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D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid

Department of Pharmacy (DiFAR), University of Genoa, Viale Cembrano 4, 16148 Genova, Italy
Department of Experimental Medicine—DIMES, University of Genoa, Via Alberti L.B. 2, 16132 Genova, Italy
Department of Sciences for the Quality of Life, University of Bologna, Corso D’Augusto 237, 47921 Rimini, Italy
Author to whom correspondence should be addressed.
Academic Editor: Dimitris Tsiourvas
Pharmaceuticals 2021, 14(3), 212;
Received: 5 February 2021 / Revised: 25 February 2021 / Accepted: 26 February 2021 / Published: 4 March 2021
(This article belongs to the Special Issue Applications of Micro-Nanosystems in Retinoids Delivery)
All-trans-retinoic acid (ATRA) represents the first-choice treatment for several skin diseases, including epithelial skin cancer and acne. However, ATRA’s cutaneous side effects, like redness and peeling, and its high instability limit its efficacy. To address these drawbacks and to improve ATRA solubilization, we prepared ATRA-loaded micelles (ATRA-TPGSs), by its encapsulation in D-α-tocopheryl-polyethylene-glycol-succinate (TPGS). First, to explore the feasibility of the project, a solubility study based on the equilibrium method was performed; then, six ATRA-TPGS formulations were prepared by the solvent-casting method using different TPGS amounts. ATRA-TPGSs showed small sizes (11–20 nm), low polydispersity, slightly negative zeta potential, and proved good encapsulation efficiency, confirmed by a chemometric-assisted Fourier transform infrared spectroscopy (FTIR) investigation. ATRA-TPGS stability was also investigated to choose the most stable formulation. Using Carbopol® 980 as gelling agent, ATRA-TPGS-loaded gels were obtained and analyzed for their rheological profiles. Ex vivo release studies from ATRA-TPGSs were performed by Franz cells, demonstrating a permeation after 24 h of 22 ± 4 µ cm−2. ATRA-TPGSs showed enhanced cytotoxic effects on melanoma cells, suggesting that these formulations may represent a valid alternative to improve patient compliance and to achieve more efficacious therapeutic outcomes. View Full-Text
Keywords: retinoic acid; micelles; TPGS; nanocarriers; drug delivery systems; topical application; nanocarrier-loaded gels retinoic acid; micelles; TPGS; nanocarriers; drug delivery systems; topical application; nanocarrier-loaded gels
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MDPI and ACS Style

Zuccari, G.; Baldassari, S.; Alfei, S.; Marengo, B.; Valenti, G.E.; Domenicotti, C.; Ailuno, G.; Villa, C.; Marchitto, L.; Caviglioli, G. D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid. Pharmaceuticals 2021, 14, 212.

AMA Style

Zuccari G, Baldassari S, Alfei S, Marengo B, Valenti GE, Domenicotti C, Ailuno G, Villa C, Marchitto L, Caviglioli G. D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid. Pharmaceuticals. 2021; 14(3):212.

Chicago/Turabian Style

Zuccari, Guendalina, Sara Baldassari, Silvana Alfei, Barbara Marengo, Giulia E. Valenti, Cinzia Domenicotti, Giorgia Ailuno, Carla Villa, Leonardo Marchitto, and Gabriele Caviglioli. 2021. "D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid" Pharmaceuticals 14, no. 3: 212.

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