Preparation of targeted liposome and application thereof

A targeted and compound technology, which is applied in the direction of liposome delivery, digestive system, non-active ingredients of polymer compounds, etc., can solve problems such as inability to complete targeted delivery

Active Publication Date: 2015-09-16
SHANGHAI JIBEI PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, ordinary liposomes cannot achieve the effect of targeted delivery, so ordinary liposomes need to be modified to achieve active targetin

Method used

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  • Preparation of targeted liposome and application thereof
  • Preparation of targeted liposome and application thereof
  • Preparation of targeted liposome and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0064] 1. Materials and methods

[0065] 1.1 Cells and main reagents

[0066] Human liver cancer cell line HepG2 cells were subcultured and preserved in our laboratory; RNeasy Mini Kit was purchased from QIAGEN; Premix Ex Taq Version2.0 was purchased from Takara; FastDigest Xho I and FastDigest EcoR I were purchased from ThermoFisher; Mal-PEG 2000 -DSPE and mPEG 2000 -DSPE was purchased from NANOCS Company in the United States; soybean phosphatidylcholine DSPC S-100 was purchased from Lipoid Company in Germany; cholesterol (Cholesterol) and sodium fluorescein were purchased from SIGMA Company; peptides used in the experiment were synthesized by Hangzhou Zhongpei Biochemical Co., Ltd.

[0067] 1.2 Construction and identification of HepG2-NTCP cells

[0068] Total RNA was extracted from human liver tissue, reverse transcription PCR was performed, and the NTCP coding sequence was amplified; the pCMV vector was constructed by Xho I and EcoR I, and the NTCP expression plasmid pCM...

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Abstract

The present invention relates to preparation of target liposom and uses thereof, particularly to the target hepatocellular compound of formula 1, the composition and pharmaceutical composition containing the compound for delivering drugs. In formula 1, X is a polypeptide derived from hepatitis B virus adventitial protein PreS1 zone, specifically binding with natrium ion-taurocholic acid co-transferred polypeptide (NTCP); B is a maleimide-polyethyleneglycol-stearoyl phosphatidyl ethanolamine polymer represented by formula 2; in formula 2, n is an integer of 2-100, DSPE is stearoyl phosphatidyl ethanolamine; X is linked with B by the maleimide portion of formula 2.

Description

technical field [0001] The invention relates to the preparation and application of targeting liposome, in particular to the preparation and application of liver targeting liposome. Background technique [0002] Liver-related diseases are one of the important diseases affecting human health. In my country, more than 300,000 people die from end-stage liver disease every year. However, most of the drugs currently used for the treatment of liver diseases are systemically administered, which has the disadvantages of less liver distribution, instability in the body, and more extrahepatic side effects, which limits the clinical application of drugs. Therefore, how to efficiently deliver drugs to the liver, better play a therapeutic role, and reduce extrahepatic side effects is a major problem to be solved in the field of liver disease treatment (Poelstra K, Prakash J, Beljaars L.Drug targeting to the diseased liver[J] .Journal of controlled release: official journal of the Control...

Claims

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Application Information

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IPC IPC(8): C08G65/00A61K9/127A61K47/42A61P1/16A61P31/20
CPCA61K9/1271A61P1/16A61P31/20C08G65/3312C08G65/3322C08G65/33306C08G65/33337
Inventor 刘宏利韩超
Owner SHANGHAI JIBEI PHARMA TECH
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