The poor water solubility of a significant number of active pharmaceutical ingredients (API) remains one of the main challenges in the drug development process, causing low bioavailability and therapeutic failure of drug candidates. Curcumin is a well-known Biopharmaceutics Classification System (BCS) class IV drug, characterized by lipophilicity and low permeability, which hampers topical bioavailability. Given these premises, the aim of this work was the design and the development of curcumin nanocrystals and their incorporation into natural inorganic hydrogels for topical application. Curcumin nanocrystals were manufactured by the wet ball milling technique and then loaded in clay-based hydrogels. Bentonite and/or palygorskite were selected as the inorganic gelling agents. Curcumin nanocrystal-loaded hydrogels were manufactured by means of a homogenization process and characterized with respect to their chemico-physical properties, in vitro release, antioxidant activity and skin permeation. The results highlighted that the presence of bentonite provided an increase of curcumin skin penetration and simultaneously allowed its radical scavenging properties, due to the desirable rheological characteristics, which should guarantee the necessary contact time of the gel with the skin.
Nanomedicine manipulates materials at atomic, molecular, and supramolecular scale, with at least one dimension within the nanometer range, for biomedical applications. The resulting nanoparticles have been consistently shown beneficial effects for antifungal drugs delivery, overcoming the problems of low bioavailability and high toxicity of these drugs. Due to their unique features, namely the small mean particle size, nanoparticles contribute to the enhanced drug absorption and uptake by the target cells, potentiating the therapeutic drug effect. The topical route is desirable due to the adverse effects arising from oral administration. This review provides a comprehensive analysis of the use of nano compounds for the current treatment of topical fungal infections. A special emphasis is given to the employment of lipid nanoparticles, due to their recognized efficacy, versatility and biocompatibility, attracting the major attention as novel topical nanocompounds used for the administration of antifungal drugs.
The use of Solid Lipid Nanoparticles (SLN) has become a very popular approach in the development of innovative pharmaceutical drug delivery systems. The first step is the assessment the lipids' suitability. This paper is focused on the physicochemical characterization of lipids, namely cetyl alcohol and cetearyl alcohol, for the production of SLN. The bulk lipids were analyzed by Differential Scanning Calorimetry (DSC) and Wide Angle X-ray Diffraction (WAXD) without any treatment, after tempering the raw materials (bulk lipid) for 1 hour at 80 °C, and after their spray-drying process. Hydrophilic-Lipophilic Balance (HLB) values were determined using a combination of surfactants (polysorbate 20 and trioleate sorbitan) for the production of the hot o/w emulsion. Results of DSC and WAXD showed that after the thermal stress applied to the bulk lipids, both the melting point and the intensity of the refractogram peaks have decreased. Cetyl alcohol and cetearyl alcohol crystallized in more unstable polymorphic forms, which anticipate the suitability of these lipids for the production of SLN. The best HLB values obtained for the produced emulsions were 15.5, 16.0, and 16.7, combining accepted surfactants. The results showed that both cetearyl alcohol and cetyl alcohol are adequate lipids for the development of stable SLN.
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