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The objective of present research work was to formulate and evaluate topical gel containing tretinoin–cyclodextrin (CD) binary complex loaded into nanostructured lipid carriers (NLCs). Use of cyclodextrin and nanolipid carrier together in a system produced a synergistic effect by increasing the drug release and skin permeation, thus improving the o...
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... However, although Curcumin solubility increased greatly compared with the raw polyphenol, it was not as high as desired. In addition, EpiβCD has already been tested for topical use, resulting in an enhanced pharmacological efficacy [13]. For these reasons, epichlorohydrinβ-cyclodextrin (EpiβCD) was chosen. ...
... EpiβCD is known for its ability to enhance drug permeation, as Gidwani et al., (2017) stated. In their studies, when tretinoin was combined with this polymeric CD and lipid nanostructures, the amount of drug permeated almost doubled [13]. In some permeation assays, raw Curcumin have demonstrated an extremely low permeation [5,52]. ...
Curcumin (Cur) is an anti-inflammatory polyphenol that can be complexed with polymeric cyclodextrin (CD) to improve solubility and bioavailability. The aim of the present work was to prepare a CurCD hydrogel to treat inflammatory skin conditions. Epichlorohydrin-β-CD (EpiβCD) was used as polymeric CD. To characterize the binary system, solid-state and in-solution studies were performed. Afterwards, an experimental design was performed to optimize the hydrogel system. Finally, the CurEpiβCD hydrogel system was tested for anti-inflammatory activity using a HaCat psoriasis cell model. Co-grinded Cur/EpiβCD binary system showed a strong interaction and Curcumin solubility was much improved. Its combination with Pluronic® F-127/hyaluronate hydrogel demonstrated an improvement in release rate and Curcumin permeation. After testing its anti-inflammatory activity, the system showed a significant reduction in IL-6 levels. Hydrogel-containing CurEpiβCD complex is a great alternative to treat topical inflammatory diseases.
... To the best of our knowledge, there is still a lack of validated, simple, and suitable methods to assay TTN in different porcine skin layers for penetration/retention studies from dermatological formulations, such as creams and gels. Most studies have not evaluated TTN penetration in different skin layers, separately [24,25,26], or they used other skin models [27,28]. Porcine is the most used skin model for penetration/permeation studies due to its similarity to human skin in terms of its anatomical and physiological characteristics [29,30]. ...
A liquid chromatography (LC) method for the quantification of tretinoin (TTN) in different matrices (adhesive tape, cotton and porcine skin layers, stratum corneum, viable epidermis, and dermis) was validated and applied in in vitro porcine skin penetration/retention studies. This study proposes, for the first time, a method for assaying TTN in separated porcine skin layers (stratum corneum, viable epidermis, and dermis). The skin studies were carried out using tape stripping and cutaneous retention techniques. The procedures for the extraction of TTN from dermatological formulations (creams and gels) and biological and non-biological matrices used with the tape stripping and retention techniques were also evaluated. The LC method consisted of a mobile phase composed of a mixture of methanol, water, and glacial acetic acid (85:15:1, v/v); a C18 column used as the stationary phase; a flow rate of 1.0 mL min-1; an injection volume of 100 μL; and TTN detection at 342 nm. The method was linear in the range of 0.05-15.00 μg mL-1 (r = 0.9999), and it was precise and accurate. The limit of detection (LOD) and limit of quantification (LOQ) were 0.0165 μg mL-1 and 0.0495 μg mL-1, respectively. TTN was extracted from different matrices, showing good precision [relative standard deviation (RSD) of <5%] and accuracy (89.4-113.9%). This method was successfully applied in the evaluation of TTN skin retention/permeation from dermatological formulations (cream and gel). A higher penetration of TTN through the skin was achieved with the gel rather than the cream, showing the influence of the dosage form. Therefore, the developed method can easily be applied in porcine skin penetration/retention studies of dermatological formulations containing TTN, and it is able to discriminate the behaviours of the different formulations.
This study was aimed to evaluate the impact of water-soluble β-cyclodextrin polymer (β-CDP), as a nanocarrier, on the therapeutic efficacy of the commercial doxorubicin (DOX). The β-CDP was synthesized by cross-linking of β-CD using epichlorohydrin. The chemical structure of the cross-linked β-CDP was verified by NMR and thermogravimetric analysis. The solubility of β-CDP in water was around 880 g in 1000 mL. Next, the DOX/β-CDP was formulated by the addition of the polymer into the various concentrations of DOX in a weight ratio of 1:10 and 1:20 (DOX: β-CDP). The formation of the inclusion complex of DOX with β-CDP was studied by UV–Vis spectroscopy. The UV–Vis spectra of DOX/β-CDP formulations show the appearance of the absorption peak at 480 nm and a significant decrease in the absorbance intensity of DOX signal compared to DOX solution. This verified the formation of the DOX/β-CDP complex and also the presence of free DOX in the DOX/β-CDP formulation. The hydrodynamic size of DOX/β-CDP formulation was obtained in the range of nanometer, and the complexion of DOX by β-CDP leads to a negative shift in the zeta potential. In vitro release profile shows a burst release followed by sustained release of DOX from DOX/β-CDP formulation. This is due to the presence of both free and encapsulated DOX. The cytotoxic effect of DOX solution and DOX/β-CDP formulation was evaluated by MTT assay against breast cancer (MCF-7) cell line. The anticancer activity of the DOX/β-CDP was higher than the DOX.
