RGD-SSL lipidosome for packaging turtle shell peptide and preparation method of lipidosome

A liposome and turtle shell peptide technology, which is applied in the field of RGD-SSL liposomes encapsulating turtle shell peptide and its preparation, can solve the problems of frequent administration and poor stability, reduce the frequency of administration, improve Effects of Local Biological Effects and Circulatory Half-Life

Inactive Publication Date: 2017-01-11
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • Abstract
  • Description
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Problems solved by technology

Biejia, as the king drug of Biejia Jianwan, Fufang Biejia Ruangan Tablets, Biejia Kangxian Fang, etc., plays an important role in the treatment of liver fibrosis in traditional Chinese medicine. Biejia peptide HGRFG belongs to oligopeptides, and peptides It is easy to degrade when taken orally, has poor stability, and needs frequent administration

Method used

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  • RGD-SSL lipidosome for packaging turtle shell peptide and preparation method of lipidosome
  • RGD-SSL lipidosome for packaging turtle shell peptide and preparation method of lipidosome
  • RGD-SSL lipidosome for packaging turtle shell peptide and preparation method of lipidosome

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Embodiment Construction

[0024] The technical scheme of the present invention will be further described below through specific implementation examples:

[0025] 1. First prepare RGD-PEG2000-DSPE

[0026] The raw materials are: a cyclic peptide with arginine-glycine-aspartic acid (RGD) sequence, its structural formula is as formula II and a DSPE-Poly(Ethylene Glycol)-Maleimide, Average Mw 2000, namely DSPE-PEG2000 -Mal, its structural formula is as shown in formula III:

[0027]

[0028] The preparation method of RGD-PEG2000-DSPE comprises the following steps:

[0029] Precisely weigh an appropriate amount of RGD and DSPE-PEG2000-Mal powder and place them in PBS (pH 6.0, containing 3mM EDTA, pH 4.0) buffer solution to prepare the corresponding stock solution. The molar ratio of the same volume is 1:1. The two solutions were respectively made RGD:DSPE-PEG2000-Mal=x:1 (molar ratio, x=1, 1.5, 2), and incubated at 37°C for 2h after sufficient shaking. with 50mM Na 2 HPO 4 (pH=7.0) Prepare and prepa...

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Abstract

The invention discloses an RGD-SSL lipidosome for packaging turtle shell peptide and a preparation method of the lipidosome. The turtle shell peptide long-cycle lipidosome modified by RGD comprises a lipidosome body and the turtle shell peptide (HGRFG) in the lipidosome body. The lipidosome body is prepared from egg yolk lecithin (EPC), cholesterol (Chol), mPEG2000-DSPE and RGD-PEG2000-DSPE according to the molar ratio of 50:25:1:0.6, and the weight ratio of the turtle shell peptide (HGRFG) to the EPC is 1:5 to 1:30. The defects that turtle shell peptide and other oligopeptides can easily degrade when orally taken and are low in bioavailability and short in half-life period are overcome; the RGD modified turtle shell peptide long-cycle lipidosome (RGD-SSL-turtle shell peptide) is obtained by packaging the turtle shell peptide with the granularity and RGD modified dual-control hepatic targeting lipidosome, the local biological effect and cycle half-life period are improved, the dosage frequency is reduced, and the lipidosome is suitable for treatment of hepatic fibrosis and other hepatic diseases.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an RGD-SSL liposome encapsulating turtle shell peptide and a preparation method thereof. Background technique [0002] Liposome has a phospholipid bilayer structure, which can encapsulate hydrophilic or lipophilic drugs to improve drug stability and increase drug solubility. It has good biocompatibility and degradability, and can undergo membrane fusion and endocytosis with cells. , has strong tissue affinity. In addition, liposomes can be designed to change the pharmacokinetic properties and in vivo distribution of drugs through component changes, surface modifications, particle size control, etc., and have certain tissue or cell targeting. Among them, liposomes with a particle diameter of less than 150 nm can pass through the fenestration of hepatic sinusoidal endothelial cells to reach the cavity of Disse, and the liposomes of the present invention have a particle d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61K9/127A61K47/18A61P1/16
CPCA61K38/08A61K9/1271A61K47/183
Inventor 张永生汤晗霄赵天文盛云杰屠珏蔡月琴郑杭生
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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