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重组蜘蛛丝颗粒作为药物传递载体。

Recombinant spider silk particles as drug delivery vehicles.

机构信息

Lehrstuhl Biomaterialien, Universitätsstraße 30, Universität Bayreuth, D-95440 Bayreuth, Germany.

出版信息

Biomaterials. 2011 Mar;32(8):2233-40. doi: 10.1016/j.biomaterials.2010.11.060. Epub 2010 Dec 24.

Abstract

Spider silk has been in the focus of research mainly due to the superior mechanical characteristics of silk fibers. However, it has been previously shown that spider silk proteins can also adopt other morphologies such as submicroparticles. This study examines the applicability of such particles as drug carriers. Particle characterization revealed that particles made of the engineered spider silk protein eADF4(C16) are colloidally stable in solution. Here, it is shown that small molecules with positive net-charge can diffuse into the negatively charged spider silk protein matrix driven by electrostatic interactions. The loading efficiencies correlate with the distribution coefficient (logD) of small molecules of weak alkaline nature. Interestingly, constant release rates can be realized for a period of two weeks at physiological conditions in vitro, with accelerated release rates within acidic environments. Enzymatic degradation studies of eADF4(C16) particles indicated that the silk proteins degrade slowly and the particles decrease in size. Along with their all-aqueous and easy preparation, drug loaded eADF4(C16) particles provide a high potential for diverse applications in which controlled release from biodegradable carriers is desired.

摘要

蜘蛛丝一直是研究的焦点,主要是因为丝纤维具有优越的机械特性。然而,此前已经表明,蜘蛛丝蛋白也可以采用其他形态,如亚微米颗粒。本研究探讨了这些颗粒作为药物载体的适用性。颗粒特性研究表明,由工程化蜘蛛丝蛋白 eADF4(C16)制成的颗粒在溶液中具有胶体稳定性。这里显示,带正净电荷的小分子可以通过静电相互作用扩散到带负电荷的蜘蛛丝蛋白基质中。负载效率与弱碱性小分子的分布系数(logD)相关。有趣的是,在体外生理条件下可以实现两周的恒定释放速率,而在酸性环境中则会加速释放。对 eADF4(C16)颗粒的酶降解研究表明,丝蛋白降解缓慢,颗粒减小。eADF4(C16)载药颗粒具有全水相和易于制备的特点,为在需要可生物降解载体控制释放的各种应用中提供了很高的潜力。

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