Abstract
Poor aqueous solubility of active compounds is a major issue in today’s drug delivery. In this study the smartFilm-technology was exploited to improve the dermal penetration efficacy of a poorly soluble active compound (curcumin). Results were compared to the dermal penetration efficacy of curcumin from curcumin bulk suspensions and nanocrystals, respectively. The smartFilms enabled an effective dermal and transdermal penetration of curcumin, whereas curcumin bulk- and nanosuspensions were less efficient when the curcumin content was similar to the curcumin content in the smartFilms. Interestingly, it was found that increasing numbers of curcumin particles within the suspensions increased the passive dermal penetration of curcumin. The effect is caused by an aqueous meniscus that is created between particle and skin if the dispersion medium evaporates. The connecting liquid meniscus causes a local swelling of the stratum corneum and maintains a high local concentration gradient between drug particles and skin. Thus, leading to a high local passive dermal penetration of curcumin. The findings suggest a new dermal penetration mechanism for active compounds from nano-particulate drug delivery systems, which can be the base for the development of topical drug products with improved penetration efficacy in the future.
Highlights
Curcumin-loaded smartFilms were obtained upon the loading of paper cut outs with ethanolic curcumin solution (Figure 1—right)
Results demonstrated the loading of the curcumin into the cellulose matrix in amorphous state which resulted in an increased dissolution rate and increased kinetic solubility when compared to curcumin bulk material
The first phase is the wetting of the cellulose fibers with a slow release of curcumin
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. The advantage of the smartFilm technology for improved oral delivery was already shown in previous studies and recent studies could further demonstrate that the smartFilms can be transferred into tablets made from paper Those tablets made from paper fulfil all criteria for conventionally produced tablets according to the European Pharmacopeia, e.g., hardness, friability, disintegration time. Oral application of smartFilms is a highly promising approach for improved drug delivery of poorly soluble actives [10,11,12]. To exploit the pharmacological potential of curcumin, drug delivery systems that increase oral and its dermal penetration efficacy are of high interest In this light, smartFilms loaded with curcumin seem to be a very promising formulation approach for an improved dermal penetration efficacy of curcumin. In order to evaluate the penetration efficacy of curcumin from the smartFilms realistically, curcumin bulk suspensions and curcumin nanocrystals with an approx. mean particle size of 200 nm were produced and used as benchmark controls
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