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

Monica Argenziano (1) , Adam Haimhoffer (2) , C Bastiancich (3) , Laszlo Jicsinszky , Fabrizio Caldera (1) , Francesco Trotta (1) , Sara Scutera , Daniela Alotto , Mara Fumagalli , Tiziana Musso (1) , Carlotta Castagnoli , Roberta Cavalli (1)

1 UNITO - Università degli studi di Torino = University of Turin
2 University of Debrecen Egyetem [Debrecen]
3 INP - Institut de neurophysiopathologie

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

Mots clés: cyclodextrins; inclusion complex; nanosponges; controlled release; imiquimod

Domaines: Pharmacologie; Immunothérapie; Dermatologie

Monica Argenziano, Adam Haimhoffer, C Bastiancich, Laszlo Jicsinszky, Fabrizio Caldera, et al.. In Vitro Enhanced Skin Permeation and Retention of Imiquimod Loaded in β-Cyclodextrin Nanosponge Hydrogel. Pharmaceutics, 2019, 11 (3), pp.138. ⟨10.3390/pharmaceutics11030138⟩. ⟨hal-02076798⟩