grafted 5-aminolevulinic acid

[0038] (1) Weigh the corresponding raw materials: hyaluronic acid, drug molecule, N-hydroxysuccinimide, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, water residue quantity;

[0039] The mass ratio of described hyaluronic acid and drug molecule is 10:1, and hyaluronic acid, N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide salt The mass ratio of acid salt is: 4:2:1;

[0040] (2) Dissolve hyaluronic acid in water, then add N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, and place on a magnetic stirrer on, stirring at a speed of 200r / min for 1h;

[0041] (3) Dissolve the drug molecule in water, then add it into (2), and stir overnight; put the obtained sample into a dialysis bag (molecular weight cut-off is 500), and then immerse the dialysis bag in pure water and stir for 3 days , freeze-dried to obtain hyaluronic acid...

Embodiment 2

[0043] Embodiment 2: Preparation of hyaluronic acid grafted 5-aminolevulinic acid

[0044] (1) Weigh the corresponding raw materials: hyaluronic acid, drug molecule, N-hydroxysuccinimide, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, water residue quantity.

[0045] The mass ratio of hyaluronic acid to drug molecules is 5:1, hyaluronic acid, N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide salt The mass ratio of acid salt is: 4:2:1;

[0046] (2) Dissolve hyaluronic acid in water, then add N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, and place on a magnetic stirrer on, stirring at a speed of 200r / min for 1h;

[0047] (3) Dissolve the drug molecule in water, then add it into (2), and stir overnight; put the obtained sample into a dialysis bag (molecular weight cut-off is 500), and then immerse the dialysis bag in pure water and stir for 3 days , freeze-dried to obtain hyaluronic acid grafted with 5-a...

Embodiment 3

[0049] Embodiment 3: Preparation of hyaluronic acid grafted 5-aminolevulinic acid

[0050] (1) Weigh the corresponding raw materials: hyaluronic acid, drug molecule, N-hydroxysuccinimide, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, water residue quantity.

[0051] The mass ratio of the hyaluronic acid to the drug molecule is 2:1, and the hyaluronic acid, N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide salt The mass ratio of acid salt is: 4:2:1;

[0052] (2) Dissolve hyaluronic acid in water, then add N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, and place on a magnetic stirrer on, stirring at a speed of 200r / min for 1h;

[0053] (3) Dissolve the drug molecule in water, then add it into (2), and stir overnight; put the obtained sample into a dialysis bag (molecular weight cut-off is 500), and then immerse the dialysis bag in pure water and stir for 3 days , freeze-dried to obtain hyaluronic acid...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and discloses a hyaluronic acid prodrug as well as a preparation method thereof and application thereof in transdermal delivery. According to the preparation method, hyaluronic acid is used for grafting drug molecules so as to overcome the barrier function of stratum corneum, and the drug molecules are transmitted to the subcutaneous tissues by means of intercellular space penetration and an opening of cutaneous appendages, so that drug molecular targeting and skin absorption efficiency are improved. As a carrier for administration, hyaluronic acid can effectively improve the percutaneous permeability of a drug, and helps the drug to be absorbed into the systemic circulation, thereby enabling an effective blood concentration of local or systemic treatment to be reached. Compared with the prior art, the hyaluronic acid prodrug enables the skin penetration amount of the drug molecules to be obviously increased so as to increase the utilization rate of the drug; furthermore, the hyaluronic acid prodrug facilitates the treatment of a doctor for a patient, can realize direct administration for certain diseases, and effectively reduces risks and side effects, thus having a broad application prospect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a hyaluronic acid prodrug, its preparation method and its application in transdermal administration. Background technique [0002] Transdermal drug delivery system refers to the application of drugs on the surface of the skin, so that it is continuously delivered to the subcutaneous tissue through the skin and enters the blood circulation, so as to achieve an effective therapeutic concentration. As a new type of drug delivery system, the transdermal drug delivery system has many advantages: reduce the pain caused by injection and avoid the odor of oral drugs, improve patient compliance; release drugs at a constant rate; Overcome the adverse reactions caused by excessive blood concentration due to excessive absorption; avoid the first-pass effect of the liver and prevent the degradation of drugs in the stomach; reduce individual differences in medication; easy to use, su...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/61A61K31/197
CPCA61K9/0014A61K31/197A61K47/61
Inventor 马栋谢婕思胡云峰薛巍
Owner JINAN UNIVERSITY
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