Triphenylphosphine-polyethyleneglycol 1000 vitamin E succinate (TPGS 1000-TPP) conjugated compound, and preparation method and application thereof

The technology of a conjugated compound and polyethylene glycol is applied in the application field of the conjugated compound in the construction of paclitaxel liposomes, and can solve the problems of reduced curative effect of free drugs, low water solubility of paclitaxel and the like
CN102977360AInactive Publication Date: 2013-03-20PEKING UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
PEKING UNIV
Publication Date
2013-03-20
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a triphenylphosphine-polyethyleneglycol 1000 vitamin E succinate (TPGS 1000-TPP) conjugated compound, and a preparation method and application thereof. The structural formula of the compound is disclosed as Formula I. The preparation method of the conjugated compound comprises the following steps: (1) reacting triphenylphosphine and 6-bromocaproic acid to obtain 5-carboxyamyltriphenylphosphonium bromide disclosed as Formula IV; and (2) carrying out esterification reaction on the 5-carboxyamyltriphenylphosphonium bromide disclosed as Formula IV and polyethyleneglycol 1000 vitamin E succinate to obtain the conjugated compound disclosed as Formula I. The invention also discloses a mitochondrion targeted taxol liposome comprising the conjugated compound. The drug effect test proves that the mitochondrion targeted taxol liposome has strong cell toxicant action in the in-vitro cell experiment and in-vivo transplantation tumor model of human lung adenocarcinoma A549 cells and drug-resistant A549 / cDDP cells thereof and can enhance the antitumor effect of taxol on drug-resistant A549 / cDDP cells.
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Description

technical field

[0001] The present invention relates to a kind of triphenylphosphine-polyethylene glycol 1000 vitamin E succinate (TPGS 1000 -TPP) conjugated compound and its preparation method and application, specifically relating to the application of the conjugated compound in the construction of paclitaxel liposomes. Background technique

[0002] Drug delivery systems modified with functional materials offer a potential strategy for refractory cancers. Tumor refractory is not only related to the pathophysiological state of the patient, but also related to drug delivery. Chemotherapy drugs are usually administered in the form of injection of free drugs, and this method of administration will lead to less accumulation of drugs in tumor lesions and non-targeted distribution of pharmaceuticals in tissues and organs throughout the body.

[0003] In addition, tumor multidrug resistance is the main reason for the failure of chemotherapy, which can lead to drug resistance, re...

Claims

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