Ph-responsive biodegradable polymer vesicles and its preparation method and application

A technology for degrading polymers and polymers, used in the fields of polymer chemistry and pharmaceutical biomedical engineering

Inactive Publication Date: 2015-10-21
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Doxorubicin hydrochloride (doxorubicin hydrochloride) is the first-line drug for the clinical treatment of cancer. It has good therapeutic effects on a variety of solid tumors, leukemia, lymphoma, breast cancer, etc., but it also has certain side effects. Such as hematopoietic inhibition, nausea, vomiting, hair loss, etc., but the most serious is its cardiotoxicity (Journal of Molecular and Cellular Cardiology, 2012, 52, 1213-1225). In recent years, studies have reported that doxorubicin is encapsulated in polymers Vesicles can effectively reduce its cardiotoxicity (Biomaterials, 2010, 31, 2882~2892)

Method used

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  • Ph-responsive biodegradable polymer vesicles and its preparation method and application
  • Ph-responsive biodegradable polymer vesicles and its preparation method and application
  • Ph-responsive biodegradable polymer vesicles and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1: Synthesis of pH-responsive triblock polymers

[0053] Synthetic route such as figure 1 As shown, the specific steps are as follows:

[0054] (1) Diblock copolymer mPEG 2000 -PCL 6000 Synthesis

[0055] Dissolve 20g of mPEG in 200ml of toluene, heat to boiling at 120°C, reflux for 10 hours, evaporate toluene, add 200ml of cold anhydrous ether to precipitate mPEG, filter, and store the dried mPEG in a vacuum oven.

[0056] 10gε-CL and 0.1gCaH 2 Put it in a 100ml round bottom flask, under magnetic stirring, reflux at 60°C to remove water for 12h, then distill ε-CL out under reduced pressure at 115°C; discard the remaining liquid in the flask.

[0057] 2gmPEG (molecular weight: 2000Da), 6gε-CL and 24μl catalyst stannous octoate were added to the reaction flask, nitrogen (N 2 ) replacement 3 times, reacted at 120°C for 12h, cooled to room temperature, added 100ml of cold diethyl ether to precipitate the product, filtered and dried under vacuum to obtain mPE...

Embodiment 2

[0068] Example 2: Study on Aggregation Behavior of pH Responsive Triblock Polymers

[0069] The prepared mass concentration is 0.1-6mg·ml -1 A series of polymer (polymer is prepared in Example 1) solution, using a surface tension meter, 25 ℃, the surface tension of the sample is measured by the hanging method, the results are as follows Figure 5 As shown, the results show that this polymer can make the surface tension of water from 70mN·m -1 reduced to 45mN·m -1 , and its critical aggregation concentration is about 4 mg·ml -1 .

Embodiment 3

[0070] Example 3: Preparation of pH-responsive triblock polymersomes by nanoprecipitation method

[0071] 20mg of polymer (prepared in Example 1) was dissolved in 0.2mlDMSO (heatable to dissolve), then under stirring, phosphate buffer solution of 1.8mlpH7.4 was added dropwise thereto, and the mixed solution was transferred to a dialysis bag (MWCO 3500 Da ), and finally dialyzed in 500ml phosphate buffer solution (pH7.4) to remove DMSO to obtain pH-responsive triblock polymersomes. Dialysis was carried out for 4 hours, the medium was changed every 0.5 hours for the first 2 hours, and every 1 hour for the next 2 hours.

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Abstract

The invention discloses a triblock copolymer with pH responsiveness, which is simple and convenient to synthesize. The polymer is an A-B-C segmented copolymer, wherein the block A is polyethylene glycol monomethyl ether (mPEG), and has the molecular weight of 2000 Da; the block B is poly(epsilon-caprolactone) (PCL), and has the molecular weight of 6000 Da; the block C is polyglutamic acid (PGA), and has the molecular weight of 1000 Da. The invention also discloses a biodegradable polymer vesicle with pH responsiveness, which is formed by self-assembly of the triblock copolymer with pH responsiveness, wherein a membrane core is formed by hydrophobic block PCL; the inner and outer walls of the membrane are formed by mPEG and PGA. The invention also discloses a drug-coated biodegradable polymer vesicle with pH responsiveness, which is high in encapsulation efficiency and drug loading capacity, and is formed by coating a hydrophilic drug by the triblock copolymer with pH responsiveness, wherein the hydrophilic drug is selected from doxorubicin hydrochloride, mitoxantrone hydrochloride, daunomycin hydrochloride, and cytosine arabinoside hydrochloride.

Description

technical field [0001] The invention relates to a novel drug carrier and its preparation technology, in particular to a pH-responsive biodegradable polymer vesicle and its preparation method and application, belonging to the fields of polymer chemistry and drug biomedical engineering. Background technique [0002] Biodegradable polymersomes are aggregated from biodegradable amphiphilic block polymers. A typical polymer vesicle is a spherical structure with a double-layer membrane surrounding the inner liquid core (Journal of Controlled Release, 2012, 161, 473-483). The double-layer membrane core is formed by aggregation of hydrophobic blocks, which can be used to solubilize hydrophobic drugs; the internal liquid cavity can be used to encapsulate hydrophilic molecules. Since the double-layer film isolates the wrapped substance from the external environment and protects the wrapped substance from the damage of the external environment, the contained substance can maintain goo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G69/48C08G69/40C08G69/10C08G63/91C08G63/664C08G65/48A61K47/34A61K9/127A61K31/704A61P35/00
Inventor 栾玉霞赵兰霞
Owner SHANDONG UNIV
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