含胡椒碱的多西他赛负载纳米粒子的设计与表征

Priyanka Saharan, Shyo Paraksh Saharan
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引用次数: 0

摘要

研究目的本研究的主要目的是开发一种含有草药生物强化剂的新型制剂,以提高一种难溶于水的抗癌药物的生物利用度,并克服其半衰期短的局限性。研究方法在乳化溶剂蒸发过程中使用 Eudragit RLPO 作为聚合物,生成负载多西他赛的生物增强剂(胡椒碱)纳米粒子,并评估其参数。结果表明研究表明,将多西他赛与草药生物增强剂(胡椒碱)封装在纳米颗粒系统中,可有效增强其体外释放谱。粒径范围(142 至 189 nm)是纳米颗粒给药增强细胞吸收和提高生物利用度的最佳范围,所有批次的药物释放量都很显著,24 小时内的释放率为 83.69% 至 96.44%。这表明纳米颗粒具有可控的释放特性,这对于长期维持治疗药物水平是非常理想的。释放数据符合菲克扩散定律,表明药物释放机制是扩散控制的。樋口模型对释放动力学进行了最佳描述,表明释放速率与时间的平方根成正比,这是药物释放受聚合物基质扩散控制的系统的典型特征。结论研究表明,将多西他赛与草药生物增强剂(胡椒碱)封装在纳米粒子系统中,可有效增强其体外释放谱。粒径范围(142 至 189 nm)是纳米颗粒给药的最佳粒径,根据樋口模型得出的释放动力学证实了控释机制。胡椒碱的用量越高,药物释放率越高,这一重大发现凸显了利用生物增强剂提高多西他赛等水溶性较差药物的生物利用度的潜力。这些令人鼓舞的体外研究结果为进一步开展体内药代动力学和细胞毒性研究铺平了道路,以便全面评估这种新型制剂的治疗潜力和生物利用度的提高。
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Designing and Characterization of Docetaxel Loaded Nanoparticles with Piperine
Objective: The main objective of this research was to develop a novel formulation with an herbal bioenhancer to boost the bioavailability of an anticancer drug that was poorly soluble in water and overcome its limitations of short half-life. Methods: Eudragit RLPO was used as a polymer in an emulsification solvent evaporation process to generate Docetaxel loaded bioenhancer (Piperine) nanoparticles and to evaluate its parameters. Results: The study demonstrated that encapsulating Docetaxel with herbal bioenhancers (Piperine) in a nanoparticle system effectively enhanced its in vitro release profile. The particle size range (142 to 189 nm) is optimal range for enhanced cellular uptake and improved bioavailability for nanoparticle drug delivery, and the drug release from all batches was significant, with a release percentage ranging from 83.69% to 96.44% over 24 hours. This indicates a controlled release profile, which is desirable for maintaining therapeutic drug levels over an extended period. The release data adhered to Fick's law of diffusion, suggesting that the drug release mechanism is diffusion-controlled. Higuchi's model best described the release kinetics, indicating that the release rate is proportional to the square root of time, which is typical for systems where the drug release is controlled by diffusion through a polymer matrix. Conclusion: The study demonstrated that encapsulating Docetaxel with herbal bioenhancers (Piperine) in a nanoparticle system effectively enhanced its in vitro release profile. The particle size range (142 to 189 nm) is optimal for nanoparticle drug delivery, and the release kinetics following Higuchi’s model confirm the controlled release mechanism. The significant finding that higher amounts of Piperine enhance drug release rates underscores the potential of using bioenhancers to improve the bioavailability of poorly water-soluble drugs like Docetaxel. These promising in vitro results pave the way for further in vivo pharmacokinetic and cytotoxicity studies to fully assess the therapeutic potential and bioavailability improvements provided by this novel formulation.
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