Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.
Pharmacology Department, Faculty of Pharmacy, New Valley University, Kharga, Egypt.
Drug Deliv. 2023 Dec;30(1):2179127. doi: 10.1080/10717544.2023.2179127.
The brain is a vital organ that is protected from the general circulation and is distinguished by the presence of a relatively impermeable blood brain barrier (BBB). Blood brain barrier prevents the entry of foreign molecules. The current research aims to transport valsartan (Val) across BBB utilizing solid lipid nanoparticles (SLNs) approach to mitigate the adverse effects of stroke. Using a 3-factorial design, we could investigate and optimize the effect of several variables in order to improve brain permeability of valsartan in a target-specific and sustained-release manner, which led to alleviation of ischemia-induced brain damage. The impact of each of the following independent variables was investigated: lipid concentration (% w/v), surfactant concentration (% w/v), and homogenization speed (RPM) on particle size, zeta potential (ZP), entrapment efficiency (EE) %, and cumulative drug release percentage (CDR) %. TEM images revealed a spherical form of the optimized nanoparticles, with particle size (215.76 ± 7.63 nm), PDI (0.311 ± 0.02), ZP (-15.26 ± 0.58 mV), EE (59.45 ± 0.88%), and CDR (87.59 ± 1.67%) for 72 hours. SLNs formulations showed sustained drug release, which could effectively reduce the dose frequency and improve patient compliance. DSC and X-ray emphasize that Val was encapsulated in the amorphous form. The results revealed that the optimized formula successfully delivered Val to the brain through intranasal rout as compared to a pure Val solution and evidenced by the photon imaging and florescence intensity quantification. In a conclusion, the optimized SLN formula (F9) could be a promising therapy for delivering Val to brain, alleviating the negative consequences associated with stroke.
大脑是一个重要的器官，它受到一般循环的保护，并以存在相对不可渗透的血脑屏障（BBB）为特征。血脑屏障阻止外来分子的进入。目前的研究旨在利用固体脂质纳米粒（SLN）方法将缬沙坦（Val）转运穿过血脑屏障，以减轻中风的不良影响。使用 3 因素设计，我们可以研究和优化几个变量的影响，以便以靶向和持续释放的方式改善缬沙坦的脑通透性，从而减轻缺血性脑损伤。研究了以下每个独立变量的影响：脂质浓度（%w/v）、表面活性剂浓度（%w/v）和匀浆速度（RPM）对粒径、Zeta 电位（ZP）、包封效率（EE）%和累积药物释放百分比（CDR）%的影响。TEM 图像显示优化后的纳米粒呈球形，粒径（215.76±7.63nm）、PDI（0.311±0.02）、ZP（-15.26±0.58mV）、EE（59.45±0.88%）和 CDR（87.59±1.67%）在 72 小时内。SLN 制剂显示出持续的药物释放，可有效减少剂量频率并提高患者依从性。DSC 和 X 射线强调 Val 以无定形形式被包裹。结果表明，与纯 Val 溶液相比，优化后的配方通过鼻内途径成功地将 Val 递送到大脑，并通过光子成像和荧光强度定量得到证实。总之，优化的 SLN 配方（F9）可能是一种有前途的治疗方法，可将 Val 递送到大脑，减轻与中风相关的负面后果。
