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首页> 外文期刊>Journal of drug delivery science and technology >The impact of bioceramic nanocarriers on the intranasal delivery of zaleplon nanoscale powder through new adsorption techniques: Improvement in bioavailability and hypnotic effect
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The impact of bioceramic nanocarriers on the intranasal delivery of zaleplon nanoscale powder through new adsorption techniques: Improvement in bioavailability and hypnotic effect

机译：生物陶瓷纳米载体对通过新吸附技术的唑仑纳米级粉末的影响：改善生物利用度和催眠作用

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The current work presents a new approach for nanosizing zaleplon (ZPN) powder aiming for enhancing its dissolution, bioavailability and hypnotic efficacy. Particles are adsorbed onto nanocarriers thereby acquiring their respective nanosizes. Nanoscale zaleplon was prepared by adsorption onto hydroxyapatite (ZHP) or halloysite (ZHA), respectively. Rotary evaporation enabled arrangement of particles onto outer surfaces of nanocarriers, with 100% loading capacity. Dissolution completed within 30?min, with a half-life of 7?min. The particle size was 645?nm for ZHP and 391?nm for ZHA. Drug particles were present at outer surfaces of nanocarriers as deduced from the DSC, XRDP, nitrogen sorption-desorption and as observed in transmission electron microscope (TEM) images. ZHP showed enhanced penetration through cattle nasal mucosa. Permeability coefficient rose from 0.085?cm/h for the untreated ZPN to 0.2?cm/h for the optimized powder with no alteration in the configuration of epithelial tissues. Significant impairment of locomotor activity accompanied by muscle relaxation and decreased coordination was noticed upon intranasal instillation of ZHP to rats. The relative bioavailability of intranasal ZPN in rabbits increased 2.4 times compared to oral Sleep aid? tablets. Therefore, the new adsorption technique enabled the successful preparation of nanoscale powder of zaleplon with enhanced dissolution and bioavailability.
机译：目前的工作呈现了一种新方法，用于旨在提高其溶解，生物利用度和催眠效果的纳米氧化甘醇（ZPN）粉末。将颗粒吸附在纳米载体上，从而获取它们各自的纳米型。通过吸附到羟基磷灰石（ZhP）或Holloysite（Zha）上制备纳米级Zaleplon。旋转蒸发使颗粒排列到纳米载体的外表面上，100％负载能力。溶解在30？分钟内完成，半衰期为7？分钟。 ZHP的粒度为645Ω·NM和ZHA的391.NM。从DSC，XRDP，氮吸附 - 解吸中推导的纳米载波的外表面积存在于纳米载体的外表面上，并且如在透射电子显微镜（TEM）图像中观察到的。 ZHP通过牛鼻腔粘膜显示出渗透率。对于未处理的ZPN，渗透系数从0.085Ωcm/ h升至0.2Ωcm/ h，对于优化的粉末，没有改变上皮组织的构型。肌肉松弛伴随的运动活性和协调减少的重大损害被注意到ZHP对大鼠的鼻内滴注。与口腔睡眠援助相比，兔鼻内ZPN的相对生物利用度增加了2.4倍？平板电脑。因此，新的吸附技术使得Zaleplon纳米级粉末的成功制备具有增强的溶解和生物利用度。

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