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      Diclofenac-Derived Hybrids for Treatment of Actinic Keratosis and Squamous Cell Carcinoma

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          Abstract

          In this work, hybrid compounds 1– 4 obtained by conjugation of the non-steroidal anti-inflammatory drug diclofenac, with natural molecules endowed with antioxidant and antiproliferative activity were prepared. The antiproliferative activity of these hybrids was evaluated on immortalized human keratinocyte (HaCaT) cells stimulated with epidermal growth factor (EGF), an actinic keratosis (AK) model, and on human squamous cell carcinoma (SCC) cells (A431). Hybrid 1 presented the best activity in both cell models. Self-assembling surfactant nanomicelles have been chosen as the carrier to drive the hybrid 1 into the skin; the in vitro permeation through and penetration into pig ear skin have been evaluated. Among the nanostructured formulations tested, Nano3Hybrid20 showed a higher tendency of the hybrid 1 to be retained in the skin rather than permeating it, with a desirable topical and non-systemic action. On these bases, hybrid 1 may represent an attractive lead scaffold for the development of new treatments for AK and SCC.

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          Porcine ear skin: an in vitro model for human skin.

          Ute Jacobi, Marco Kaiser, Rani Toll … (2007)
          Porcine ear skin is used in studies of percutaneous penetration as a substitute for human skin. The structure of this tissue, including hair follicles, was studied qualitatively and quantitatively in comparison with human skin. Sections of shock-frozen biopsies, biopsies embedded in paraffin and cyanoacrylate skin surface biopsies were investigated using microscopy. The thickness of the different skin layers and the follicular characteristics were determined. The thickness of the stratum corneum was 17-28 microm, whereas the viable epidermis was 60-85 microm thick. On 1 cm(2), 11-25 hairs were detected, showing a diameter of 58-97 microm and a maximal extension depth of 0.96-1.38 mm into the skin. The orifices of the porcine infundibula showed a diameter of approximately 200 microm. The results obtained are similar to those of human skin, indicating the suitability of this porcine tissue as a model for human skin.
          Article 0 comments Cited 109 times – based on 0 reviews     Review now
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            Recent Advances in the Application of Vitamin E TPGS for Drug Delivery

            Conglian Yang, Tingting Wu, Yan Qi … (2018)
            D-ɑ-tocopheryl polyethylene glycol succinate (Vitamin E TPGS or TPGS) has been approved by FDA as a safe adjuvant and widely used in drug delivery systems. The biological and physicochemical properties of TPGS provide multiple advantages for its applications in drug delivery like high biocompatibility, enhancement of drug solubility, improvement of drug permeation and selective antitumor activity. Notably, TPGS can inhibit the activity of ATP dependent P-glycoprotein and act as a potent excipient for overcoming multi-drug resistance (MDR) in tumor. In this review, we aim to discuss the recent advances of TPGS in drug delivery including TPGS based prodrugs, nitric oxide donor and polymers, and unmodified TPGS based formulations. These potential applications are focused on enhancing delivery efficiency as well as the therapeutic effect of agents, especially on overcoming MDR of tumors. It also demonstrates that the clinical translation of TPGS based nanomedicines is still faced with many challenges, which requires more detailed study on TPGS properties and based delivery system in the future.
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              The Role of Antioxidants in Skin Cancer Prevention and Treatment

              Aleksandar Godic, Borut Poljšak, Metka Adamic … (2014)
              Skin cells are constantly exposed to reactive oxygen species (ROS) and oxidative stress from exogenous and endogenous sources. UV radiation is the most important environmental factor in the development of skin cancer and skin aging. The primary products caused by UV exposure are generally direct DNA oxidation or generation of free radicals which form and decompose extremely quickly but can produce effects that can last for hours, days, or even years. UV-induced generation of ROS in the skin develops oxidative stress when their formation exceeds the antioxidant defense ability. The reduction of oxidative stress can be achieved on two levels: by lowering exposure to UVR and/or by increasing levels of antioxidant defense in order to scavenge ROS. The only endogenous protection of our skin is melanin and enzymatic antioxidants. Melanin, the pigment deposited by melanocytes, is the first line of defense against DNA damage at the surface of the skin, but it cannot totally prevent skin damage. A second category of defense is repair processes, which remove the damaged biomolecules before they can accumulate and before their presence results in altered cell metabolism. Additional UV protection includes avoidance of sun exposure, usage of sunscreens, protective clothes, and antioxidant supplements.
              Article 0 comments Cited 77 times – based on 0 reviews     Review now
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                Author and article information

                Journal
                Journal ID (nlm-ta): Molecules
                Journal ID (iso-abbrev): Molecules
                Journal ID (publisher-id): molecules
                Title: Molecules
                Publisher: MDPI
                ISSN (Electronic): 1420-3049
                Publication date (Electronic): 09 May 2019
                Publication date Collection: May 2019
                Volume: 24
                Issue: 9
                Electronic Location Identifier: 1793
                Affiliations
                [1 ]Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy; silvia.tampucci@ 123456unipi.it (S.T.); sara.carpi@ 123456unipi.it (S.C.); b.polini@ 123456studenti.unipi.it (B.P.); susi.burgalassi@ 123456unipi.it (S.B.); marco.macchia@ 123456unipi.it (M.M.); Paola.nieri@ 123456unipi.it (P.N.); clementina.manera@ 123456unipi.it (C.M.); daniela.monti@ 123456unipi.it (D.M.)
                [2 ]Interdepartmental Research Center “Nutraceuticals and Food for Health” (NutraFood), University of Pisa, 56126 Pisa, Italy
                [3 ]Department of Clinical and Experimental Medicine, University of Pisa, Via Savi 10, 56126 Pisa, Italy; stefano.fogli@ 123456unipi.it
                Author notes
                [* ]Correspondence: maria.digiacomo@ 123456unipi.it ; Tel.: +39-0502219594
                [†]

                These authors contributed equally to this work.

                Author information
                https://orcid.org/0000-0002-8927-6083
                https://orcid.org/0000-0002-3291-9009
                https://orcid.org/0000-0003-0653-6642
                https://orcid.org/0000-0002-0795-2886
                https://orcid.org/0000-0001-7622-4367
                Article
                Publisher ID: molecules-24-01793
                DOI: 10.3390/molecules24091793
                PMC ID: 6539072
                PubMed ID: 31075867
                SO-VID: aba677b3-80d7-487f-9881-8c511c0bfdeb
                Copyright © © 2019 by the authors.
                License:

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                Date received : 30 March 2019
                Date accepted : 05 May 2019
                Categories
                Subject: Article

                Keywords: diclofenac,hybrid,squamous cell carcinoma,actinic keratosis,antiproliferative activity,nanomicelles,in vitro skin permeation/penetration
                Data availability:
                Keywords: diclofenac, hybrid, squamous cell carcinoma, actinic keratosis, antiproliferative activity, nanomicelles, in vitro skin permeation/penetration

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