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Flexible liposome containing drugs and preparation method thereof

A flexible liposome and liposome technology, applied in the field of medicine, can solve problems such as limited transdermal efficiency

Active Publication Date: 2019-07-12
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although flexible liposomes with general formulations can carry drugs into the epidermis, their transdermal efficiency is limited.

Method used

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  • Flexible liposome containing drugs and preparation method thereof
  • Flexible liposome containing drugs and preparation method thereof
  • Flexible liposome containing drugs and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] Embodiment 1 Preparation of drug-containing flexible liposomes of the present invention

[0089] Accurately weigh soybean lecithin, sodium deoxycholate or polysorbate 80, and vitamin E according to the formula, dissolve them in chloroform / ethanol or ethanol respectively, dissolve and mix them in a 250ml pear-shaped bottle, and rotate the evaporation at room temperature for 2 hours. The films were placed in a vacuum oven overnight. The next day, distilled water and appropriate amount of hydrophobically modified polypeptide DP7-C or PAL-DP7 were added, and a 400w probe was sonicated for 30 minutes to obtain a blank transfersome solution. Slowly add an appropriate amount of lidocaine or GLP-1 analogue (Ex-4) or EPO or NY-ESO-1, etc., and after incubating at room temperature for 40 minutes, filter the resulting mother liquor with a 0.2 μm polycarbonate membrane several times, add The excipient is 5% mannitol, which is divided into vials and freeze-dried to obtain the drug-...

Embodiment 2

[0178] Embodiment 2 The transdermal effect verification of the drug-containing flexible liposome of the present invention

[0179] The in vitro transdermal experiment uses a modified single-chamber Franz diffusion cell, and mouse skin is used as the skin for in vitro transdermal experiment. The transdermal absorption results of different drug-containing flexible liposomes are compared, and samples are taken at different time points. Small molecules By HPLC method, macromolecules are measured by ELISA method to measure the drug concentration in the transdermal receiving solution, and the cumulative transdermal amount is calculated.

[0180] Test Example 2-1 Verification of the transdermal effect of flexible liposomes containing lidocaine

[0181] 1. Materials

[0182] Sample: the lyophilized powder (1-1, 1-2, 1-3, 1-4) of the flexible liposome containing lidocaine prepared in Test Example 1 and the liposome containing lipocaine without DP7-C or PAL-DP7 modification The flexib...

Embodiment 3

[0230] Example 3 In vivo activity verification of drug-containing flexible liposomes of the present invention

[0231] The drug-containing flexible liposomes of the present invention all use relevant animal models to detect the drug activity after transdermal, and all use animal models and methods recognized in this field to verify.

[0232] Test Example 3-1 The effect of the flexible liposome comprising Ex-4 in the diet-induced obesity mouse (DIO) model

[0233] Exendin-4 (Ex-4) is a glucagon-like peptide 1 (GLP-1) analog, a polypeptide hormone isolated from the saliva of the Greek poisonous lizard, a polypeptide molecule containing 39 amino acids, and its amino acid The sequence has 53% homology with GLP-1. In mammals, Ex-4 has the same physiological function as GLP-1, and they act on the same receptor. Ex-4 can secrete insulin in a glucose concentration-dependent manner to lower blood sugar levels, stimulate the regeneration of islet β cells, induce the transcription of p...

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Abstract

The invention belongs to the technical field of medicine, and in particular, relates to a flexible liposome containing drugs and a preparation method thereof. Because of the barrier effect of skin, many drugs have low transdermal efficiency and poor absorption. Focusing on the problems, the invention provides the flexible liposome containing the drugs, wherein the flexible liposome is prepared from the flexible liposome-contained drugs modified by hydrophobically modified polypeptide. The specially modified liposome is prepared from the following main raw materials by the weight percentage: according to the weight ratio, the ratio of lecithin to sodium deoxycholate or polysorbate 80 or a derivative thereof is 7:(2-4), and the specially modified liposome contains 0.1-1 wt% of antioxidants,1-10 wt% of a hydrophobically modified polypeptide DP7-C or PAL-DP7 or the derivative thereof, and 1-10 wt% of the contained drugs. The designed and screened flexible liposome hydrophobically modifiedby the polypeptide can effectively carry drugs into a deep layer of skin, helps the drugs to play a role in cells, and has a good application prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a flexible liposome containing medicine and a preparation method thereof. Background technique [0002] Transdermal Drug Delivery (Transdermal Drug Delivery) is a new way of drug delivery through skin absorption into human blood circulation to achieve effective blood drug concentration, to achieve disease treatment or prevention. Transdermal drug delivery is an important field of drug research and development, and it is a new way of non-invasive drug delivery. Its advantages are as follows: 1) Drug absorption is not affected by complex factors such as pH value in the digestive tract, food and drug moving time in the intestinal tract, etc. ; 2) It can effectively avoid the first-pass effect of the drug in the liver; 3) The drug administration speed can be controlled continuously; 4) The drug site is on the body surface, and the patient can administer it by himself, an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/42A61K47/28A61K47/12A61K31/167A61K38/22A61K38/18A61K39/00
CPCA61K9/0014A61K9/1271A61K31/167A61K38/1816A61K38/2278A61K39/0011A61K47/12A61K47/28A61K47/42
Inventor 杨莉魏于全
Owner SICHUAN UNIV
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