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Medicine carrying micelle capable of increasing bioavailability of ursolic acid and structural modifier thereof

A technology of drug-loaded micelles and ursolic acid, which is applied in the field of biofunctional materials and nanometers, can solve the problems that the solubility has not been significantly improved, the average particle size of drug-loaded micelles is large, and the requirements for equipment are high, so as to achieve stable and reliable drug loading Quantity, improve bioavailability, low equipment requirements

Inactive Publication Date: 2014-06-25
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this series of derivatives can improve their anticancer activity to varying degrees, their solubility in water has not been significantly improved, resulting in low bioavailability.
[0009] Patent CN101889983A discloses a drug-loaded nanoparticle of polymer material. The nanoparticle adopts PEG-PLGA diblock polymer to form micelles, and the distribution range of nanoparticle size is too wide (50-500nm). High equipment requirements
[0010] Patent CN103271874A discloses a kind of macromolecular material loaded paclitaxel nanoparticles, which uses PEG-PLGA-PEG triblock polymer to form micelles, and the distribution range of nanoparticle size is too wide (20-500nm). Disadvantages of higher requirements
In this patent, surfactants need to be added during the preparation of drug-loaded nanomicelles, and the average particle size of drug-loaded micelles obtained is relatively large

Method used

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  • Medicine carrying micelle capable of increasing bioavailability of ursolic acid and structural modifier thereof
  • Medicine carrying micelle capable of increasing bioavailability of ursolic acid and structural modifier thereof
  • Medicine carrying micelle capable of increasing bioavailability of ursolic acid and structural modifier thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Blank group:

[0044] Accurately weigh 30 mg of PLGA-PEG-PLGA and dissolve in 10 mL of acetone to form the organic phase. Slowly drop dropwise into 50mL of vigorously stirred ultrapure water, stir magnetically at room temperature to completely volatilize acetone, pass the solution through a 0.45μm microporous membrane to obtain a PLGA-PEG-PLGA empty carrier micellar solution, and freeze-dry to prepare Blank micelles. The stirring speed is 1200 rpm (stirring for 48 hours), and the dropping speed is controlled by using a constant pressure funnel to control 1 drop every 3 minutes. Drug-loaded micelles particle size test results (DLS) see figure 1 .

Embodiment 2

[0046] Accurately weigh 30mg of PLGA-PEG-PLGA and 30mg of US580 and dissolve in 10mL of acetone to form the organic phase. Slowly add dropwise to 50mL vigorously stirred ultrapure water, stir magnetically at room temperature to completely volatilize acetone, pass the solution through a 0.45μm microporous membrane to remove unencapsulated drugs, and obtain PLGA-PEG-PLGA-loaded US597 gel Beam solution, lyophilized to prepare US597-loaded micelles. The stirring speed is 1100 rpm (stirring for 36 hours), and the dropping speed is controlled by a constant pressure funnel to control 1 drop every 5 minutes. Drug-loaded micelles particle size test results (DLS) see figure 2 .

Embodiment 3

[0048] Accurately weigh 30mg of PLGA-PEG-PLGA and 5mg of US597 and dissolve in 10mL of acetone to form the organic phase. Slowly add dropwise to 50mL vigorously stirred ultrapure water, stir magnetically at room temperature to completely volatilize acetone, pass the solution through a 0.45μm microporous membrane to remove unencapsulated drugs, and obtain PLGA-PEG-PLGA-loaded US597 gel Beam solution, lyophilized to prepare US597-loaded micelles. The stirring speed is 1000 rpm (stirring for 48 hours), and the dropping speed is controlled by using a constant pressure funnel to control 1 drop every 4 minutes. Drug-loaded micelles particle size test results (DLS) see image 3 .

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Abstract

The invention relates to the fields of biological functional materials and nanotechnologies and particularly relates to a novel amphiphilic polymer nano medicine carrying micelle which is proper in particle size distribution range, stable in encapsulation rate and medicine carrying rate, high in biological safety and capable of increasing bioavailability of ursolic acid and a structural modifier thereof. The technical scheme of the invention provides a medicine carrying micelle capable of increasing bioavailability of ursolic acid and a structural modifier thereof. The medicine carrying micelle is characterized in that the preparation method comprises the following steps of 1, synthesizing PLGA-PEG-PLGA (poly(lactic-co-glycolic acid)-polyethylene glycol-poly(lactic-co-glycolic acid)) by using a ring opening polymerization method; 2, simultaneously dissolving an insoluble drug and a triblock copolymer into an organic solvent to prepare an oil phase; 3, dropwise adding the oil phase into a water phase stirred at a high speed; 4, stirring until the oil phase is completely volatilized, and filtering a membrane in the solution to obtain a medicine carrying nanoparticle contained ultrapure water solution; freezing and drying to obtain the medicine carrying micelles.

Description

technical field [0001] The invention relates to the field of biofunctional materials and nanotechnology, in particular to a new type of ursolic acid with suitable particle size distribution range, stable encapsulation rate and drug loading rate, high biological safety, and can improve the bioavailability of ursolic acid and its derivatives Amphiphilic polymer nano drug-loaded micelles. Background technique [0002] In recent years, a natural source of pentacyclic triterpenoid ursolic acid (Ursolic acid, UA) has attracted attention at home and abroad due to its wide range of biological activities such as anti-tumor, liver protection, anti-inflammation, anti-virus, anti-oxidation, etc. researchers' attention. Especially for its remarkable anti-cancer effect and good liver protection effect, it has been valued. Pharmacological experimental studies have proved that UA has: 1) inhibition of malignant tumor cell proliferation; 2) induction of tumor cell differentiation and apopt...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/56A61K47/34A61P35/00
Inventor 邵敬伟杨祥向利平许煜陈孝炜贾力
Owner FUZHOU UNIV
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