Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen 2100, Denmark.
Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen 2100, Denmark.
Eur J Pharm Sci. 2022 Jul 1;174:106204. doi: 10.1016/j.ejps.2022.106204. Epub 2022 May 10.
Polyelectrolyte complexes (PECs) have been used as the matrix of solid foams for drug delivery. This study aimed at investigating the effect of graphene oxide (GO) and the composition of excipients in chitosan/alginate-based buccal foams on the clotrimazole release and antifungal activities. The investigation has been focused on the interactions of the drug with excipients in the foams, and the changes of ionization degree upon exposure to various media are discussed. The solid foams were prepared by mixing the excipients and clotrimazole via probe sonication, followed by a freeze-drying method. The pH values of the formulations were measured during the foam preparation process to estimate the ionization degree of clotrimazole and the other excipients. The foam matrix was the PECs between the cationic chitosan and anionic alginate. The mechanical strength of clotrimazole-loaded foams was lower than that of drug-free foams due to the positively charged clotrimazole interacting with the anionic alginate and interfering the PECs between chitosan and alginate. Addition of GO in the clotrimazole-loaded matrix made the foams mechanically stronger and contributed to a faster release of clotrimazole from the buccal foams by disrupting the electrostatic interactions between alginate and clotrimazole. However, addition of 1 wt% GO in the formulations didn't affect the antifungal activity of clotrimazole-loaded foams significantly. A lower amount GO in the formulation may be required for enhancing the antifungal effect, which should be further investigated in future.
聚电解质复合物（PECs）已被用作药物输送的固体泡沫基质。本研究旨在研究氧化石墨烯（GO）和壳聚糖/海藻酸钠基口腔泡沫中赋形剂的组成对克霉唑释放和抗真菌活性的影响。研究集中在药物与泡沫中赋形剂的相互作用上，并讨论了暴露于不同介质时电离度的变化。通过探针超声混合赋形剂和克霉唑来制备固体泡沫，然后进行冷冻干燥法。在泡沫制备过程中测量配方的 pH 值，以估计克霉唑和其他赋形剂的电离度。泡沫基质是阳离子壳聚糖和阴离子海藻酸钠之间的 PECs。由于带正电荷的克霉唑与阴离子海藻酸钠相互作用并干扰壳聚糖和海藻酸钠之间的 PECs，因此载药泡沫的机械强度低于无载药泡沫。GO 的加入使载药基质中的泡沫具有更高的机械强度，并通过破坏海藻酸钠和克霉唑之间的静电相互作用，促进克霉唑从口腔泡沫中的更快释放。然而，在配方中添加 1wt%的 GO 对载药泡沫的抗真菌活性没有显著影响。可能需要在配方中加入更少的 GO 来增强抗真菌效果，这将在未来进一步研究。
