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基于碳多孔纳米胶囊载体的高载药释放系统。布洛芬案例研究。

High load drug release systems based on carbon porous nanocapsule carriers. Ibuprofen case study.

机构信息

Department of Chemical Engineering, Universidad Autónoma de Madrid, 28049 Madrid, Spain.

出版信息

J Mater Chem B. 2020 Jun 24;8(24):5293-5304. doi: 10.1039/d0tb00329h.

Abstract

This work shows the application of carbon nanocapsules as carriers for sodium ibuprofen release. Hard templating was used to prepare spherical carbon nanocapsules (mean diameter and thick shell of 690 and 70 nm, respectively), exhibiting both micro and mesoporosity. For comparison purposes, a microporous commercial activated carbon and a home-made mesoporous CMK-3 were also studied. All carbons showed similar drug uptake, although microporous commercial carbon and nanocapsules showed higher uptake at low equilibrium concentration due to higher adsorption potential in micropores. Higher and faster release of sodium ibuprofen was observed for carbon nanocapsules at pH 1.8 and 7.4 for a starting load ca. 250 mg g-1. Subsequent loading of carbon nanocapsules by successive evaporation cycles led to a remarkable load of ca. 6010 mg g-1 thanks to sodium ibuprofen filling the internal void volume. In spite of the very high load a fast release was observed at pH 7.4, reaching a release of ca. 100% of the initial sodium ibuprofen load. However, a much slower and lower release was observed at pH 1.8. Thus, the system developed has interesting features for oral drug administration thanks to low toxicity of porous carbon, low release in gastric medium and important release in intestinal medium.

摘要

本工作展示了碳纳米胶囊作为布洛芬钠释放载体的应用。硬模板法被用于制备具有球形形貌的碳纳米胶囊(平均直径和厚壳分别为 690nm 和 70nm,同时具有微孔和介孔)。为了进行对比,还研究了商业微孔活性炭和自制介孔 CMK-3。所有碳均表现出相似的药物摄取量,尽管商业微孔碳和纳米胶囊在低平衡浓度下表现出更高的摄取量,因为微孔中具有更高的吸附势能。在 pH 值为 1.8 和 7.4 时,碳纳米胶囊对布洛芬钠的释放更高且更快,起始负载约为 250mg g-1。通过连续蒸发循环对碳纳米胶囊进行后续负载,由于布洛芬钠填充了内部空隙体积,负载量高达约 6010mg g-1。尽管负载量非常高,但在 pH 值为 7.4 时仍观察到快速释放,达到初始布洛芬钠负载量的约 100%。然而,在 pH 值为 1.8 时,释放速度较慢且较低。因此,由于多孔碳的低毒性、在胃介质中的低释放和在肠介质中的重要释放,所开发的系统具有用于口服药物给药的有趣特征。

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