Remote Loading: The Missing Piece for Achieving High Drug Payload and Rapid Release in Polymeric Microbubbles.
Remote Loading: The Missing Piece for Achieving High Drug Payload and Rapid Release in Polymeric Microbubbles.
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DOI：
10.3390/pharmaceutics15112550
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发表时间：
2023-10-28
期刊：
影响因子：
5.4
通讯作者：
Sirsi SR
中科院分区：
文献类型：
--
作者：
Rastegar G;Salman MM;Sirsi SR
近年来，利用载药微泡进行靶向药物递送，特别是在癌症治疗中，已经得到了广泛的研究。然而，由于微气泡的表面积，其承载能力受到限制。通常，药物分子被装载在壳上或壳内，或者装载药物的纳米颗粒被包裹在微泡表面。为了解决这个重要的限制，我们引入了一种新的方法。我们首次采用跨膜硫酸铵和pH梯度将多柔比星以结晶形式装载在聚合物微胶囊的核心中。随后，我们通过升华微胶囊的液体核心来创建远程加载微泡（rlmb）。远程加载的微胶囊与物理加载的微胶囊相比，药物有效载荷增加了18倍。此外，我们研究了暴露于超声场时rlmb的药物释放。120 s后，负载的阿霉素释放率高达82.4±5.5%，显示了远程负载微泡按需释放药物的卓越能力。这项研究首次报道了这种微泡能够使药物从核心快速释放。这种创新技术在提高药物装载能力和推进靶向给药方面具有很大的前景。
The use of drug-loaded microbubbles for targeted drug delivery, particularly in cancer treatment, has been extensively studied in recent years. However, the loading capacity of microbubbles has been limited due to their surface area. Typically, drug molecules are loaded on or within the shell, or drug-loaded nanoparticles are coated on the surfaces of microbubbles. To address this significant limitation, we have introduced a novel approach. For the first time, we employed a transmembrane ammonium sulfate and pH gradient to load doxorubicin in a crystallized form in the core of polymeric microcapsules. Subsequently, we created remotely loaded microbubbles (RLMBs) through the sublimation of the liquid core of the microcapsules. Remotely loaded microcapsules exhibited an 18-fold increase in drug payload compared with physically loaded microcapsules. Furthermore, we investigated the drug release of RLMBs when exposed to an ultrasound field. After 120 s, an impressive 82.4 ± 5.5% of the loaded doxorubicin was released, demonstrating the remarkable capability of remotely loaded microbubbles for on-demand drug release. This study is the first to report such microbubbles that enable rapid drug release from the core. This innovative technique holds great promise in enhancing drug loading capacity and advancing targeted drug delivery.
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影响因子：
50.5
作者：
O'Brien, MER;Wigler, N;Tendler, C
通讯作者：
Tendler, C
影响因子：
5.4
作者：
Honari A;Merillat DA;Bellary A;Ghaderi M;Sirsi SR
通讯作者：
Sirsi SR
影响因子：
5.4
作者：
Navarro-Becerra JA;Borden MA
通讯作者：
Borden MA
DOI：
10.1016/j.jconrel.2010.07.115
发表时间：
2010-11-20
期刊：
Journal of controlled release : official journal of the Controlled Release Society
影响因子：
--
作者：
Klibanov AL;Shevchenko TI;Raju BI;Seip R;Chin CT
通讯作者：
Chin CT
影响因子：
3.9
作者：
Jamburidze, Akaki;Huerre, Axel;Garbin, Valeria
通讯作者：
Garbin, Valeria