Abstract
Rutin is a natural compound with several pharmacological effects. Among these, antioxidant activity is one of the best known. Despite its numerous benefits, its topical application is severely limited by its physicochemical properties. For this reason, the use of suitable systems could be necessary to improve its delivery through skin, thus enhancing its pharmacological effects. In this regard, the aim of this work is to optimize the ethosomal dispersion modifying both lipid and ethanol concentrations and encapsulating different amounts of rutin. Characterization studies performed on the realized systems highlighted their great stability properties. Studies of encapsulation efficiency and loading degree allowed us to identify a better formulation (EE% 67.5 ± 5.2%, DL% 27 ± 1.7%), which was used for further analyses. The data recorded from in vitro studies showed that the encapsulation into these nanosystems allowed us to overcome the photosensitivity limitation of rutin. Indeed, a markable photostability of the loaded formulation was recorded, compared with that reported from the free rutin solution. The efficacy of the nanosystems was finally evaluated both in vitro on keratinocyte cells and in vivo on human healthy volunteers. The results confirmed the potentiality of rutin-loaded nanosystems for skin disease, mainly related to their anti-inflammatory and antioxidant effects.
Highlights
From ancient times, the application of natural products was widespread as therapy for several pathological conditions [1] such as skin inflammation, erythematous rashes, skin photosensitivity, urticaria, psoriasis, etc
The results obtained from this research work confirmed the suitability of ethosomes as topical drug delivery systems for a pharmacologically active natural compound, namely rutin
Observing the effect of rutin applied as a hydroalcoholic solution, we can note that, during the first 30 min and in the first hour of experiment, the induced inflammation was maintained at significantly higher values (p < 0.05) with respect to the same sites treated with NaCl
Summary
The application of natural products was widespread as therapy for several pathological conditions [1] such as skin inflammation, erythematous rashes, skin photosensitivity, urticaria, psoriasis, etc. Ethosomes® have represented one of the main biocompatible nanosystems that better cross the skin layers, providing an effective and safe drug delivery [4] This need arises from the limitations of conventional nanosystems such as liposomes because of their lack of deformability, leading to a massive release of cargo in the upper SCE [5]. Ethosomes’ composition and in particular the presence of ethanol in the phospholipid bilayer as a penetration enhancer to increase its deformable capability permit the deeper layers to be reached both in an occlusive and in a non-occlusive manner [6] Since they were conceived [7], these nanocarriers were performed for the topical delivery of several compounds, both hydrophilic and lipophilic ones [8]. Godin et al demonstrated that ethosomes can exploit the intercellular lipid domains between corneocytes in the SCE, allowing for drug penetration [9]
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