Nanoformulations for dermal delivery of imiquimod: The race of "soft" against "hard".

Autor: Petrová E; Department of Organic Technology, University of Chemistry and Technology Prague, Technická 5, Prague, Czech Republic., Chvíla S; Department of Chemical Engineering, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague 6, Czech Republic., Balouch M; Department of Chemical Engineering, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague 6, Czech Republic., Štěpánek F; Department of Chemical Engineering, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague 6, Czech Republic., Zbytovská J; Department of Organic Technology, University of Chemistry and Technology Prague, Technická 5, Prague, Czech Republic. Electronic address: jarmila.zbytovska@vscht.cz.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2023 Dec 15; Vol. 648, pp. 123577. Date of Electronic Publication: 2023 Nov 04.
DOI: 10.1016/j.ijpharm.2023.123577
Abstrakt: Imiquimod (IMQ) is an immunostimulating agent used in the treatment of basal cell carcinoma and actinic keratosis. Due to its low solubility and poor skin bioavailability, the dermal formulation of IMQ remains challenging. In analogy to tyre compounds used in Formula 1 racing, we compare four types of nanosystems belonging to three groups: (i) "hard" nanoparticles in the form of IMQ nanocrystals, (ii) "intermediate" nanoparticles in the form of liposomes and lipid nanocapsules, and (iii) "soft" nanoparticles in the form of a nanoemulsion based on oleic acid. The nanoemulsion and nanocrystals were able to incorporate the highest amount of IMQ (at least 2 wt%) compared to liposomes (0.03 wt%) and lipid nanocapsules (0.08 wt%). Regarding size, liposomes, and lipid nanocapsules were rather small (around 40 nm) whereas nanocrystals and nanoemulsion were larger (around 200 nm). All developed nanoformulations showed high efficiency to deliver IMQ into the skin tissue without undesirable subsequent permeation through the skin to acceptor. Especially, the 2 wt% IMQ nanoemulsion accumulated 129 μg/g IMQ in the skin, compared to 34 μg/g of a 5 wt% commercial cream. The effects of the respective nanoparticulate systems were discussed with respect to their possible diffusion kinetics (Brownian motion vs. settling) in the aqueous phase.
Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2023 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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