College of Pharmacy, Qiqihar Medical University, Qiqihar 161006, China.
Molecules. 2019 May 7;24(9):1770. doi: 10.3390/molecules24091770.
Mesoporous carriers have been extensively applied to improve the dissolution velocity and bioavailability of insoluble drugs. The goal of this work was to compare the drug-loading efficiency (LE) and drug-dissolution properties of mesoporous silica nanoparticles (MSN) and mesoporous carbon nanoparticles (MCN) as drug vectors oral delivery of water-insoluble drugs. For this purpose, MSN and MCN with similar particle size, surface area, and mesoporous diameter were prepared to precisely evaluate the effects of different textures on the drug-loading and dissolution behavior of insoluble drugs. Carvedilol (CAR), a Bio-pharmaceutic Classification System (BCS) class II drug, was loaded in the MSN and MCN by the solvent adsorption method and solvent evaporation method with different carrier-drug ratios. The carboxylated MCN (MCN-COOH) had a higher LE for CAR than MSN for both the two loading methods due to the strong adsorption effect and π-π stacking force with CAR. In vitro drug dissolution study showed that both MSN and MCN-COOH could improve the dissolution rate of CAR compared with the micronized CAR. In comparison to MSN, MCN-COOH displayed a slightly slower dissolution profile, which may be ascribed to the strong interaction between MCN-COOH and CAR. Observation of cell cytotoxicity and gastrointestinal mucosa irritation demonstrated the good biocompatibility of both MSN and MCN-COOH. The present study encourages further research of different carriers to determine their potential application in oral administration.
介孔载体已广泛应用于提高难溶性药物的溶解速度和生物利用度。本工作旨在比较介孔硅纳米粒子（MSN）和介孔碳纳米粒子（MCN）作为药物载体口服递送难溶性药物时的载药效率（LE）和药物溶出性能。为此，制备了具有相似粒径、比表面积和介孔直径的 MSN 和 MCN，以精确评估不同结构对难溶性药物载药和溶出行为的影响。卡维地洛（CAR）是生物药剂学分类系统（BCS）II 类药物，采用溶剂吸附法和溶剂蒸发法，以不同的载体-药物比将其载入 MSN 和 MCN。由于与 CAR 具有较强的吸附作用和π-π堆积力，羧基化 MCN（MCN-COOH）对 CAR 的 LE 高于 MSN，这两种加载方法均如此。体外药物溶出研究表明，与微米化 CAR 相比，MSN 和 MCN-COOH 均可提高 CAR 的溶解速率。与 MSN 相比，MCN-COOH 的溶解曲线稍慢，这可能归因于 MCN-COOH 与 CAR 之间的强相互作用。细胞毒性和胃肠道黏膜刺激性观察表明 MSN 和 MCN-COOH 均具有良好的生物相容性。本研究鼓励进一步研究不同载体，以确定它们在口服给药中的潜在应用。
