IRGD peptide modified co-loaded curcumin and piperine liposome and preparation method thereof

A technology of piperine fat and curcumin, applied in the field of biomedicine, can solve problems such as unsatisfactory curative effect, low solubility and limitation of curcumin, and achieve the effects of improving bioavailability, increasing therapeutic effect and saving operation time.

Pending Publication Date: 2022-04-15
FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, curcumin's low solubility and easy elimination in the body limit its clinical application.
After oral administration, curcumin will also be metabolized into water-soluble glucuron

Method used

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  • IRGD peptide modified co-loaded curcumin and piperine liposome and preparation method thereof
  • IRGD peptide modified co-loaded curcumin and piperine liposome and preparation method thereof
  • IRGD peptide modified co-loaded curcumin and piperine liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] (CUR+PIP)-LPs ((CUR+PIP)-LPs (curcumin and piperine combined liposomes) were prepared by thin film hydration method: lecithin (PC), cholesterol (CHO), turmeric In a round bottom flask, PC: 500mg, CHO: 100mg, CUR: 10mg, PIP: 0.5mg, dissolved in 20mL of chloroform by ultrasonic, and then evaporated by rotary evaporation at 40℃ Evaporate the solvent to form a film, then add 20mL phosphate buffer (pH=6.5), rotate at 60°C for 20min to dissolve the film, stir magnetically at a constant temperature of 60°C for 20min, and filter through a 0.22μm filter membrane.

Embodiment 2

[0070] Determination of maximum absorption wavelength of CUR and PIP

[0071] Preparation of CUR and PIP reference solution

[0072] Reference substance stock solution: take 1.28mg of CUR reference substance, accurately weigh it, place it in a 10mL brown measuring bottle, add methanol to dissolve and dilute, and set the volume to the mark to prepare curcumin reference substance stock solution with a mass concentration of 128μg / mL ; Take 1.35 mg of the PIP reference substance, accurately weighed, place in a 10mL brown measuring bottle, add methanol to dissolve and dilute, and set the volume to the mark to prepare a piperine reference substance stock solution with a mass concentration of 135 μg / mL.

[0073] Reference substance dilution: Dilute curcumin reference stock solution and piperine reference substance stock solution 10 times with methanol to prepare curcumin reference substance dilution of 12.8 μg / mL and piperine reference substance of 13.5 μg / mL Diluent.

[0074] Mixe...

Embodiment 4

[0099] Determination of Encapsulation Efficiency

[0100] (1) Determination of Curcumin Encapsulation Efficiency

[0101] Take 0.5 mL of the prepared unfiltered liposomes, add methanol and ultrasonically break the emulsion for 20 minutes, centrifuge at 13,000 r / min for 10 minutes, filter the supernatant with a 0.22 μm filter membrane, inject samples according to the chromatographic conditions under "3.1", and record the peak area . Take it into the mixed standard solution to calculate the content of curcumin, as the total amount of curcumin W1; absorb and filter the equal volume of liposomes, add methanol for 20 minutes to ultrasonically break the emulsification, centrifuge at 13000r / min for 10 minutes, and filter the supernatant with a 0.22 μm membrane After filtration, inject samples according to the chromatographic conditions under "3.1", and record the peak area. Bring into the mixed standard song solution to calculate the content of curcumin, as the quality W2 of curcum...

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Abstract

The invention discloses a preparation method of iRGD peptide modified and co-loaded curcumin and piperine lipidosome, which comprises the following steps: mixing curcumin, piperine, lecithin, cholesterol, iRGD-PEG2000-DSPE, DSPE-PEG2000 and trichloromethane to obtain a mixture; performing rotary evaporation on the mixture to form a film; and dissolving the membrane in an acid environment, and sequentially stirring and filtering to obtain the iRGD peptide modified co-loaded curcumin and piperine liposome. The invention further discloses the iRGD peptide modified and co-loaded curcumin and piperine lipidosome. The invention also discloses an application of the iRGD peptide modified co-loaded curcumin and piperine liposome in establishing an in-vitro A549 cell inhibition model and a rotary evaporator. The iRGD peptide nano-drug delivery system has the advantages that the iRGD peptide is used as a specific targeting ligand of the nano-drug delivery system, aggregation of drugs in tumor cells can be increased, distribution of the drugs in normal tissues can be reduced, and a better anti-tumor effect can be achieved.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to iRGD peptide modified co-loaded curcumin and piperine liposomes and a preparation method thereof. Background technique [0002] Lung cancer is one of the most common malignant tumors in my country, and its morbidity and mortality rate ranks first among malignant tumors. The 5-year survival rate is only 19.7%. Chemotherapy is currently one of the main methods for the clinical treatment of lung cancer. However, due to the large dosage and lack of specificity of most chemotherapy drugs, they can also produce toxicity to normal tissues and cells, leading to serious side effects and multidrug resistance. And allergies, efficacy is limited. Therefore, it is extremely urgent to seek a safe and efficient anti-lung cancer targeted drug delivery system. [0003] The iRGD peptide is a targeted penetrating peptide, which can specifically recognize the integrin αvβ3 receptor on the surf...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/62A61K31/12A61K31/4525A61P35/00C12N5/09C12N5/071C12Q1/02
CPCA61K47/6911A61K47/62A61K31/12A61K31/4525A61P35/00C12N5/0693C12N5/0688G01N33/5011C12N2503/02G01N2500/10A61K2300/00Y02A50/30
Inventor 王英豪肖志勇方丽金
Owner FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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