In Vitro Enhanced Skin Permeation and Retention of Imiquimod Loaded in β-Cyclodextrin Nanosponge Hydrogel

authors

• Argenziano Monica
• Haimhoffer Adam
• Bastiancich C
• Jicsinszky Laszlo
• Caldera Fabrizio
• Trotta Francesco
• Scutera Sara
• Alotto Daniela
• Fumagalli Mara
• Musso Tiziana
• Castagnoli Carlotta
• Cavalli Roberta

keywords

• Cyclodextrins
• Inclusion complex
• Nanosponges
• Controlled release
• Imiquimod

abstract

Imiquimod (IMQ) is an immune response modifier clinically used for the treatment of various topical diseases. However, its poor aqueous solubility and skin penetration capability make the topical delivery of IMQ a challenging task. This work aims at developing a nanomedicine-based topical formulation, carrying IMQ to control the scarring process for the treatment of aberrant wounds. For this purpose, IMQ was loaded in β-cyclodextrin-based nanosponges and dispersed in a hydrogel suitable for dermal application. The formulation was characterized in vitro and compared with IMQ inclusion complexes, with (2-hydroxy)propyl β-cyclodextrin(HPβCD) and carboxymethyl β-cyclodextrin (CMβCD) showing enhanced penetration properties. The hydrogel containing IMQ-loaded nanosponges could act as a drug reservoir and guarantee the sustained release of IMQ through the skin. A greater inhibitory effect on fibroblast proliferation was observed for IMQ loaded in nanosponges compared to the other formulations

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