PDF(Pubmed)
Abstract：
UNASSIGNED: The commercial docetaxel (DTX) formulation causes severe side effects due to polysorbate 80 and ethanol. Novel surfactant-free nanoparticle (NP) systems are needed to improve bioavailability and reduce side effects. However, controlling the particle size and stability of NPs and improving the batch-to-batch variation are the major challenges.
UNASSIGNED: DTX-loaded bovine serum albumin nanoparticles (DTX-BSA-NPs) were prepared by a novel thermal-driven self-assembly/microfluidic technology. Single-factor analysis and orthogonal test were conducted to obtain the optimal formulation of DTX-BSA-NPs in terms of particle size, encapsulation efficiency (EE), and drug loading (DL). The effects of oil/water flow rate and pump pressure on the particle size, EE, and DL were investigated to optimize the preparation process of DTX-BSA-NPs. The drug release, physicochemical properties, stability, and pharmacokinetics of NPs were evaluated.
UNASSIGNED: The optimized DTX-BSA-NPs were uniform, with a particle size of 118.30 nm, EE of 89.04%, and DL of 8.27%. They showed a sustained release of 70% over 96 hours and an increased stability. There were some interactions between the drug and excipients in DTX-BSA-NPs. The half-life, mean residence time, and area under the curve (AUC) of DTX-BSA-NPs increased, but plasma clearance decreased when compared with DTX.
UNASSIGNED: The thermal-driven self-assembly/microfluidic combination method effectively produces BSA-based NPs that improve the bioavailability and stability of DTX, offering a promising alternative to traditional formulations.
UNASSIGNED: DTX-loaded bovine serum albumin nanoparticles (DTX-BSA-NPs) were prepared by a novel thermal-driven self-assembly/microfluidic technology. Single-factor analysis and orthogonal test were conducted to obtain the optimal formulation of DTX-BSA-NPs in terms of particle size, encapsulation efficiency (EE), and drug loading (DL). The effects of oil/water flow rate and pump pressure on the particle size, EE, and DL were investigated to optimize the preparation process of DTX-BSA-NPs. The drug release, physicochemical properties, stability, and pharmacokinetics of NPs were evaluated.
UNASSIGNED: The optimized DTX-BSA-NPs were uniform, with a particle size of 118.30 nm, EE of 89.04%, and DL of 8.27%. They showed a sustained release of 70% over 96 hours and an increased stability. There were some interactions between the drug and excipients in DTX-BSA-NPs. The half-life, mean residence time, and area under the curve (AUC) of DTX-BSA-NPs increased, but plasma clearance decreased when compared with DTX.
UNASSIGNED: The thermal-driven self-assembly/microfluidic combination method effectively produces BSA-based NPs that improve the bioavailability and stability of DTX, offering a promising alternative to traditional formulations.
摘要：
商业多西他赛(DTX)制剂由于聚山梨酯80和乙醇而引起严重的副作用。需要新型的不含表面活性剂的纳米颗粒(NP)系统来提高生物利用度并减少副作用。然而,控制NPs的粒度和稳定性以及改善批次间的变化是主要挑战。
■通过新型热驱动自组装/微流体技术制备了负载DTX的牛血清白蛋白纳米颗粒（DTX-BSA-NP）。通过单因素分析和正交试验,得到DTX-BSA-NP的最佳配方,封装效率(EE)，和载药量（DL）。油/水流量和泵压力对颗粒尺寸的影响，EE,对DTX-BSA-NP的制备工艺进行了优化。药物释放，物理化学性质，稳定性,并对NPs的药代动力学进行了评价。
■优化的DTX-BSA-NP是均匀的，粒径为118.30nm，EE为89.04%，DL为8.27%。它们在96小时内表现出70%的持续释放和增加的稳定性。DTX-BSA-NP中的药物和赋形剂之间存在一些相互作用。半衰期,平均停留时间，DTX-BSA-NP的曲线下面积（AUC）增加，但与DTX相比，血浆清除率下降。
■热驱动自组装/微流体组合方法有效地产生了基于BSA的NPs，该NPs提高了DTX的生物利用度和稳定性，为传统配方提供了一个有希望的替代品。
■通过新型热驱动自组装/微流体技术制备了负载DTX的牛血清白蛋白纳米颗粒（DTX-BSA-NP）。通过单因素分析和正交试验,得到DTX-BSA-NP的最佳配方,封装效率(EE)，和载药量（DL）。油/水流量和泵压力对颗粒尺寸的影响，EE,对DTX-BSA-NP的制备工艺进行了优化。药物释放，物理化学性质，稳定性,并对NPs的药代动力学进行了评价。
■优化的DTX-BSA-NP是均匀的，粒径为118.30nm，EE为89.04%，DL为8.27%。它们在96小时内表现出70%的持续释放和增加的稳定性。DTX-BSA-NP中的药物和赋形剂之间存在一些相互作用。半衰期,平均停留时间，DTX-BSA-NP的曲线下面积（AUC）增加，但与DTX相比，血浆清除率下降。
■热驱动自组装/微流体组合方法有效地产生了基于BSA的NPs，该NPs提高了DTX的生物利用度和稳定性，为传统配方提供了一个有希望的替代品。
