Vasile Aurelia, Ignat Maria, Zaltariov Mirela Fernanda, Sacarescu Liviu, Stoleriu Iulian, Draganescu Dan, Dumitras Mihai, Ochiuz Lacramioara
Acta Chim Slov. 2018 Mar;65(1):97-107.
The present study reports the first time use of MCM-41 mesoporous silica as highly efficient carrier for bexarotene - an antineoplastic agent specific for cutaneous T-cell lymphoma treatment. Bexarotene is highly toxic and poor-water soluble, having low bioavailability in the conventional pharmaceutical forms. Comparative uptake of bexarotene on amino-functionalized silica host at various functionalization degrees is discussed in details taking into account all structural features, of matrix as well as properties of the drug molecules. The obtained results proved a successful bexarotene loading on amino-functionalized MCM-41 silica. The bexarotene molecules are adsorbed on the active centers in non-crystalline state proving the major role of the silica amino-functionalization for the drug solubility and bioavailability enhancing. In vitro dissolution tests showed a prolonged release of bexarotene during 12 h, reaching 50% release of loaded active molecules. The prolonged release has been demonstrated to be a result of the presence of aminopropyl groups on the silica pore walls.
本研究首次报道了使用MCM-41介孔二氧化硅作为高效载体负载贝沙罗汀，贝沙罗汀是一种用于治疗皮肤T细胞淋巴瘤的抗肿瘤药物。贝沙罗汀毒性高且水溶性差，在传统药物剂型中的生物利用度低。考虑到基质的所有结构特征以及药物分子的性质，详细讨论了贝沙罗汀在不同功能化程度的氨基功能化二氧化硅载体上的比较摄取情况。所得结果证明贝沙罗汀成功负载于氨基功能化的MCM-41二氧化硅上。贝沙罗汀分子以非晶态吸附在活性中心上，证明了二氧化硅氨基功能化对提高药物溶解度和生物利用度的主要作用。体外溶出试验表明，贝沙罗汀在12小时内持续释放，负载的活性分子释放率达到50%。已证明这种持续释放是由于二氧化硅孔壁上存在氨丙基。
