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In vitro anticancer evaluation of micelles containing N-(4-(2-((4-methoxybenzyl)amino)ethyl)phenyl)heptanamide, an analogue of fingolimod

Archives of Pharmacal Research 2020년 43권 10호 p.1046 ~ 1055
윤문섭, 이유진, 박천웅, 홍진태, 백동재, 신대환,
소속 상세정보
윤문섭 ( Yoon Moon-Sup ) - Chungbuk National University College of Pharmacy
이유진 ( Lee Yu-Jin ) - Chungbuk National University College of Pharmacy
박천웅 ( Park Chun-Woong ) - Chungbuk National University College of Pharmacy
홍진태 ( Hong Jin-Tae ) - Chungbuk National University College of Pharmacy
백동재 ( Baek Dong-Jae ) - Mokpo National University College of Pharmacy
신대환 ( Shin Dae-Hwan ) - Chungbuk National University College of Pharmacy

Abstract


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.

키워드

MPH; Micelle; Physicochemical characterization; Drug release; Anti-cancer efficacy

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