Division of Pharmaceutical Sciences, University of Missouri-Kansas City School of Pharmacy, Kansas City, Missouri 64110-2499, USA.
AAPS PharmSciTech. 2009;10(3):1040-7. doi: 10.1208/s12249-009-9296-0. Epub 2009 Aug 18.
The purpose of this study is to investigate the combined influence of process parameters (independent variables) such as homogenization speed (X(1)), duration (X(2)), and temperature (X(3)) during the preparation of dacarbazine-loaded cubosomes. Box-Behnken design was used to rationalize the influence of these three factors on two responses, namely particle size (Y(1)) and encapsulation efficiency (Y(2)). Independent and dependent variables were analyzed with multiple regressions to establish a full-model second-order polynomial equation. F value was calculated to confirm the omission of insignificant parameters or interactions of parameters from the analysis to derive a reduced-model polynomial equation to predict the Y(1) and Y(2) of dacarbazine-loaded cubosomes. Pareto charts were also obtained to show the effects of X(1), X(2), and X(3) on Y(1) and Y(2). For Y(1), there was a model validated for more accurate prediction of response parameter by performing checkpoint analysis. The optimization process and Pareto charts were obtained automatically and they predicted the levels of independent parameters X(1), X(2), and X(3) (0.889794, 0.11886, and 0.56201, respectively) and minimized Y(1). The optimal process parameters (homogenization's speed = approximately 24,000 rpm, duration = 5.5 min, and temperature = 76 degrees C) led to the production of cubosomes with 85.6 nm in size and 16.7% in encapsulation efficiency. The Box-Behnken design proved to be a useful tool in the preparation and optimization of dacarbazine-loaded cubosomes. For encapsulation efficiency (Y(2)), further studies are needed to enhance the result and improve the model for such water-soluble drug encapsulation in cubosomes.
本研究的目的是探讨在制备载达卡巴嗪立方脂质体过程中,匀浆速度(X(1))、时间(X(2))和温度(X(3))等工艺参数(自变量)的综合影响。采用 Box-Behnken 设计来合理化这三个因素对两个响应值,即粒径(Y(1))和包封效率(Y(2))的影响。通过多元回归分析独立和因变量,建立全模型二阶多项式方程。计算 F 值以确认从分析中忽略不显著的参数或参数之间的相互作用,得出简化模型多项式方程,以预测载达卡巴嗪立方脂质体的 Y(1)和 Y(2)。还获得了 Pareto 图表,以显示 X(1)、X(2)和 X(3)对 Y(1)和 Y(2)的影响。对于 Y(1),通过执行检查点分析,为响应参数的更准确预测建立了模型验证。优化过程和 Pareto 图表是自动获得的,它们预测了独立参数 X(1)、X(2)和 X(3)的水平(分别为 0.889794、0.11886 和 0.56201),并最小化了 Y(1)。最佳工艺参数(匀浆速度约为 24,000 rpm,时间为 5.5 分钟,温度为 76 摄氏度)导致粒径为 85.6nm、包封效率为 16.7%的立方脂质体的生成。Box-Behnken 设计证明是制备和优化载达卡巴嗪立方脂质体的有用工具。对于包封效率(Y(2)),需要进一步研究以提高结果并改进此类水溶性药物在立方脂质体中的包封模型。