In vitro anticancer evaluation of micelles containing N-(4-(2-((4-methoxybenzyl)amino)ethyl)phenyl)heptanamide, an analogue of fingolimod
| Autor: | Jin Tae Hong, Dae Hwan Shin, Yu Jin Lee, Dong Jae Baek, Moon Sup Yoon, Chun-Woong Park |
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| Rok vydání: | 2020 |
| Předmět: |
0301 basic medicine
Stability test Polymers Antineoplastic Agents Micelle 03 medical and health sciences 0302 clinical medicine Drug Stability Cell Line Tumor mental disorders Drug Discovery medicine Humans Particle Size Micelles chemistry.chemical_classification Drug Carriers Aqueous solution Polymeric micelles Fingolimod Hydrochloride Organic Chemistry Water Polymer Combinatorial chemistry Fingolimod In vitro Drug Liberation 030104 developmental biology chemistry Solubility 030220 oncology & carcinogenesis Molecular Medicine Particle size Drug Screening Assays Antitumor human activities medicine.drug |
| Zdroj: | Archives of pharmacal research. 43(10) |
| ISSN: | 1976-3786 |
| Popis: | Fingolimod has been evaluated for use as an anticancer agent. However, many steps are required to synthesize fingolimod because of its intricate structure. A fingolimod analogue, N-(4-(2-((4-methoxybenzyl)amino)ethyl)phenyl)heptanamide (MPH), also has anti-cancer effects and is easier to synthesize but is poorly soluble in water. To compensate for its poor water solubility, MPH-loaded polymeric micelles were prepared by thin film hydration method using various polymers and the physicochemical properties of the MPH-loaded micelles such as particle size, drug-loading (DL, %), and encapsulation efficiency (EE, %) were evaluated. A storage stability test was conducted to select the final formulation and the release profile of the MPH-loaded micelles was confirmed by in vitro release assay. MPH-loaded mPEG-b-PLA micelles were selected for further testing based on their stability and physicochemical properties; they were stable for stable for 14 days at 4 °C and 25 °C and for 7 days at 37 °C. They showed anti-cancer efficacy against both A549 and U87 cancer cells. Encapsulation of MPH in polymeric micelles did not decrease the in vitro cytotoxicity of MPH. The findings of this study lay the groundwork for future formulations that enable the effective and stable delivery of poorly water-soluble agents. |
| Databáze: | OpenAIRE |
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