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首页> 美国卫生研究院文献>International Journal of Pharmaceutics: X >The role interplay between mesoporous silica pore volume and surface area and their effect on drug loading capacity
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The role interplay between mesoporous silica pore volume and surface area and their effect on drug loading capacity

机译：介孔二氧化硅孔体积和表面积之间的相互作用及其对载药量的影响

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class="kwd-title">Keywords: Mesoporous silica, Loading capacity, Differential scanning calorimetry (DSC), Poorly soluble drugs, Amorphous stability, Surface area, Pore volume, Pore diameter class="head no_bottom_margin" id="ab010title">AbstractIn this study, the influence of the mesoporous silica (MS) textural properties (surface area, pore diameter, and pore volume) on drug loading capacity (monomolecular loading capacity and pore filling capacity) was investigated theoretically and experimentally using a thermoanalytical method. The loading capacities of three model drugs (celecoxib, cinnarizine, and paracetamol) were determined in five different MS grades of Sylysia® with identical chemical composition, but varying surface area, pore diameter and pore volume. The experimentally determined loading capacities were compared to theoretical loading capacities, calculated based on the surface area and amorphous density of the drugs, and the surface area and pore volume of the MS. The findings of the study showed that the monomolecular loading capacity generally increased with increasing surface area and decreasing pore volume of the MS. However, the MS grade with the highest surface area did not display the highest monomolecular loading capacity for any of the three drugs. This was probably a result of the decreasing pore diameter necessary to accommodate the increasing surface area of the MS i.e., if the pore is smaller than the drug molecule, the drug cannot access the available surface area. For these systems, the amorphous density of the drug and the pore volume of the MS was used to estimate the theoretical pore filling capacity, which was in good agreement with the experimentally determined loading capacity. In conclusion, this study showed that both the pore volume and surface area of the MS will have an influence on the drug loading capacity and that this can be estimated with good accuracy both theoretically and experimentally.
机译：<！-fig ft0-> <！-fig @ position =“ anchor” mode =文章f4-> <！-fig mode =“ anchred” f5-> <！-fig / graphic | fig / alternatives / graphic mode =“ anchored” m1-> class =“ kwd-title”>关键字：中孔二氧化硅，负载量，差示扫描量热法（DSC），难溶药物，无定形稳定性，表面面积，孔体积，孔直径 class =“ head no_bottom_margin” id =“ ab010title”>摘要在这项研究中，介孔二氧化硅（MS）的结构特性（表面积，孔直径和孔）的影响使用热分析方法从理论上和实验上研究了药物载量（单分子载量和孔填充量）对药物载量的影响。在具有相同化学组成但表面积，孔径和孔体积变化的五个不同MS等级的Sylysia®中测定了三种模型药物（塞来昔布，肉桂利嗪和扑热息痛）的负载量。将实验确定的负载量与理论负载量进行比较，这些负载量是根据药物的表面积和无定形密度以及MS的表面积和孔体积计算得出的。研究结果表明，单分子负载能力通常随表面积的增加和MS的孔体积的减小而增加。但是，表面积最高的MS级对于三种药物中的任何一种均未显示出最高的单分子负载能力。这可能是由于容纳MS表面积增加所必需的孔径减小，即，如果孔径小于药物分子，则药物将无法获得可用的表面积。对于这些系统，使用药物的无定形密度和MS的孔体积来估算理论上的孔填充量，这与实验确定的负载量非常吻合。总之，这项研究表明，MS的孔体积和表面积都会对载药量产生影响，并且无论是从理论上还是从实验上都可以很好地估计载药量。

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