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Hydroxyurea-Loaded Albumin Nanoparticles: Preparation Characterization and In Vitro Studies

机译:羟基脲负载白蛋白纳米粒子:制备表征和体外研究。

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摘要

Human serum albumin nanoparticles (HSA-NPs) have been widely used as drug delivery systems. In most cases, HSA-NPs are formed by the method of desolvation in the presence of glutaraldehyde as a crosslinking agent. In the present study, we showed the possibility of crosslinking human serum albumin (HSA) molecules with natural agents, urea, and cysteine at the nanoparticle level under mild conditions (at room temperature of 20–25 °C). Optimal concentrations of the interacting components (HSA, urea, and cysteine) were found to produce nanoparticles with optimal physico-chemical parameters (particle size, polydispersity, zeta potential, yield, etc.) for application as drug carriers. We used hydroxyurea (HU), a simple organic compound currently used as a cancer chemotherapeutic agent. The results indicated sizes of 196 ± 5 nm and 288 ± 10 nm with a surface charge of −22 ± 3.4 mV and −17.4 ± 0.5 mV for HSA-NPs (20 mg/mL of HSA, 0.01 mg/mL of cysteine, and 10 mg/mL of urea) and HSA–HU-NPs (2 mg/mL of HU), respectively. The yield of the HSA–HU-NPs was ~93% with an encapsulation efficiency of ~77%. Thus, the particles created (immobilized with HU) were stable over time and able to prolong the effect of the drug.
机译:人血清白蛋白纳米颗粒(HSA-NPs)已被广泛用作药物递送系统。在大多数情况下,在戊二醛作为交联剂的情况下,通过去溶剂化方法形成HSA-NP。在本研究中,我们显示了在温和条件下(室温20–25°C)将人血清白蛋白(HSA)分子与天然制剂,尿素和半胱氨酸交联的可能性。已发现相互作用成分(HSA,尿素和半胱氨酸)的最佳浓度可产生具有最佳物理化学参数(粒径,多分散性,ζ电位,产率等)的纳米颗粒,用作药物载体。我们使用了羟基脲(HU),一种目前用作癌症化学治疗剂的简单有机化合物。结果表明,对于HSA-NPs(20 mg / mL的HSA,0.01 mg / mL的半胱氨酸和50mg的半胱氨酸,其表面电荷分别为196±5 nm和288±10 nm,表面电荷为−22±3.4 mV和−17.4±0.5 mV。 10 mg / mL尿素)和HSA–HU-NPs(2 mg / mL的HU)。 HSA–HU-NPs的产率约为93%,封装效率约为77%。因此,产生的颗粒(用HU固定)随时间推移是稳定的,并能够延长药物的作用。

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