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A kind of scutellarin aglycone liposome preparation and preparation method thereof

A technology of scutellarin aglycone lipid and scutellarin aglycone, which is applied in the field of liposome containing insoluble Chinese herbal medicine active ingredient scutellarin aglycon and its preparation field, can solve the influence of scutellarin aglycon on stability , Poor chemical stability, short half-life, etc., to achieve good shape and encapsulation rate, maintain blood drug concentration, and increase drug concentration

Active Publication Date: 2019-03-29
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, scutellarin aglycon has the following problems: 1. The water solubility of scutellarin aglycon is extremely low (about 1 μg / ml); 2. The stability of scutellarin aglycone is relatively poor; the pH value of the solution, the temperature , Various enzymes and other factors in the body have a significant impact on the stability of scutellarin aglycon; 3. The protein binding rate of scutellarin aglycone is higher, and the half-life in vivo is shorter
[0006] Due to the extremely low water solubility and poor chemical stability of scutellarin aglycon, there are no research reports on scutellarin aglycon preparations

Method used

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  • A kind of scutellarin aglycone liposome preparation and preparation method thereof
  • A kind of scutellarin aglycone liposome preparation and preparation method thereof
  • A kind of scutellarin aglycone liposome preparation and preparation method thereof

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preparation example Construction

[0083] Preparation method of scutellarin aglycone liposome preparation

[0084] The preparation method of the scutellarin aglycone liposome preparation of the present invention comprises:

[0085] (1) prepare inner aqueous phase and outer aqueous phase and all contain the blank liposome of acetate aqueous solution;

[0086] (2) preparing blank liposomes whose inner water phase contains acetate aqueous solution and whose outer water phase contains physiological isotonic solution;

[0087] (3) Mix the blank liposome obtained in step (2) with the scutellarin aglycone solution, incubate, remove free scutellarin aglycone, and obtain a scutellarin aglycone liposome preparation.

[0088] The acetate may be sodium acetate or calcium acetate.

[0089] The concentration of acetate in the acetate aqueous solution may be 50mM˜500mM. It can also be 150mM-500mM.

[0090] The pH range of the acetate aqueous solution may be 5.0-9.0. The pH value range of the acetate aqueous solution may ...

Embodiment 1

[0114] Example 1 The solubilization of different cosolvents to scutellarin aglycon

[0115] 1. Sodium bicarbonate, PEG300, PEG400, and propylene glycol were purchased from Sinopharm Chemical Reagent Co., Ltd., and hydroxypropyl-β-cyclodextrin (HPCD) was purchased from Shifeng Biological Co., Ltd.

[0116] 2. The influence of different co-solvents on the solubility of scutellarin aglycone:

[0117] (1) Precisely weigh 4.9983g of sodium bicarbonate and dissolve it in 100ml of 18.2MΩ water to obtain a 5% sodium bicarbonate aqueous solution; precisely weigh 1.2034mg of scutellarin aglycon and dissolve it in 1ml of 5% sodium bicarbonate solution.

[0118](2) Accurately weigh 9.8174mg, 9.9035mg, and 9.8665mg scutellarin aglycone respectively, dissolve them in 1 mg PEG300, PEG400, and propylene glycol solution respectively, vortex for 3 minutes, and ultrasonicate for 30 minutes, and the scutellarin aglycone is fully dissolved to obtain scutellarin Vegetarian aglycone suspension, the...

Embodiment 2

[0134] Example 2 Preparation and characterization of scutellarin aglycone liposomes

[0135] 1. Hydrogenated soy lecithin (HSPC) was purchased from NOF Corporation, and pegylated phospholipids: distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) and cholesterol were purchased from Avanti PolarLipids, USA ; Scutellarin aglycone was purchased from Nanjing Jingzhu Biotechnology Co., Ltd.; calcium acetate was purchased from Sinopharm Chemical Reagent Co., Ltd.

[0136] 2. Preparation of scutellarin aglycon liposomes

[0137] (1) Accurately weigh 479.9 mg of cholesterol (CHOL, molecular weight 386.7), 160.9 mg of hydrogenated soybean lecithin (HSPC, molecular weight 783.8) and 160.8 mg of distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000), add 1 milliliter of ethanol was bathed in a water bath at 70 degrees Celsius to fully dissolve and mix to obtain a lipid-ethanol mixed solution;

[0138] (2) Add 10 milliliters of pH 7.40300mM calc...

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Abstract

The invention belongs to the technical field of nano-drug delivery, and particularly relates to a lipidosome containing an insoluble Chinese herb effective ingredient scutellarein and a preparing method thereof. By utilizing the good lipotropy (logD is 2.54 (chemspider)) of scutellarein, scutellarein can pass through a lipid bilayer and enter the inner water phase in the form of molecules, and scutellarein can be ionized into scutellarein ions under the high pH condition of the inner water phase. As a phospholipid membrane almost has no permeability for ions, the pH gradient of the inner water phase and the outer water phase of the lipidosome can be utilized to achieve the purpose of stably encapsulating scutellarein. Meanwhile, by wrapping scutellarein in the inner water phase of the lipidosome, the chemical stability of scutellarein in the storage process can be easily improved.

Description

technical field [0001] The invention belongs to the technical field of nano-medicine delivery, and in particular relates to a liposome containing scutellarin aglycon, an effective component of insoluble Chinese herbal medicine, and a preparation method thereof. Background technique [0002] Erigeron breviscapus, also known as Erigeron breviscapus, sagegrass, and double sunflower, is the dry whole herb of Asteraceae breviscapita, mainly distributed in Southwest China. Erigeron breviscapus is cold in nature, slightly bitter, sweet and warm, and has the effects of anti-inflammatory and pain relief, expelling wind and dampness, promoting blood circulation and removing blood stasis, dredging meridian and activating collaterals, and can be used to treat cardiovascular and cerebrovascular diseases. It was first collected in "Southern Yunnan Materia Medica". As one of the common Chinese herbal medicines, breviscapus is widely spread among the people. It is commonly used in the pres...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/352A61K47/12A61P9/10A61P25/00A61P7/02
CPCA61K9/127A61K31/352A61K47/12
Inventor 魏晓慧金玲玲徐宇虹
Owner SHANGHAI JIAO TONG UNIV
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