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Folate receptor-targeted antihypertensive peptide composition and preparation method thereof

A technology of folic acid receptor and antihypertensive peptide, which is applied in the field of antihypertensive peptide to achieve good antihypertensive effect, increase the amount of blood entering the blood, and reduce the effect of administration dose

Active Publication Date: 2016-08-03
SHENZHEN POLYTECHNIC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The applicant (recombinant antihypertensive peptide lactic acid-glycolic acid copolymer sustained-release microspheres preparation and in vitro release research. Chinese Journal of Pharmaceutical Sciences, 2012, 47 (24)) used polyester material lactic acid / glycolic acid copolymer (poly( D, L-lactide-co-glycolide), PLGA) prepared antihypertensive peptide-PLGA sustained-release microspheres, and in vitro release experiments showed that the microspheres had a good sustained-release effect in phosphate buffer at pH 7.4; After oral administration (the antihypertensive effect of recombinant antihypertensive peptide-poly(lactic acid-glycolic acid) copolymer sustained-release microspheres on spontaneously hypertensive rats. Chinese Journal of Pharmaceutical Sciences, 2012, 47(16)), on spontaneous Hypertensive rats showed a relatively stable antihypertensive effect; however, the oral bioavailability of the preparation still needs to be further improved

Method used

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  • Folate receptor-targeted antihypertensive peptide composition and preparation method thereof
  • Folate receptor-targeted antihypertensive peptide composition and preparation method thereof
  • Folate receptor-targeted antihypertensive peptide composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～6

[0033] Examples 1-6 Prepare folic acid-modified cholesterol with α-carboxy-ω-aminopolyethylene glycol as a spacer

[0034] The specific feed is shown in Table 1.

[0035] Table 1

[0036]

[0037] The specific operation is: take 0.5 mmol of α-carboxy-ω-amino polyethylene glycol (protected at the amino end), 0.75 mmol of cholesterol, 0.75 mmol of 4-dimethylaminopyridine and 1-ethyl-3-(3-dimethyl Dissolve 0.75 mmol of aminopropyl)-carbodiimide in 100 ml of dichloromethane, and react for about 72 to 96 hours. The organic solvent was removed by rotary evaporation under reduced pressure, and the crude product of aminopolyethylene glycol cholesterol was obtained by vacuum drying. Weigh 1mmol of folic acid, 2.5mmol of N-hydroxysuccinimide, 2.5mmol of 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide and 10mmol of triethylamine in 50ml of anhydrous DMSO Add about 0.5mmol aminopolyethylene glycol crude cholesterol product, react at 25-30°C for about 72-96h, transfer the reaction sol...

Embodiment 7～12

[0038] Examples 7-12 Prepare folic acid-modified cholesterol with diaminopolyethylene glycol as a spacer

[0039] The specific feed is shown in Table 2.

[0040] Table 2

[0041] Example

[0042] The specific operation is: dissolve cholesterol (10mmol), succinic anhydride (50mmol), and DMAP (5mmol) in 50mL of dichloromethane, reflux vigorously at 45°C, and stir for 48h to obtain succinylated lipids (cholesterol or phospholipids). Take succinylated lipid (4mmol), 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide (10mmol), N-hydroxysuccinimide (10mmol) dissolved in a small amount Dichloromethane, dropwise added to 100ml of bisaminopolyethylene glycol (5mmol) dichloromethane solution, stirred at room temperature for about 72-96h. The reaction solution was mixed with 60-80 mesh silica gel, packed with 300-400 mesh silica gel by wet method, and loaded by dry method. Using the dichloromethane-methanol system as the eluent, the ratio is from 80:1, 60:1, 40:1 to 20:1 (volume...

Embodiment 13

[0043] Example 13 Preparation of Folic Acid Modified VP5-PLGA Nanoparticles by Thin Film-Nano Hydration Method

[0044] Take 10 mg of PLGA and dissolve it ultrasonically in 1 ml of dichloromethane, add 200 μl of the inner aqueous phase containing 0.5 mg of VP5, and sonicate the probe for 1 min. Then add 4ml of 0.5% PVA solution, and ultrasonically treat the probe for 3min. The organic solvent was removed by rotary evaporation at 37°C to obtain a VP5-PLGA nanocolloid solution. Take 0.1 mg of folic acid-modified cholesterol, 1 mg of phospholipid, and 0.25 mg of cholesterol in Example 1, dissolve in 1 ml of chloroform, remove the organic solvent by rotary evaporation at 30°C, and obtain a lipid film, add VP5-PLGA nanocolloid solution, and hydrate with rotary at 60°C for 30 minutes. Ultrasound, that is. The encapsulation efficiency is 54%, and the particle size is 138nm.

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Abstract

The invention discloses a folate receptor-targeted antihypertensive peptide composition and a preparation method thereof, and relates to antihypertensive peptide. The antihypertensive peptide composition is prepared from 0.5-10 parts of antihypertensive peptide VP5, 0.1-5 parts of folate-modified lipid, 1-30 parts of phospholipid, 0.25-10 parts of cholesterol and 10-100 parts of a polyester material. The preparation method comprises the steps that 1, polyester nanoparticles loaded with the VP5 are prepared; 2, the folate-modified lipid, phospholipid and cholesterol are dissolved in an organic solvent, pressure reduction is conducted, rotary evaporation is conducted to remove the organic solvent, a thin film is obtained, the polyester nanoparticles loaded with the VP5 are added, hydration is conducted to remove the thin film, homogenizing or extruding is conducted after ultrasonic treatment is conducted, and the antihypertensive peptide composition is prepared; or the folate-modified lipid, phospholipid and cholesterol are dissolved in the organic solvent, pressure reduction is conducted, rotary evaporation is conducted to remove the organic solvent, a homogeneous thin film is prepared, then a normal saline solution or a glucose solution or a phosphate buffer solution is added, hydration is conducted to remove the thin film, the polyester nanoparticles loaded with the VP5 are added, homogenizing or extruding is conducted after ultrasonic treatment is conducted, and the antihypertensive peptide composition is prepared.

Description

technical field [0001] The invention relates to antihypertensive peptides, in particular to a folic acid receptor-targeted antihypertensive peptide composition and a preparation method thereof. Background technique [0002] Antihypertensive peptide is a general term for a class of small molecule peptides that can lower blood pressure in humans. It is an angiotensin-converting enzyme inhibitor, which can lower blood pressure by inhibiting the production of angiotensin II in the human body. It has the advantages of obvious antihypertensive effect and no effect on normal blood pressure. The applicant (genetic recombination and high-efficiency expression of antihypertensive peptides have acute antihypertensive effects on spontaneously hypertensive rats. Chinese Journal of Hypertension, 2010, 18 (1).) constructed a number of antihypertensive peptides, after a large number of screening studies, In the end, Val-Leu-Pro-Val-Pro (VLPVP, VP5) was selected to have a better antihyperte...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/51A61K38/08A61K47/34A61K47/48A61P9/12
CPCA61K9/5153A61K38/08
Inventor 杨剑宋相容孙海燕刘冬
Owner SHENZHEN POLYTECHNIC
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