A fluorous biphase drug delivery system triggered by low frequency ultrasound: controlled release from perfluorous discoidal porous silicon particles.

A fluorous biphase drug delivery system triggered by low frequency ultrasound: controlled release from perfluorous discoidal porous silicon particles.
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低频超声触发的氟双相药物递送系统:全氟盘状多孔硅颗粒的控释

DOI:
10.1039/d0na00324g
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发表时间:
2020-08-11
期刊:
影响因子:
4.7
通讯作者:
--
中科院分区:
材料科学3区
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--
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传统的给药系统存在载药效率不高、生物旁路不畅、释药不可控等问题,这些都是提高许多疾病治疗水平的巨大障碍。本文首次提出了低频超声触发的氟两相给药系统(FB-DDS)的概念验证,该系统通过氟-氟相互作用促进治疗药物在纳米载体中的掺入和稳定,并通过外部来源控制药物的释放,从而将非特异性毒性降至最低,提高了治疗效果。FB-DDS是由单分散的盘状多孔硅颗粒(PSP)构建的,并用1H,1H,2H,2H-全氟十二烷基三甲氧基硅烷(FAS17)官能化,通过氟-氟相互作用负载全氟戊烷(PFP)和氟化药物。模型化合物包括含氟标记的荧光素和含氟抗生素环丙沙星,证明了该给药系统。氟之间的相互作用促进了模型分子在氟碳涂层载体上的装载,而通过LFUS快速蒸发PFP促进了模型分子的排出。在体外实验中,载氟环丙沙星载体对铜绿假单胞菌生物被膜具有良好的抗菌活性。总体而言,这种创新的刺激响应型氟两相药物输送系统将是一个有希望的实际应用候选者,并鼓励进一步研究药物输送和控制释放策略。为实现含氟药物的高效给药,研制了低频超声触发的氟两相给药系统(FB-DDS)。
Conventional drug delivery systems face unsatisfactory loading efficiency, poor biological bypass, and uncontrollable release, which are great barriers for improving the treatment of many diseases. Herein, a proof-of-concept of a fluorous biphase drug delivery system (FB-DDS) trigged by low frequency ultrasound (LFUS) is proposed for the first time, where promoted incorporation and stabilization of therapeutic agents in nanocarriers was achieved through fluorine–fluorine interactions, and the encapsulated drugs were controllably released by external sources, resulting in minimized nonspecific toxicity and enhanced therapeutic efficacy. The FB-DDS was constructed from monodisperse, discoidal porous silicon particles (PSP) and was functionalized with 1H,1H,2H,2H-perfluorodecyltrimethoxysilane (FAS17) for loading perfluoropentane (PFP) and fluorinated drugs through fluorine–fluorine interactions. This delivery system was demonstrated by utilizing model compounds including a fluorous-tagged fluorescein and a fluorine containing antibiotic ciprofloxacin. Loading of the model molecules into fluorocarbon-coated carriers was facilitated by fluorous interactions, whereas ejection of the model molecules was promoted by applying LFUS to rapidly evaporate PFP. In the in vitro test, these carriers loaded with fluorine containing ciprofloxacin exhibited excellent antimicrobial activity against Pseudomonas aeruginosa biofilm formation. Overall, this innovative stimulus-responsive fluorous biphase drug delivery system will be a promising candidate for practical applications as well as encouraging further investigation of drug delivery and controlled release strategies. A fluorous biphase drug delivery system (FB-DDS) trigged by low frequency ultrasound (LFUS) was developed for efficient delivery of fluorine containing pharmaceuticals.
DOI: 10.1007/s11095-010-0277-5
发表时间: 2010-12
影响因子: 3.7
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DOI: 10.1016/j.actbio.2013.03.027
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影响因子: 9.7
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