Nazarkina Zhanna K, Savostyanova Tatyana A, Chelobanov Boris P, Romanova Irina V, Simonov Pavel A, Kvon Ren I, Karpenko Andrey A, Laktionov Pavel P
Institute of Chemical Biology and Fundamental Medicine, Siberian Branch, Russian Academy of Sciences, 630090 Novosibirsk, Russia.
Department of Natural Sciences, Novosibirsk State University, 630090 Novosibirsk, Russia.
Pharmaceutics. 2022 Jun 30;14(7):1386. doi: 10.3390/pharmaceutics14071386.
Activated carbon (AC) could be potentially useful as a drug carrier in fiber polymer scaffolds destined for prolonged drug delivery. To be introduced, AC must be ground into smaller-sized particles to be introduced in scaffolds, as most biocompatible scaffolds consist of fibers with a diameter of less than 1 µm. In this study, the adsorption of sirolimus (SRL) from phosphate-buffered saline (PBS) solution and blood plasma (BP) onto AC of AX-21 type, as well as the release of SRL from AC depending on its fragmentation, were studied. Two-stage grinding of the AC, first with a ball mill, and then with a bead mill, was performed. Grinding with a bead mill was performed either in water or in polyvinylpyrrolidone to prevent aggregation of AC particles. Dynamic light scattering and scanning electron microscopy (SEM) demonstrated that the size of the particles obtained after grinding with a ball mill was 100-10,000 nm, and after grinding with a bead mill, 100-300 nm. Adsorption in PBS was significantly higher than in BP for all fractions, and depended on SRL concentration. The fraction obtained after grinding with a ball mill showed maximal SRL adsorption, both in PBS and BP, and slow SRL release, in comparison with other fractions. The 100-300 nm AC fractions were able to adsorb and completely release SRL into BP, in contrast to other fractions, which strongly bound a significant amount of SRL. The data obtained are to be used for controlled SRL delivery, and thus in the modification of drug delivery in biological media.
活性炭（AC）在用于长期药物递送的纤维聚合物支架中可能是一种潜在有用的药物载体。要将AC引入支架，必须将其研磨成更小尺寸的颗粒，因为大多数生物相容性支架由直径小于1 µm的纤维组成。在本研究中，研究了西罗莫司（SRL）从磷酸盐缓冲盐水（PBS）溶液和血浆（BP）吸附到AX - 21型AC上的情况，以及SRL从AC根据其破碎程度的释放情况。对AC进行了两阶段研磨，首先用球磨机，然后用珠磨机。用珠磨机研磨在水中或聚乙烯吡咯烷酮中进行，以防止AC颗粒聚集。动态光散射和扫描电子显微镜（SEM）表明，用球磨机研磨后获得的颗粒尺寸为100 - 10,000 nm，用珠磨机研磨后为100 - 300 nm。所有级分在PBS中的吸附均显著高于在BP中的吸附，且取决于SRL浓度。与其他级分相比，用球磨机研磨后获得的级分在PBS和BP中均表现出最大的SRL吸附以及缓慢的SRL释放。与其他强烈结合大量SRL的级分相比，100 - 300 nm的AC级分能够吸附SRL并将其完全释放到BP中。所获得的数据将用于控制SRL的递送，从而用于生物介质中药物递送的修饰。
