Rinaldi Federica, Hanieh Patrizia N, Chan Lik King Nicholas, Angeloni Livia, Passeri Daniele, Rossi Marco, Wang Julie Tzu-Wen, Imbriano Anna, Carafa Maria, Marianecci Carlotta
Center for Life Nano Science@Sapienza, Istituto Italiano di Tecnologia (ITT), Viale Regina Elena 291, 00161 Rome, Italy.
Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, P.zzle A. Moro 5, 00185 Roma, Italy.
Pharmaceutics. 2018 Mar 22;10(2):38. doi: 10.3390/pharmaceutics10020038.
The aim of this in vitro study is to prepare and characterize drug free and pentamidine loaded chitosan glutamate coated niosomes for intranasal drug delivery to reach the brain through intranasal delivery. Mucoadhesive properties and stability testing in various environments were evaluated to examine the potential of these formulations to be effective drug delivery vehicles for intranasal delivery to the brain. Samples were prepared using thin film hydration method. Changes in size and ζ-potential of coated and uncoated niosomes with and without loading of pentamidine in various conditions were assessed by dynamic light scattering (DLS), while size and morphology were also studied by atomic force microscopy (AFM). Bilayer properties and mucoadhesive behavior were investigated by fluorescence studies and DLS analyses, respectively. Changes in vesicle size and ζ-potential values were shown after addition of chitosan glutamate to niosomes, and when in contact with mucin solution. In particular, interactions with mucin were observed in both drug free and pentamidine loaded niosomes regardless of the presence of the coating. The characteristics of the proposed systems, such as pentamidine entrapment and mucin interaction, show promising results to deliver pentamidine or other possible drugs to the brain via nasal administration.
本体外研究的目的是制备并表征用于鼻内给药以通过鼻内递送到达脑部的无药物和载有喷他脒的壳聚糖谷氨酸包衣脂质体。评估了在各种环境中的粘膜粘附特性和稳定性测试，以检查这些制剂作为鼻内递送至脑部的有效药物递送载体的潜力。使用薄膜水化法制备样品。通过动态光散射（DLS）评估在各种条件下有和没有负载喷他脒的包衣和未包衣脂质体的尺寸和ζ电位的变化，同时还通过原子力显微镜（AFM）研究尺寸和形态。分别通过荧光研究和DLS分析研究双层性质和粘膜粘附行为。在向脂质体中加入壳聚糖谷氨酸后以及与粘蛋白溶液接触时，显示出囊泡大小和ζ电位值的变化。特别是，无论是否存在包衣，在无药物和载有喷他脒的脂质体中均观察到与粘蛋白的相互作用。所提出的系统的特性，如喷他脒包封和与粘蛋白的相互作用，显示出通过鼻腔给药将喷他脒或其他可能的药物递送至脑部的有希望的结果。
