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A kind of ph responsive polymer mixed micelle and its application

A technology of mixing micelles and polymers, which is applied in the direction of drug combinations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as sudden release, failure to achieve performance, and thinning of the micellar shell , to achieve the effect of simple synthesis process route

Inactive Publication Date: 2017-11-14
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, many materials used as drug carriers in the past were single polymers, and single polymers have their own disadvantages as drug carriers: in order to achieve the purpose of combining with drugs, there must be enough hydrophobic blocks so that hydrophilic blocks The decrease of the segment ratio, along with the decrease of the hydrophilic block ratio, will inevitably lead to the thinning of the micelle shell or even the phenomenon that the hydrophilic block is not enough to embed the surface of the micelle. Low and disintegration of micelles, etc.; in addition, a single polymer as a carrier also has the function of pH response, so that once the carrier starts to respond to pH, the pH response block of the carrier can no longer embed the drug. There must be some sudden release phenomenon
[0006] At present, judging from the existing research reports, the polymer mixed micelle drug-loading system applied to the injection drug delivery system of hydrophobic drugs is far from achieving satisfactory performance. How to maintain a high drug-loading capacity? Relieve or eliminate the phenomenon of burst release; how to improve the pH targeting ability and therapeutic efficiency of drug carriers are the two main problems currently facing

Method used

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  • A kind of ph responsive polymer mixed micelle and its application
  • A kind of ph responsive polymer mixed micelle and its application
  • A kind of ph responsive polymer mixed micelle and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] Synthesis of brominated polyethylene glycol (MPEG-Br): Weigh MPEG (5g, Mn=5000) and add the solvent into a dry 100ml anhydrous and oxygen-free reaction bottle, seal it with a reverse rubber stopper, and vacuumize - After blowing nitrogen gas for 3 times, under the protection of nitrogen gas, add the dehydrated solvent dichloromethane (30ml) and dehydrated triethylamine (TEA, 0.5ml) sequentially with a syringe, and then cool to 0°C in an ice bath, Slowly add 2,4-dibromoisobutyryl bromide (NA, 0.5ml) dropwise under stirring conditions, react at 0°C for 2h after the dropwise addition, then raise the temperature to 40°C, continue the reaction for 12h, after the reaction Wash with dilute hydrochloric acid and pure water three times respectively, drop the organic phase into 0°C n-hexane of ten times its volume to precipitate, filter, and finally vacuum-dry at 40°C for 48 hours.

Embodiment 2

[0078] Synthetic MPEG-b-PDEAEMA 20 :

[0079] The pH responsive monomer DEAEMA (1.43g), MPEG-Br (2g), catalyst CuBr 2 (2.78mg) and solvent were added to a 150ml anhydrous and oxygen-free reaction bottle, sealed with a reverse rubber stopper, vacuumed-nitrogen three times, under the protection of nitrogen, added THF (35ml) to remove water with a syringe in turn, and prepared Body PMDETA (33.64mg) and reducing agent Sn(Oct) 2 (78.6 mg), after freezing in liquid nitrogen, vacuumize and blow nitrogen three times, stir for 15 minutes after thawing, then start to heat up, and react in an oil bath at 65°C for 24 hours. After most of THF was removed by rotary evaporation under reduced pressure, the organic phase was slowly added dropwise to 200ml of cold n-hexane to precipitate, filtered, and finally vacuum-dried at 45°C for 48h, Mn=9075.8, PDI=1.047.

Embodiment 3

[0081] Synthetic MPEG-b-PDEAEMA 35 :

[0082] The pH responsive monomer DEAEMA (2.5185g), MPEG-Br (2g), catalyst CuBr 2 (10.5mg) and solvent were added to a 150ml anhydrous and oxygen-free reaction bottle, sealed with a reverse rubber stopper, vacuumed-nitrogen three times, under the protection of nitrogen, add dehydrated toluene (30ml) with a syringe in turn, and prepare Body PMDETA (42.34mg) and reducing agent Sn(Oct) 2(89.6 mg), after freezing in liquid nitrogen, vacuumize and blow nitrogen three times, stir for 15 minutes after thawing, then start to heat up, and react in an oil bath at 80°C for 12 hours. After most of the toluene was removed by rotary evaporation under reduced pressure, the organic phase was slowly added dropwise to 200ml of cold n-hexane to precipitate, filtered, and finally vacuum-dried at 45°C for 48h, Mn=11098, PDI=1.054.

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Abstract

The invention relates to a pH-responsive polymer mixed micelle and an application thereof, belonging to the technical field of pharmaceutical functional carrier materials. Mixed micelles are prepared by mixing two polymers MPEG‑b‑PDEAEMA and MPEG‑b‑PCL with hydrophobic anticancer drugs in a certain proportion, wherein MPEG‑b‑PDEAEMA is obtained by mixing hydrophilic block monomethyl polyethylene Diol MPEG bromination, and then use ATRP method to introduce N,N-diethylaminoethyl methacrylate into the polymer as a pH responsive block, which has pH responsiveness; another polymer MPEG-b ‑PCL is obtained by ring-opening polymerization of ε‑caprolactone as a hydrophobic block directly initiated by the hydrophilic block MPEG, and has amphiphilicity. The hybrid polymer micelle has amphiphilicity and pH responsiveness at the same time, and the drug loading capacity of hydrophobic anticancer drugs can be as high as 26.79%. It has a good pH-controlled release effect and can make the drug stable for a long time at neutral pH Existence, space velocity release drug at acidic pH. In addition, the synthetic routes and preparation processes of the two polymers are very brief.

Description

technical field [0001] The invention relates to a pH-responsive polymer mixed micelle and its application, in particular to a block polymer mixed micelle carrier material with targeted slow-controlled release of drugs, its preparation method and example application, belonging to the functional carrier of drugs field of materials technology. Background technique [0002] Nano-drug delivery system is a research hotspot in recent years. Nano-drug carrier refers to a new type of carrier with a particle size of 10-300nm. It is generally made of natural or synthetic polymer materials and can pass through the skin, Subcutaneous, intramuscular injection, intravenous injection, arterial injection, and body cavity mucosal adsorption and oral administration can deliver drugs to the lesion and release the drug to achieve therapeutic purposes, so it has broad application prospects. Commonly used nano drug carriers include nanoparticles, liposomes, hydrogels, micelles and so on. However...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/34A61K47/32A61K45/00A61P35/00C08F293/00C08F220/34C08G63/664
Inventor 杨楚芬陈劲锐郭建维崔亦华彭进平魏关铎
Owner GUANGDONG UNIV OF TECH
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