Formulation and optimization of itraconazole polymeric lipid hybrid nanoparticles (Lipomer) using box behnken design
Formulation and optimization of itraconazole polymeric lipid hybrid nanoparticles (Lipomer) using box behnken design
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DOI：
10.1186/s40199-014-0087-0
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发表时间：
2015-01-21
影响因子：
3.6
通讯作者：
Patel, Ravi
中科院分区：
文献类型：
--
作者：
Gajra, Balaram;Dalwadi, Chintan;Patel, Ravi
背景：本研究的目的是制定并研究3个自变量在优化含有疏水性抗真菌药物伊曲康唑的聚合物脂质杂化纳米粒子（PLHNs）（Lipomer）并改善肠道通透性中的综合影响。方法：通过乳化溶剂蒸发法制备聚合物脂质杂化纳米粒子制剂，并使用3因素3水平Box Behnken统计设计来优化和推导二阶多项式方程并构建等高线图来预测反应。使用可生物降解的聚己内酯、大豆卵磷脂和聚乙烯醇制备PLHN。选择的自变量是脂质与聚合物的比例 (X-1) 表面活性剂浓度 (X-2) 药物浓度 (X-3)。结果：Box-Behnken 设计证明了导出方程和等高线图在预测伊曲康唑 PLHN 制备和优化因变量值中的作用。伊曲康唑 PLHN 具有纳米尺寸 (210 +/- 1.8 nm)，包封效率为 83 +/- 0.6%，负 zeta 电位为 -11.7 mV，并且随着渗透系数 (P-app) 和吸收增强比较高，伊曲康唑的渗透性也增强。结论：PLHN 的可调粒径、表面电荷和良好的包封效率以及持续的药物释放曲线表明它可以该系统有望通过淋巴吸收、支付者贴片的 M 细胞或细胞旁途径改善肠道通透性，从而提高生物利用度，这已通过共聚焦显微镜证实。
Background: The objective of the study was to formulate and to investigate the combined influence of 3 independent variables in the optimization of Polymeric lipid hybrid nanoparticles (PLHNs) (Lipomer) containing hydrophobic antifungal drug Itraconazole and to improve intestinal permeability.Method: The Polymeric lipid hybrid nanoparticle formulation was prepared by the emulsification solvent evaporation method and 3 factor 3 level Box Behnken statistical design was used to optimize and derive a second order polynomial equation and construct contour plots to predict responses. Biodegradable Polycaprolactone, soya lecithin and Poly vinyl alcohol were used to prepare PLHNs. The independent variables selected were lipid to polymer ratio (X-1) Concentration of surfactant (X-2) Concentration of the drug (X-3).Result: The Box-Behnken design demonstrated the role of the derived equation and contour plots in predicting the values of dependent variables for the preparation and optimization of Itraconazole PLHNs. Itraconazole PLHNs revealed nano size (210 +/- 1.8 nm) with an entrapment efficiency of 83 +/- 0.6% and negative zeta potential of -11.7 mV and also enhance the permeability of itraconazole as the permeability coefficient (P-app) and the absorption enhancement ratio was higher.Conclusion: The tunable particle size, surface charge, and favourable encapsulation efficiency with a sustained drug release profile of PLHNs suggesting that it could be promising system envisioned to increase the bioavailability by improving intestinal permeability through lymphatic uptake, M cell of payer's patch or paracellular pathway which was proven by confocal microscopy.