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首页> 美国卫生研究院文献>BioMed Research International >Systematic Approach for the Formulation and Optimization of Solid Lipid Nanoparticles of Efavirenz by High Pressure Homogenization Using Design of Experiments for Brain Targeting and Enhanced Bioavailability
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Systematic Approach for the Formulation and Optimization of Solid Lipid Nanoparticles of Efavirenz by High Pressure Homogenization Using Design of Experiments for Brain Targeting and Enhanced Bioavailability

机译：利用高压均质法设计和优化脑靶向性和生物利用度的实验设计依法韦仑固体脂质纳米颗粒的系统方法

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摘要

The nonnucleoside reverse transcriptase inhibitors, used for the treatment of HIV infections, are reported to have low bioavailability pertaining to high first-pass metabolism, high protein binding, and enzymatic metabolism. They also show low permeability across blood brain barrier. The CNS is reported to be the most important HIV reservoir site. In the present study, solid lipid nanoparticles of efavirenz were prepared with the objective of providing increased permeability and protection of drug due to biocompatible lipidic content and nanoscale size and thus developing formulation having potential for enhanced bioavailability and brain targeting. Solid lipid nanoparticles were prepared by high pressure homogenization technique using a systematic approach of design of experiments (DoE) and evaluated for particle size, polydispersity index, zeta potential, and entrapment efficiency. Particles of average size 108.5 nm having PDI of 0.172 with 64.9% entrapment efficiency were produced. Zeta potential was found to be −21.2 mV and the formulation was found stable. The in-vivo pharmacokinetic studies revealed increased concentration of the drug in brain, as desired, when administered through intranasal route indicating its potential for an attempt towards complete eradication of HIV and cure of HIV-infected patients.
机译：据报道，用于治疗HIV感染的非核苷类逆转录酶抑制剂与高首过代谢，高蛋白结合和酶促代谢相关的生物利用度较低。它们还显示出穿过血脑屏障的低渗透性。据报道，中枢神经系统是最重要的艾滋病毒储存地点。在本研究中，依非韦伦的固体脂质纳米颗粒的制备旨在由于生物相容性脂质含量和纳米级尺寸而提供增加的渗透性和药物保护，从而开发具有增强生物利用度和脑靶向性的潜力的制剂。使用系统化的实验设计方法（DoE），通过高压均质技术制备固体脂质纳米颗粒，并评估其粒径，多分散指数，ζ电位和包封效率。制备平均粒径为108.5μm，PDI为0.172，包封率为64.9％的颗粒。发现ζ电位为-21.2 mV，并且发现该制剂稳定。体内药代动力学研究表明，通过鼻内途径给药时，该药物在大脑中的浓度增加了，这表明它有可能试图彻底根除HIV和治愈HIV感染的患者。

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