Liposomal formulation of alpha-tocopheryl maleamide: In vitro and in vivo toxicological profile and anticancer effect against spontaneous breast carcinomas in mice

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00027162%3A_____%2F09%3A%230000491" target="_blank" >RIV/00027162:_____/09:#0000491 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/86652036:_____/09:00340455

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Liposomal formulation of alpha-tocopheryl maleamide: In vitro and in vivo toxicological profile and anticancer effect against spontaneous breast carcinomas in mice

Popis výsledku v původním jazyce

The vitamin E analogue alpha-tocopheryl succinate (a-TOS) is an efficient anti-cancer drug. Improved efficacy was achieved through the synthesis of alpha-tocopheryl maleamide (a-TAM), an esterase-resistant analogue of alpha -tocopheryl maleate. In vitrotests demonstrated significantly higher cytotoxicity of a-TAM towards cancer cells compared to a-TOS and other analogues prone to esterase-catalyzed hydrolysis.We developed lyophilized liposomal formulations of both a-TOS and a-TAM to solve the problem with solubility of free drugs. Liposomal formulation of a-TAM demonstrated anti-cancer activity at levels 10-fold lower than those of a-TOS. Remarkably, neither acute toxicity nor immunotoxicity was detected in vivo after application of liposomal a-TAM, which significantly reduced the growth of cancer cells in hollow fiber implants. Moreover, liposomal formulation of a-TAM and a-TOS each prevented the growth of tumours in transgenic FVB/N c-neu mice bearing spontaneous breast carcinomas.

Název v anglickém jazyce

Liposomal formulation of alpha-tocopheryl maleamide: In vitro and in vivo toxicological profile and anticancer effect against spontaneous breast carcinomas in mice

Popis výsledku anglicky

The vitamin E analogue alpha-tocopheryl succinate (a-TOS) is an efficient anti-cancer drug. Improved efficacy was achieved through the synthesis of alpha-tocopheryl maleamide (a-TAM), an esterase-resistant analogue of alpha -tocopheryl maleate. In vitrotests demonstrated significantly higher cytotoxicity of a-TAM towards cancer cells compared to a-TOS and other analogues prone to esterase-catalyzed hydrolysis.We developed lyophilized liposomal formulations of both a-TOS and a-TAM to solve the problem with solubility of free drugs. Liposomal formulation of a-TAM demonstrated anti-cancer activity at levels 10-fold lower than those of a-TOS. Remarkably, neither acute toxicity nor immunotoxicity was detected in vivo after application of liposomal a-TAM, which significantly reduced the growth of cancer cells in hollow fiber implants. Moreover, liposomal formulation of a-TAM and a-TOS each prevented the growth of tumours in transgenic FVB/N c-neu mice bearing spontaneous breast carcinomas.

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>Z - Vyzkumny zamer (s odkazem do CEZ)

Rok uplatnění

2009

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Toxicology and Applied Pharmacology

ISSN

0041-008X

e-ISSN

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Svazek periodika

237

Číslo periodika v rámci svazku

3

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

9

Strana od-do

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Kód UT WoS článku

000266689800001

EID výsledku v databázi Scopus

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