All-trans retinoic acid liposome preparation and preparation and application thereof

A technology of all-trans retinoic acid and liposome preparations, which is applied in the direction of liposome delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve the problem of all-trans retinoic acid liposomes Unsatisfactory drug loading and in vivo stability, to achieve good in vivo stability, high drug loading, and high drug loading

Active Publication Date: 2018-03-06
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Limited by the physical properties of all-trans retinoic acid, the all-trans retinoic acid liposomes prepared by this method are not ideal in terms of drug loading and in vivo stability

Method used

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  • All-trans retinoic acid liposome preparation and preparation and application thereof
  • All-trans retinoic acid liposome preparation and preparation and application thereof
  • All-trans retinoic acid liposome preparation and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Preparation and identification of embodiment 1 all-trans retinoic acid liposome

[0075] 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; Trans-retinoic acid was purchased from Sigma, USA.

[0076] One, the preparation of all-trans retinoic acid liposome

[0077] (1) Weigh 121.742 grams of hydrogenated soybean lecithin (HSPC, molecular weight 783.8), 38.22 grams of distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) and 40.04 grams of cholesterol, dissolve them with 1.6 milliliters of ethanol, and Water bath in a water bath at 70 degrees Celsius to dissolve and mix to obtain an ethanol mixture;

[0078] (2) Add 6.4 ml of the ethanol mixture obtained in step (1) to calcium acetate buffer (pH 9.0, which consists of 200 mM calcium acetate and water), and place in a w...

Embodiment 2

[0094] Embodiment 2, active drug loading prepares all-trans retinoic acid liposome and passive drug loading prepares all-trans retinoic acid liposome comparison

[0095] 1. Preparation of all-trans retinoic acid liposomes by active drug loading method and passive drug loading method

[0096] 1. Preparation of all-trans retinoic acid liposomes by active drug loading method

[0097] (1) Weigh 121.742 grams of hydrogenated soybean lecithin (HSPC, molecular weight 783.8), 38.22 grams of distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) and 40.04 grams of cholesterol, dissolve them with 1.6 milliliters of ethanol, and Water bath in a water bath at 70 degrees Celsius to dissolve and mix to obtain an ethanol mixture;

[0098] (2) Add 6.4 ml of the ethanol mixture obtained in step (1) to calcium acetate buffer (pH 9.0, which consists of 200 mM calcium acetate and water), and place in a water bath at 70 degrees Celsius for 30 minutes to obtain liposome vesicle...

Embodiment 3

[0116] Example 3. All-trans retinoic acid liposomes induce differentiation of tumor myeloid suppressor cells in vitro

[0117] 1. Tumor model establishment in Balb / c mice

[0118] (1) When CT-26 cells were cultured to the logarithmic growth phase, they were digested with trypsin, and the digested cells were collected and centrifuged in a centrifuge at a speed of 300g for 5 minutes, the supernatant was discarded, and the cells were resuspended with sterile PBS. Count the cells and adjust the cell concentration to 1*10 7 cells / ml;

[0119] (2) Purchase 6-week-old Balb / c white mice, shave the fur on the side of the subcutaneous inoculation in advance, inject 200 μl of 4% chloral hydrate intraperitoneally to anesthetize the mouse, and inject it subcutaneously in the right underarm for digestion The CT-26 suspension, the cell seeding volume is 5*10 5 -1*10 6 / only, continue to raise after inoculation;

[0120] (3) After feeding for about 2-3 weeks, use a vernier caliper to me...

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Abstract

The invention belongs to the technical field of biological pharmacy, and particularly relates to an all-trans retinoic acid liposome preparation and a preparation technology thereof. The all-trans retinoic acid liposome preparation comprises all-trans retinoic acid and a liposome vector. According to the method, the all-trans retinoic acid liposome preparation is prepared through an active drug loading method, and an all-trans retinoic acid preparation which is high in drug loading capacity and stable in liposome is formed. The all-trans retinoic acid liposome preparation prepared through themethod greatly improves plasma drug concentration in all-trans retinoic acid liposome, and prolongs the half life.

Description

technical field [0001] The invention belongs to the technical field of biopharmaceuticals, and in particular relates to an all-trans retinoic acid liposome preparation and its preparation and application. Background technique [0002] Retinoic acid is a metabolite of vitamin A in the body. All-trans retinoic acid (ATRA) is used as a drug to treat acne, and it is also an important drug for the clinical treatment of acute promyelocytic leukemia (APL). All-trans retinoic acid (ATRA) affects gene expression by binding to specific receptors (RARs, RXRs and RORs) in cells. In the treatment of acute promyelocytic leukemia, it can promote the differentiation of APL cells and the degradation of PML / RARαgene , to achieve the therapeutic effect. [0003] However, the clinical application of all-trans retinoic acid is limited by the following aspects: 1. the water solubility of all-trans retinoic acid is extremely low (4.77e-03g / l); 2. the plasma half-life of all-trans retinoic acid i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/203A61K47/40A61K47/10A61K47/32A61K47/38A61P35/00
CPCA61K9/0019A61K9/127A61K31/203A61K47/10A61K47/32A61K47/38A61K47/40A61P35/00A61K9/1271A61K47/24A61K47/28A61K9/1272A61K9/1278
Inventor 徐宇虹郑安杰陈晓龙
Owner SHANGHAI JIAO TONG UNIV
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