Effective strategies for small molecule encapsulation: preparation of nanosystems for potential biomedical and food applications

Nanosystems capable of delivering active ingredients to biological compartments arouse interest for biomedical applications, as well as the nanoencapsulation of functional molecules is an effective strategy to increase their bioavailability and to mask any unpleasant flavours in food field. Here, two main general approaches for small molecule encapsulation are described: 1) A supramolecular nanoaggregate of a calix[4]arene derivative was designed for delivering active ingredients to biological targets. The micellar nanoaggregate showed intrinsic antibacterial properties and ability to encapsulate bioactives and photoactivable drugs. For instance, curcumin-loaded nanoaggregate in the form of micellar solution [1] or nanohydrogel [2] exhibited significant efficacy in the treatment of a model of LPS-induced uveitis [1] and imiquimod-induced psoriasis in mouse [3], respectively. 2) Lipid-core nanocapsules based on a biocompatible and biodegradable polymer were prepared for encapsulating bioactive ingredients to use as potential additives for functional foods [4], and preservatives against food-borne bacteria [5]. The nanosuspensions displayed a monomodal distribution, low polydispersity index, good encapsulation efficiency and stability over time. Some properties of curcumin-loaded nanocapsules including the behaviour of the nanoformulation in a simulated digestive environment and, preliminary tests of addition to food matrix were investigated. Acknowledgement: This work was supported by the projects: PON R&C 02_00355_2964193 (MIUR, Rome); PO FESR 2014/2020 - Azione 1.1.5 n. 082120090383. References [1]. G. Granata, I. Paterniti, C. Geraci, F. Cunsolo, E. Esposito, M. Cordaro, A. R. Blanco, S. Cuzzocrea, G.M.L. Consoli. Mol. Pharm., 14(5), 1610, 2017. [2]. G. Granata, S. Petralia, G. Forte, S. Conoci, G.M.L. Consoli. Mater. Sci. Eng. C., 111, 110842, 2020. [3]. A. Filippone, G.M.L. Consoli, G. Granata, G. Casili, M. Lanza, A. Ardizzone, S. Cuzzocrea, E. Esposito I. Paterniti. Int. J. Mol. Sci., 21(14), 5053, 2020. [4]. G. Granata, G.M.L. Consoli, R. Lo Nigro, C. Geraci. Food Chem., 245, 551, 2018. [5]. G. Granata, S. Stracquadanio, M. Leonardi, E., Napoli, G.M.L. Consoli, V. Cafiso, S. Stefani C. Geraci. Food Chem., 269, 286, 2018.