A kind of liposome loaded with camptothecin class antitumor drug, preparation method and application thereof
A technology of anti-tumor drugs and liposomes, which is applied in the direction of anti-tumor drugs, liposome delivery, drug combination, etc. It can solve the problems that SN38 cannot be introduced into the drug delivery system, liposome incompatibility, low encapsulation efficiency, etc.
Inactive Publication Date: 2019-01-29
金华市人民医院
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Problems solved by technology
[0006] Our previous experiments showed that due to its unique chemical structure, SN38 is not compatible with liposomes, which leads to the inability of SN38 to be introduced into the drug delivery system of liposomes and low encapsulation efficiency, or the drug may be rapidly absorbed in the body. release problem
Method used
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Embodiment 1
[0028] The synthesis method of linoleic acid-SN38 (LA-SN38) refers to the applicant's previous patent "7-ethyl-10-hydroxycamptothecin prodrug and its preparation method and application", and the patent application number is 201410295432.X.
Embodiment 2
[0030] The synthesis method of RA-SN38 refers to the applicant's previous patent "An all-trans retinoic acid-camptothecin anticancer drug conjugate and its preparation method and application", the patent application number or patent number is 201410692682.7.
Embodiment 3
[0032] The synthesis method of linolenic acid-SN38 refers to the applicant's previous patent "7-ethyl-10-hydroxycamptothecin prodrug and its preparation method and application", and the patent application number is 201410295432.X.
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Abstract
The invention discloses a camptothecin-carried alkaline antitumor drug liposome as well as a preparation method and an application of the camptothecin-carried alkaline antitumor drug liposome. The liposome comprises a liposome bilayer and an antitumor drug, wherein the liposome bilayer comprises phospholipid, cholesterol and a PEG (polyethylene glycol) modified substance. The preparation method is simple, easy to operate and good in repeatability. The prepared antitumor drug liposome has the advantages of slowly releasing the drug and prolonging the circulation time of the drug in blood and has better tumor targeting property, the capacity of efficiently inhibiting proliferation or growth of tumor cells or tumor tissue is shown in vivo and in vitro, broad antitumor application prospect of the antitumor drug liposome is confirmed, and a novel research program is provided for research of cancer therapy.
Description
technical field [0001] The invention relates to a liposome loaded with camptothecin class antitumor drugs, a preparation method of the liposome loaded with drugs, and an application thereof in tumor treatment. Background technique [0002] Irinotecan (CPT-11) is a semi-synthetic derivative of camptothecin, which is approved for the treatment of various cancer diseases. CPT-11 uses topoisomerase as the target site, and inhibits topoisomerase I- The combination of DNA complexes prevents the reconnection of broken single strands, unwinds the DNA double-strand structure and exerts anti-tumor effects. However, after water-soluble CPT-11 enters the body, there are defects such as instability, rapid elimination, and short maintenance time of blood drug concentration; in addition, CPT-11 is transformed into the active ingredient 7-ethyl-10-hydroxylhibidium in vivo, which has anticancer effects. Dencine (SN38) requires enzymatic hydrolysis by carboxylesterase, but the conversion rat...
Claims
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IPC IPC(8): A61K9/127A61K47/60A61K47/69A61K47/54A61K31/4745A61P35/00
CPCA61K9/0002A61K9/1271A61K31/4745
Inventor 方韬
Owner 金华市人民医院
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