Goscianska Joanna, Ejsmont Aleksander, Kubiak Anita, Ludowicz Dominika, Stasiłowicz Anna, Cielecka-Piontek Judyta
Department of Chemical Technology, Faculty of Chemistry, Adam Mickiewicz University in Poznań, Uniwersytetu Poznańskiego 8, 61-614 Poznań, Poland.
Department of Pharmacognosy, Faculty of Pharmacy, Poznań University of Medical Sciences, Święcickiego 4, 61-781 Poznań, Poland.
Materials (Basel). 2021 Apr 24;14(9):2188. doi: 10.3390/ma14092188.
Smart porous carriers with defined structure and physicochemical properties are required for releasing the therapeutic drug with precise control of delivery time and location in the body. Due to their non-toxicity, ordered structure, and chemical and thermal stability, mesoporous carbons can be considered modern carriers for active pharmaceutical ingredients whose effectiveness needs frequent dosing algorithms. Here, the novel benzocaine delivery systems based on ordered mesoporous carbons of the cubic structure were obtained with the use of a hard template method and functionalization with amine groups at 40 °C for 8 h. It has been shown that amine grafting strongly modifies the surface chemistry and textural parameters of carbons. All samples indicated good sorption ability towards benzocaine, with evident improvement following the functionalization with the amine groups. The sorption capacity and drug release kinetics were strongly affected by the porosity of carbon carriers and the surface functional groups. The smallest amount of benzocaine (12%) was released from pristine mesoporous carbon, which could be correlated with strong API-carrier interactions. Faster and more efficient release of the drug was observed in the case of triethylenetetramine modified carbon (62%). All benzocaine delivery platforms based on amine-grafted mesoporous carbons revealed high permeability through the artificial membrane.
为了在精确控制药物在体内的递送时间和位置的情况下释放治疗药物,需要具有明确结构和物理化学性质的智能多孔载体。由于其无毒、有序的结构以及化学和热稳定性,介孔碳可被视为活性药物成分的现代载体,其有效性需要频繁给药算法。在此,通过硬模板法并在40°C下用胺基官能化8小时,获得了基于立方结构有序介孔碳的新型苯佐卡因递送系统。结果表明,胺接枝强烈改变了碳的表面化学和结构参数。所有样品对苯佐卡因均表现出良好的吸附能力,胺基官能化后有明显改善。吸附容量和药物释放动力学受到碳载体孔隙率和表面官能团的强烈影响。原始介孔碳释放的苯佐卡因量最少(约12%),这可能与药物-载体的强相互作用有关。在三乙烯四胺改性碳的情况下,观察到药物释放更快、更有效(约62%)。所有基于胺接枝介孔碳的苯佐卡因递送平台都显示出通过人工膜的高渗透性。