Nappini Silvia, Fogli Silvia, Castroflorio Benedetta, Bonini Massimo, Baldelli Bombelli Francesca, Baglioni Piero
Department of Chemistry "U. Schiff" and CSGI, via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy.
J Mater Chem B. 2016 Jan 28;4(4):716-725. doi: 10.1039/c5tb02191j. Epub 2016 Jan 4.
The final fate of nano-scaled drug delivery systems into the body is highly affected by their interaction with proteins in biological fluids (serum, plasma, etc.). Nanocarriers dispersed in biological fluids bear a protein "corona" that covers their surface. Thus, it is extremely important to evaluate the drug release efficiency also in the biological environment where protein-nanocarrier complexes are formed. The purpose of this work is to determine how drug release from lipid vesicle carriers is influenced by the interaction with serum proteins, highlighting the importance to test the effectiveness of such systems in the biological milieu. In particular, this paper describes the magnetically triggered release behaviour of magnetoliposomes (MLs) dispersed both in aqueous physiological buffer and in bovine serum at two different concentrations (10% and 55% v/v) upon exposure to a low-frequency alternating magnetic field (LF-AMF). We studied the release from MLs loaded with two types of magnetic nanoparticles (MNPs): citrate coated FeO and oleic acid coated γ-FeO. The permeability in the above-mentioned fluids was evaluated in terms of the fluorescence self-quenching of carboxyfluorescein (CF) entrapped inside the liposome aqueous pool. The results showed a strong reduction of the release in biological fluids, in particular at high serum concentration. We related this decrease to the formation of protein-liposome complexes that, under LF-AMF exposure, are subjected to destabilization and tend to form aggregates. Our results clearly highlight the importance of testing the release efficiency of self-assembled drug delivery systems in biological fluids, in order to understand their behaviour in the presence of proteins and biomolecules.
纳米级药物递送系统进入体内的最终命运受到其与生物流体(血清、血浆等)中蛋白质相互作用的高度影响。分散在生物流体中的纳米载体表面带有一层蛋白质“冠层”。因此,在形成蛋白质 - 纳米载体复合物的生物环境中评估药物释放效率极其重要。这项工作的目的是确定脂质囊泡载体的药物释放如何受到与血清蛋白相互作用的影响,强调在生物环境中测试此类系统有效性的重要性。特别是,本文描述了磁脂质体(MLs)在两种不同浓度(10%和55% v/v)的牛血清和水性生理缓冲液中,在暴露于低频交变磁场(LF - AMF)时的磁触发释放行为。我们研究了负载两种类型磁性纳米颗粒(MNPs)的MLs的释放情况:柠檬酸盐包覆的FeO和油酸包覆的γ - FeO。通过脂质体水相池中包裹的羧基荧光素(CF)的荧光自猝灭来评估上述流体中的渗透率。结果表明,在生物流体中释放量大幅降低,尤其是在高血清浓度下。我们将这种降低归因于蛋白质 - 脂质体复合物的形成,在LF - AMF暴露下,这些复合物会发生不稳定并倾向于形成聚集体。我们的结果清楚地强调了在生物流体中测试自组装药物递送系统释放效率的重要性,以便了解它们在存在蛋白质和生物分子时的行为。