Corazza Elisa, Abruzzo Angela, Giordani Barbara, Cerchiara Teresa, Bigucci Federica, Vitali Beatrice, di Cagno Massimiliano Pio, Luppi Barbara
Department of Pharmacy and Biotechnology, Alma Mater Studiorum, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy.
Department of Pharmacy, Faculty of Mathematics and Natural Sciences, University of Oslo, Sem Sælands vei 3, 0371 Oslo, Norway.
Pharmaceutics. 2022 Feb 26;14(3):524. doi: 10.3390/pharmaceutics14030524.
The inclusion of a chemical permeation enhancer in a dosage form is considered an effective approach to improve absorption across the nasal mucosa. Herein we evaluated the possibility of exploiting biosurfactants (BS) produced by BC9 as innovative natural excipients to improve nasal delivery of hydrocortisone (HC). BC9-BS ability to improve HC solubility and the BS mucoadhesive potential were investigated using the surfactant at a concentration below and above the critical micelle concentration (CMC). In vitro diffusion studies through the biomimetic membrane PermeaPad and the same synthetic barrier functionalized with a mucin layer were assessed to determine BC9-BS absorption enhancing properties in the absence and presence of the mucus layer. Lastly, the diffusion study was performed across the sheep nasal mucosa using BC9-BS at a concentration below the CMC. Results showed that BC9-BS was able to interact with the main component of the nasal mucosa, and that it allowed for a greater solubilization and also permeation of the drug when it was employed at a low concentration. Overall, it seems that BC9-BS could be a promising alternative to chemical surfactants in the nasal drug delivery field.
在剂型中加入化学渗透促进剂被认为是提高药物跨鼻黏膜吸收的有效方法。在此,我们评估了利用BC9产生的生物表面活性剂(BS)作为创新的天然辅料来改善氢化可的松(HC)鼻腔给药的可能性。使用低于和高于临界胶束浓度(CMC)的表面活性剂,研究了BC9-BS提高HC溶解度的能力以及BS的黏膜黏附潜力。通过仿生膜PermeaPad以及用粘蛋白层功能化的相同合成屏障进行体外扩散研究,以确定在不存在和存在黏液层的情况下BC9-BS的吸收增强特性。最后,使用低于CMC浓度的BC9-BS在绵羊鼻黏膜上进行扩散研究。结果表明,BC9-BS能够与鼻黏膜的主要成分相互作用,并且当以低浓度使用时,它能够使药物有更大的溶解度和渗透性。总体而言,在鼻腔给药领域,BC9-BS似乎可能是化学表面活性剂的一个有前景的替代品。