Mışraklı Merve, Rizzo Sebastiano Antonio, Bordano Valentina, Bozza Annalisa, Ferraris Luca, Marini Elisabetta, Muntoni Elisabetta, Capucchio Maria Teresa, Scomparin Anna, Battaglia Luigi
Faculty of Pharmacy, Ege University, Erzene Street, Ankara Avenue, No 172/98, 35040 Izmir, Türkiye.
Department of Drug Science and Technology, University of Turin, Via Pietro Giuria 9, 10125 Turin, Italy.
Materials (Basel). 2024 Oct 11;17(20):4959. doi: 10.3390/ma17204959.
Nasal delivery is a non-invasive strategy for effective drug delivery. Nevertheless, in order to promote drug uptake by the nasal mucosa, it is fundamental to increase its residence time in the administration site. To this aim, nano-sized drug delivery systems are widely exploited. Within this context, the commercially available nanoemulsion for parenteral nutrition is a biocompatible, safe and clinically approved vehicle for drug delivery. Furthermore, the nanodroplet surface can be modified via a well-established protocol to graft Concavalin A, a lectin capable of improving the mucosal adhesion, by binding to the α-mannose and α-glucose residues of the mucosal glycocalyx. The obtained targeted formulation is able to induce haemagglutination, as opposite to non-modified nanoemulsion. Furthermore, the ConA grafting maintains the physicochemical properties of the nanodroplets (size~230 nm, Z < -35 mV) and does not interfere with the loading of the Rose Bengal fluorescent probe. Fluorescently labelled ConA grafted nanodroplets showed enhanced permeation and accumulation in ex vivo bovine nasal mucosa. This study is a proof of concept that Concanavalin A can be used to decorate the surface of nanodroplets, acting as a permeation promoter.
鼻腔给药是一种用于有效药物递送的非侵入性策略。然而，为了促进药物被鼻黏膜吸收，延长其在给药部位的停留时间至关重要。为实现这一目标，人们广泛采用纳米级药物递送系统。在此背景下，市售的用于胃肠外营养的纳米乳剂是一种生物相容性良好、安全且经临床批准的药物递送载体。此外，可通过成熟的方案对纳米液滴表面进行修饰，以接枝伴刀豆球蛋白A，这是一种能够通过与黏膜糖萼的α-甘露糖和α-葡萄糖残基结合来改善黏膜黏附的凝集素。与未修饰的纳米乳剂不同，所得的靶向制剂能够诱导血细胞凝集。此外，伴刀豆球蛋白A接枝保持了纳米液滴的物理化学性质（尺寸约230 nm，Z < -35 mV），并且不干扰玫瑰红荧光探针的负载。荧光标记的伴刀豆球蛋白A接枝纳米液滴在离体牛鼻黏膜中显示出增强的渗透和蓄积。这项研究证明了伴刀豆球蛋白A可用于修饰纳米液滴表面，起到渗透促进剂的作用。
