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Hydrogel eye drug carrier containing polymer micelles and preparation method thereof

A polymer glue and polymer technology, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and non-active components of polymer compounds, etc., can solve the problems of difficult to release drugs at a fixed point, lack of fixed shapes, etc., and achieve large Social and economic benefits, the effect of good oxygen permeability

Active Publication Date: 2017-07-21
普润德百目通(北京)科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, polymer micelles usually exist in the form of solutions, lacking a fixed shape, and it is difficult to achieve targeted release of drugs

Method used

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  • Hydrogel eye drug carrier containing polymer micelles and preparation method thereof
  • Hydrogel eye drug carrier containing polymer micelles and preparation method thereof
  • Hydrogel eye drug carrier containing polymer micelles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Dissolve 57.6mg of β-CD in 10 ml of ultrapure water, then add 10ml of 0.72% W / V PAA (number average molecular weight 100000, the same below) aqueous solution and 10ml 0.44% W / V PEG (number average molecular weight of 6000, below Same) aqueous solution. The resulting mixture was stirred at room temperature for 24 hours, then allowed to stand overnight. The solution containing the polymer micelles was dialyzed for 3 days with a dialysis bag with a molecular weight cut-off of 3000, and the water was changed every 4 hours to remove free β-CD in the mixed solution to obtain a polymer micelles solution. The light transmission of polymer micelles is greater than 90%, such as figure 1 M-0.1-50. The particle size is 64nm, the ζ potential is -20.1±0.8, the loading capacity of ofloxacin in the polymer micelle is 3.26 μg / ml, and the loading capacity of puerarin in the polymer micelle is 6.17 μg / ml. HEMA monomer (with a volume ratio of 2:1 to water in the total system) and 2wt% M...

Embodiment 2

[0065] Dissolve 5.8 mg of β-CD in 10 ml of ultrapure water, then add 10 ml of 0.072% W / V PAA aqueous solution and 10 ml of 0.044% W / V PEG aqueous solution. The resulting mixture was stirred at room temperature for 24 hours, then allowed to stand overnight. The solution containing the polymer micelles was dialyzed for 3 days with a dialysis bag with a molecular weight cut-off of 3000, and the water was changed every 4 hours to remove free β-CD in the mixed solution to obtain a polymer micelles solution. The light transmission of polymer micelles is greater than 95%, such as figure 1 M-0.01-50. The particle size is 39nm, the zeta potential is -29.7±0.9, and the loading capacity of puerarin in the polymer micelle is 1.15μg / ml. HEMA monomer (volume ratio of water in the total system is 2:1) and 2% MPC monomer (0.5% of the total mass of micelles liquid and monomer) were mixed, and then 35% aqueous solution of polymer micelles was added (by mixing After the total mass of the mono...

Embodiment 3

[0067] 28.8 mg of β-CD was dissolved in 10 ml of ultrapure water, and then 10 ml of 0.36% W / V PAA aqueous solution and 10 ml of 0.22% W / V PEG aqueous solution were added. The resulting mixture was stirred at room temperature for 24 hours, then allowed to stand overnight. The solution containing the polymer micelles was dialyzed for 3 days with a dialysis bag with a molecular weight cut-off of 3000, and the water was changed every 4 hours to remove free β-CD in the mixed solution to obtain a polymer micelles solution. The light transmission of polymer micelles is greater than 95%, such as figure 1M-0.05-50. The particle size is 53nm, the ζ potential is -23.3±0.9, the loading capacity of ofloxacin in the polymer micelle is 1.94 μg / ml, and the loading capacity of puerarin in the polymer micelle is 3.85 μg / ml. HEMA monomer (volume ratio of water in the total system is 2:1) and 2% MPC monomer (0.5% of the total mass of micelles liquid and monomer) were mixed, and then 35% aqueous...

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Abstract

The invention discloses a hydrogel ophthalmic carrier containing polymer micelles and a preparation method thereof. The carrier is composed of polymer micelles liquid composed of polyethylene glycol, polyacrylic acid and cyclodextrin and monomeric methacrylic acid Hydroxyethyl ester and phosphorylcholine are mixed and polymerized. Its preparation method includes mixing and stirring cyclodextrin aqueous solution, polyethylene glycol aqueous solution and polyacrylic acid aqueous solution, then standing still, and then obtaining polymer micelle liquid by dialysis, combining monomer hydroxyethyl methacrylate and phosphorylcholine with polymer After the micellar liquid is mixed, it is polymerized and demoulded, and the product is obtained. The novel hydrogel provided by the invention has good oxygen permeability and drug controlled release capability, its performance meets the requirements of corneal contact lenses, it can control the release of ophthalmic drugs, and it has great social and economic benefits.

Description

technical field [0001] The invention belongs to the technical field of new materials, and specifically relates to the preparation of polymer micelles, the synthesis of composite hydrogels, and the loading and release of drugs in the hydrogels. Background technique [0002] The treatment of eye diseases is mainly done by drugs at present. In this process, too low drug concentration cannot play a therapeutic role; too high drug concentration will cause side effects and even damage normal tissues and organs. In addition, the therapeutic effect also depends on whether the drug can remain in the affected area for a sufficient time. Among the currently used ophthalmic preparations, more than 90% are eye drops or eye ointments, which stay in the eyes for only about 2 minutes, and only 1-7% of the drugs can be effectively used. Most of the drugs are discharged through the nasolacrimal duct or passed through The nasal cavity enters the blood system, causing disadvantages such as in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/40A61K47/10A61K47/32A61K47/24A61P27/02
Inventor 胡小红王昕陈频张新燕马小涵董岩
Owner 普润德百目通(北京)科技有限公司
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