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Polymer nano-vesicle for co-delivering drug and perfluorooctylbromide, as well as preparation method and application thereof

A technology of nanovesicles and polymers, applied in the fields of chemistry, pharmacy and biomedical engineering, can solve the problems of gaps reaching around tumor cells and poor therapeutic effect, so as to prevent premature release and improve therapeutic effect

Active Publication Date: 2015-06-24
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the large diameter of commercialized microbubbles, usually in the micron range, the microbubbles can only be confined in the vascular system, and cannot reach the surrounding tumor cells through the tumor vascular endothelial space, so there is a defect of poor therapeutic effect; therefore, there is still a need for Seek a drug-loading system with a smaller diameter to achieve drug delivery deep into the tumor, thereby improving the therapeutic effect of the drug

Method used

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  • Polymer nano-vesicle for co-delivering drug and perfluorooctylbromide, as well as preparation method and application thereof
  • Polymer nano-vesicle for co-delivering drug and perfluorooctylbromide, as well as preparation method and application thereof
  • Polymer nano-vesicle for co-delivering drug and perfluorooctylbromide, as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Synthesis of a sour two -parent triangular segment polymer

[0041] (1) The synthesis of 的 的 ((, the reaction mechanism and the reaction process are as follows:

[0042]

[0043] Take 500 m L single -mouth eggplant bottle, add 100 ml aquatic ether, and then add 10 ml H 2 So 4 (98%), stir while adding it to room temperature, add 100 ml benzinylol (1 mol, 1.04 g / ml, 108.06 g / mol), stir fully, and steam the ether.Add L-Skywinate for a total of 13.3 g (0.1 mol, 133.04 g / mol).After the room temperature is stirred at 24 h, add 200 ml 95%ethanol, add 50 ml pyridine, and stir severe stirring while dripping.Then place it in the refrigerator to freeze overnight, draw filtering, wash the cakes with ultra -pure water, and wash it with hydropetan not to twice.Dorde it, place it in a 500 ml triangle bottle, add 300 to 400 ml of water, heat and stir dissolved at 70 ° C, can replenish water to 400-500 ml, all dissolve in 1.5 h, and the solution becomes clear.Hot filtering, filt...

Embodiment 2

[0059] Example 2 Three -embedded segment polymer Self -assembly as nanocarbal puff

[0060] Three-embedded segment polymer PEG-PAAPBA-PASP (DMA) 10 mg and 1 mg hydroponicin obtained from the three-in-segment polymer prepared by Practicing Example 1 Soluble in 1 mL methanol, and add 20 μL of liquid fluorocarbon (omn fluanotoxane), Slowly add to the carbonate buffer of pH = 10 under the action of ultrasound, and then incubate for 10 minutes after sealing; then analyze the methanol at 4 ° C, adjust the pH to 7.4 to form a nanocarbal structure.Slow the nanocomatic foam solution for 30 minutes, charge the upper liquid for centrifugation, and absorb the lower layer of liquid to the prepared coexistence drugs and liquid fluorocarbon polymer nano -foam ultrasonic contrast agents.Filter the filter film with a pore diameter of 0.45 μm to remove the hydrophobic drugs, and use a centrifugal ultrafiltration pipe (MWCO = 100 KD) for centrifugal ultrafiltration 3 times. figure 1 The simulation s...

Embodiment 3

[0061] Example 3 The particle size and appearance test test of the polymer of the drug and liquid fluorocarbon

[0062] The particle size of the polymer of the drug and liquid fluorocarbon is measured by the size of the nanocarbal veslery of the nanocarbal veslete. figure 2 , Explain that the nano -saw pyramids obtained by Example 2 are 133 ± 6.5nm; the form is observed by transmitting electron microscope. image 3 The observed nanocarbracular pipe size is uniform (118 nm).

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Abstract

The invention relates to an acid-sensitive amphipathic tri-block polymer. The polymer is composed of a polyethylene glycol-acid sensitive segment 1-acid sensitive segment 2 tri-block copolymer, wherein the acid sensitive segment 1 is poly(acrylamidophenylboronic acid); the acid sensitive segment 2 is poly(aminoacyl dimethyl-ethylenediamine); the molecular weight of the polyethylene glycol is 2000-5000, the molecular weight of the acid sensitive segment is 2000-6000, and the molecular weight of the acid sensitive segment is 1000-2000. The invention further relates to application of the acid sensitive amphipathic tri-block polymer in preparation of polymer nano-vesicle for co-delivering drug and perfluorooctylbromide. The nano-vesicle has a uniform nano-diameter, can stably circulate in a body and can be enriched in a tumor position, has excellent capability of reinforcing ultrasonic development to realize application of ultrasonic development under diagnostic ultrasound, and has ultrasonic sensitivity to stimulate the cavitation effect under a condition of low-frequency high-energy ultrasonic-radiation so as to realize controllable release of drugs.

Description

Technical field [0001] The present invention involves the field of chemistry, pharmacy and biomedical engineering, and more specific, involves a polymer foam and its preparation methods and applications for the transmission of drugs and liquid fluorocarbon. Background technique [0002] The tumor seriously threatens human health, and the mortality rate is high.There are three main methods of tumor treatment: surgery, radiological treatment, and chemical drug treatment (chemotherapy). Chemotherapy is usually adopted when tumor diffusion and metastasis.The commonly used chemotherapy drugs are mostly hydrophobic drugs. The solubility in the water is very low. Most of the small molecular surfactants are used for hydrophobic chemotherapy drugs during use.The side effects are also very large, and the release behavior is not easy to control.The polymer beam or vesicles are a new type of drug carrier. It is a nano structure formed by the autonomous loading of the two e -lips in the water...

Claims

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Application Information

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IPC IPC(8): C08G81/02C08G69/48C08G65/48C08F293/00C08F230/06C08F8/00A61K47/34A61K9/51A61K49/22A61P35/00
Inventor 帅心涛王逸如郑荣琴尹廷辉程度
Owner SUN YAT SEN UNIV
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