Design of a nanostructured mucoadhesive system containing curcumin for buccal application: from physicochemical to biological aspects

含姜黄素的用于颊粘膜应用的纳米结构粘膜粘附系统的设计:从物理化学到生物学方面

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作者:Sabrina Barbosa de Souza Ferreira, Gustavo Braga, Évelin Lemos Oliveira, Jéssica Bassi da Silva, Hélen Cássia Rosseto, Lidiane Vizioli de Castro Hoshino, Mauro Luciano Baesso, Wilker Caetano, Craig Murdoch, Helen Elizabeth Colley, Marcos Luciano Bruschi

Abstract

Mucoadhesive nanostructured systems comprising poloxamer 407 and Carbopol 974P® have already demonstrated good mucoadhesion, as well as improved mechanical and rheological properties. Curcumin displays excellent biological activity, mainly in oral squamous cancer; however, its physicochemical characteristics hinder its application. Therefore, the aim of this study was to develop nanostructured formulations containing curcumin for oral cancer therapy. The photophysical interactions between curcumin and the formulations were elucidated by incorporation kinetics and location studies. They revealed that the drug was quickly incorporated and located in the hydrophobic portion of nanometer-sized polymeric micelles. Moreover, the systems displayed plastic behavior with rheopexy characteristics at 37 °C, viscoelastic properties and a gelation temperature of 36 °C, which ensures increased retention after application in the oral cavity. The mucoadhesion results confirmed the previous findings with the nanostructured systems showing a residence time of 20 min in porcine oral mucosa under flow system conditions. Curcumin was released after 8 h and could permeate through the porcine oral mucosa. Cytotoxicity testing revealed that the formulations were selective to cancer cells over healthy cells. Therefore, these systems could improve the physicochemical characteristics of curcumin by providing improved release and permeation, while selectivity targeting cancer cells.

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