人血清白蛋白与磷酸盐和 Tris 缓冲液的相互作用：对紫杉醇结合和纳米颗粒自组装的影响。
Interactions of human serum albumin with phosphate and Tris buffers: impact on paclitaxel binding and nanoparticles self-assembly.
机构信息
Materials Science Group, Institute of Chemistry, University of Antioquia, Medellín, Colombia.
出版信息
J Microencapsul. 2024 Nov;41(7):564-575. doi: 10.1080/02652048.2024.2389135. Epub 2024 Sep 13.
AIM
To investigate the conformational changes in human serum albumin (HSA) caused by chemical (CD) and thermal denaturation (TD) at pH 7.4 and 9.9, crucial for designing controlled drug delivery systems with paclitaxel (PTX).
METHODS
Experimental and computational methods, including differential scanning calorimetry (DSC), UV-Vis and intrinsic fluorescence spectroscopy, mean diameter, polydispersity index (PDI), ζ-potential, encapsulation efficiency (EE), release and protein docking studies were conducted to study the HSA denaturation and nanoparticles (NPs) preparation.
RESULTS
TD at pH 7.4 produced smaller NPs (287.1 ± 12.9 nm) than CD at pH 7.4 with NPs (584.2 ± 47.7 nm). TD at pH 9.9 exhibited high EE (97.3 ± 0.2%w/w) with rapid PTX release (50% within 1h), whereas at pH 7.4 (96.4 ± 2.1%w/w), release only 40%. ζ-potentials were around -30 mV.
CONCLUSION
Buffer type and pH significantly influence NP properties. TD in PBS at pH 7.4, provided optimal conditions for a stable and efficient drug delivery system.
目的
研究人血清白蛋白（HSA）在 pH 值为 7.4 和 9.9 时，由化学变性（CD）和热变性（TD）引起的构象变化，这对于设计载紫杉醇（PTX）的控释药物输送系统至关重要。
方法
采用实验和计算方法，包括差示扫描量热法（DSC）、紫外-可见和内源荧光光谱、平均粒径、多分散指数（PDI）、ζ-电位、包封效率（EE）、释放和蛋白质对接研究，研究 HSA 变性和纳米颗粒（NPs）的制备。
结果
pH 值为 7.4 时的 TD 产生的 NPs （287.1 ± 12.9nm）比 pH 值为 7.4 时的 CD 小（584.2 ± 47.7nm）。pH 值为 9.9 时的 TD 表现出高 EE（97.3 ± 0.2%w/w）和快速 PTX 释放（50%在 1 小时内），而在 pH 值为 7.4 时（96.4 ± 2.1%w/w），仅释放 40%。ζ-电位约为-30mV。
结论
缓冲液类型和 pH 值显著影响 NPs 的性质。在 pH 值为 7.4 的 PBS 中进行 TD，为稳定高效的药物输送系统提供了最佳条件。
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