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PH and temperature sensitive nano-vesicles and preparing method and application thereof

A dual-sensitivity, nano-vesicle technology, applied in the fields of polymer chemistry and biomedical engineering, to achieve the effect of increasing deep tissue penetration and excellent chain flexibility

Active Publication Date: 2016-10-12
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The optimal size for nanoparticles to be enriched in the tumor site through the EPR effect is below 200 nm, and this size is a great challenge for contrast agents with good ultrasound responsiveness

Method used

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  • PH and temperature sensitive nano-vesicles and preparing method and application thereof
  • PH and temperature sensitive nano-vesicles and preparing method and application thereof
  • PH and temperature sensitive nano-vesicles and preparing method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1 Polymer PEG-PAsp (DEA- co -His- co -DIP) preparation

[0045] 1, β -The synthesis of benzyl aspartate, reaction mechanism and reaction process are as follows:

[0046]

[0047] First prepare a one-necked flask (500 mL), add 100 mL of anhydrous diethyl ether, then slowly add 10 mL of concentrated H 2 SO 4 (98%), stirring vigorously while adding dropwise, after cooling to room temperature, add 100 mL benzyl alcohol, after fully stirring, use a rotary evaporator to rotary evaporate ether. Then add a total of 13.3 g of aspartic acid into the reaction flask in 3 times. The reaction was uniformly stirred at room temperature for 24 h, then 200 mL of 95% ethanol was added, and 50 mL of pyridine was added dropwise with a dropping funnel, and vigorously stirred while dropping. Then refrigerated overnight, pumped the filtered solid, stirred and dissolved at 80°C, filtered hot, and refrigerated the filtrate overnight. Filter, recrystallize 2 times according t...

Embodiment 2

[0061] Example 2 Drug-loaded nanovesicles mPEG-PAsp (DEA- co -His- co -DIP) preparation

[0062] A nanovesicle loaded with hydrophilic antitumor drugs is prepared by the following method: take the polymer mPEG-PAsp (DEA-PAsp) prepared in Example 1 CO -His- CO -DIP) 20 mg, with 2 mL of anhydrous CHCl 3 After dissolving, 0.2 mL of water dissolved with doxorubicin was added dropwise into chloroform by ultrasound in an ice-bath environment to form the first emulsion. Then, the first emulsion was added dropwise to 10 mL of PBS (pH 7.4, 0.05 mol / L) under the same conditions, and the second emulsion was formed after ultrasonication for 5 minutes. Chloroform was then removed by rotary evaporation, followed by dialysis against pH 7.4 PBS using a 14 KDa dialysis bag to remove uncoated doxorubicin. The final vesicle solution was filtered with a 450 nm filter to obtain doxorubicin-loaded nanovesicles (referred to as DOX-PPEHD vesicles).

[0063] A nanovesicle loaded with an ul...

Embodiment 3

[0072] Example 3 Drug-loaded nanovesicles mPEG-PAsp (DEA- co -His- co -DIP) thermogravimetric analysis

[0073] After the PFP / DOX-PPEHD vesicles were treated, the thermal weight loss of the vesicles was detected by the thermal analysis system Pyrisis-1 (PerkineElmer, USA). We used TGA to measure the thermal stability of PFP / DOX-PPEHD vesicles, and we selected DOX-PPEHD vesicles without PFP as the control group. Such as Figure 6 As shown, PFP / DOX-PPEHD vesicles experienced the first weight loss between 40 °C and 80 °C, while DOX-PPEHD vesicles did not experience this weight loss at this temperature range, the reason for this weight loss It is the PFP contained in the PFP / DOX-PPEHD vesicles that reaches the boiling point in this temperature range and turns into a gas, and the vesicles are gradually burst and released. From the weight loss rate, we can calculate that the load rate of PFP is 3.24%. In the figure, we found that both PFP / DOX-PPEHD vesicles and DOX-PPEHD vesi...

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Abstract

The invention belongs to the fields of high polymer chemistry and biomedical engineering, and particularly discloses a pH and temperature sensitive polymer. The polymer is composed of a hydrophilic polyethylene glycol segment, and a lyophobic poly-(aspartic acid-diethyl-ethylenediamine-co-histamine-co-diisopropyl ethylenediamine) segment, and the ratio of the hydrophilic segment to the lyophobic segment is (1:10)-(1:12). The pH and temperature sensitive polymer can be used for preparing nano-vesicles loaded with hydrophilic anti-tumor drugs or / and ultrasonic contrast agents, and the nano-vesicles can be used for preparing tumor diagnosis drugs or tumor treatment drugs.

Description

technical field [0001] The invention relates to the fields of polymer chemistry and biomedical engineering, in particular to a pH- and temperature-sensitive polymer nanovesicle and its preparation method and application. Background technique [0002] In the medical field, cancer is a complex disease model. With the exploration of materials chemistry and nanomedicine, the long-term innovative development of nanocarriers has completely changed the way of cancer diagnosis and treatment. This in turn has promoted the design and development of many new nanocarriers for cancer diagnosis and treatment. In particular, nanocarriers sensitive to stimuli in response to the tumor microenvironment emerge in endlessly. The original single-functional nanocarriers have gradually developed into dual or multiple responsive nanocarriers. sought after. This makes the diagnosis and treatment of cancer more miniaturized, more convenient, sensitive and accurate, which has important research sign...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K49/22A61K47/34A61K47/06C08G69/48C08G69/16A61P35/00A61K31/704
CPCA61K47/06A61K47/34A61K49/225A61K9/0009A61K9/1273C08G69/16C08G69/48A61K31/704
Inventor 帅心涛张路邱晨黄毅左明祥程度
Owner SUN YAT SEN UNIV
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