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首页> 外文期刊>RSC Advances >Intranasal delivery of asenapine loaded nanostructured lipid carriers: formulation, characterization, pharmacokinetic and behavioural assessment
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Intranasal delivery of asenapine loaded nanostructured lipid carriers: formulation, characterization, pharmacokinetic and behavioural assessment

机译：瘦细胞载荷纳米结构脂质载体的鼻内递送：制剂，表征，药代动力学和行为评估

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The aim of the present research work was to develop asenapine (ASM) loaded nanostructured lipid carriers (ANLC) for the delivery of drugs in the brain by an intranasal route to enhance therapeutic efficacy. A quality by design approach was used for development and optimization of ANLC. A total of five independent variables were selected, in which three were compositions and two were process variables, while particle size and entrapment efficiency were selected as response variables. The final optimized batch was evaluated by various in vitro characterizations as well as in vivo brain and plasma pharmacokinetic studies. Finally, the ANLC was assessed for efficacy and safety profiling for upto three weeks by a behavior model viz. catalepsy, induced locomotor and paw test in Charles Foster rats. The observed particle size, entrapment efficiency and zeta potential of ANLC was found to be 167.30 ± 7.52 nm, 83.50 ± 2.48% and ?4.33 ± 1.27 mV, respectively. Surface characterization studies demonstrated a spherical shape with a smooth surface of ANLC which follows the Korsmeyer–Peppas in vitro release kinetic model ( r ~(2) = 0.9911, n = 0.53). A brain pharmacokinetic study indicated a significantly higher ( p < 0.05) peak drug concentration ( C _(max) : 74.13 ± 6.73 ng mL ~(?1) ), area under the drug concentration–time curve (AUC _(0–24 h) : 560.93 ± 27.85 h ng mL ~(?1) ) and mean residence time (MRT: 7.1 ± 0.13 h) of ANLC compared to ASM in the brain via an intranasal route. The results of behaviour studies of ANLC showed a significant decrease in extra-pyramidal side effects with increasing antipsychotic effect after 1–2 week(s) of treatment. These findings demonstrate that nanostructured lipid carriers could be a new promising drug delivery system for intranasal delivery of asenapine in the treatment of schizophrenia.
机译：本研究工作的目的是开发亚宾滨（ASM）负载的纳米结构脂质载体（ANLC），用于通过鼻内途径递送脑中的药物，以提高治疗效果。通过设计方法的质量用于ANLC的开发和优化。选择共有五个独立变量，其中三种是组成，两个是过程变量，而粒度和夹紧效率被选择为响应变量。通过各种体外特征以及体内脑和血浆药代动力学研究评估最终优化批次。最后，通过行为模型viz评估ANLC的疗效和安全性分析。 Charles Foster大鼠的Catalepsy，诱导的机车和爪子测试。发现ANLC的观察到的粒度，夹带效率和ζ电位分别为167.30±7.52nm，分别为83.50±2.48％和α4.33±1.27mV。表面表征研究表明，具有anlc的光滑表面的球形形状，其在体外释放动力学模型中跟随Korsmeyer-Peppas（R〜（2）= 0.9911，n = 0.53）。脑药代动力学研究表明显着较高（P <0.05）峰值药物浓度（C _（最多）：74.13±6.73 ng ml〜（α1）），药物浓度 - 时间曲线下的面积（AUC _（0-24 H）：560.93±27.85h Ng ml〜（α1））和Anlc的平均停留时间（MRT：7.1±0.13h）与通过鼻内路线的大脑中的ASM相比。 ANLC的行为研究结果表明，在治疗后1-2周后的抗精神病效应增加了抗精神病效应显着降低。这些研究结果表明，纳米结构脂质载体可能是一种新的有希望的药物输送系统，用于治疗精神分裂症中的瘦细胞。

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