Ion Pair Strategy in Solid Lipid Nanoparticles: a Targeted Approach to Improve Epidermal Targeting with Controlled Adapalene Release, Resulting Reduced Skin Irritation.

Autor: Rodrigues LBO; Department of Pharmaceutics, Faculty of Pharmacy, Campus Pampulha - Universidade Federal de Minas Gerais (UFMG), Av Antônio Carlos, 662, Belo Horizonte, MG, CEP 31270-901, Brazil., Lima FA; Department of Pharmaceutics, Faculty of Pharmacy, Campus Pampulha - Universidade Federal de Minas Gerais (UFMG), Av Antônio Carlos, 662, Belo Horizonte, MG, CEP 31270-901, Brazil., Alves CPB; Department of Pharmaceutics, Faculty of Pharmacy, Campus Pampulha - Universidade Federal de Minas Gerais (UFMG), Av Antônio Carlos, 662, Belo Horizonte, MG, CEP 31270-901, Brazil., Martins-Santos E; Department of Morphology, Institute of Biological Sciences, UFMG, Belo Horizonte, MG, CEP 31270-901, Brazil., Aguiar MMG; Department of Pharmaceutics, Faculty of Pharmacy, Campus Pampulha - Universidade Federal de Minas Gerais (UFMG), Av Antônio Carlos, 662, Belo Horizonte, MG, CEP 31270-901, Brazil., Oliveira CA; Department of Morphology, Institute of Biological Sciences, UFMG, Belo Horizonte, MG, CEP 31270-901, Brazil., Oréfice RL; Department of Metallurgical and Materials Engineering, UFMG, Belo Horizonte, MG, CEP 31270-901, Brazil., Ferreira LAM; Department of Pharmaceutics, Faculty of Pharmacy, Campus Pampulha - Universidade Federal de Minas Gerais (UFMG), Av Antônio Carlos, 662, Belo Horizonte, MG, CEP 31270-901, Brazil., Goulart GAC; Department of Pharmaceutics, Faculty of Pharmacy, Campus Pampulha - Universidade Federal de Minas Gerais (UFMG), Av Antônio Carlos, 662, Belo Horizonte, MG, CEP 31270-901, Brazil. giseleacgoulart@gmail.com.
Jazyk: angličtina
Zdroj: Pharmaceutical research [Pharm Res] 2020 Jul 17; Vol. 37 (8), pp. 148. Date of Electronic Publication: 2020 Jul 17.
DOI: 10.1007/s11095-020-02866-0
Abstrakt: Purpose: Adapalene (AD) is one of the main retinoids used in the topical therapy of acne, an extremely common skin disease usually associated with psychological morbidity. However, like other retinoids, AD is frequently associated with skin irritation. To overcome the skin irritation, we proposed the encapsulation of AD in solid lipid nanoparticles (SLNs) using the ion pair strategy.
Methods: The developed SLN-AD was characterized by high-performance liquid chromatography, differential scanning calorimetry, X-ray diffraction, synchrotron small-angle X-ray scattering, and transmission electron microscopy. In vitro permeation tests using porcine skin and in vivo mice skin irritation test were performed to evaluate, respectively, the drug's skin distribution and the skin irritation.
Results: The characterization studies were able to demonstrate that the proposed strategy effectively provided high AD encapsulation in SLNs and its incorporation into a hydrophilic gel. Sustained release, epidermal targeting, and less skin irritation were observed for SLN-AD gel in comparison to the marketed AD gel.
Conclusions: The studies demonstrated that the encapsulation of AD in SLNs through the formation of an ion pair is a valuable alternative to diminish the adverse skin reactions caused by AD and can optimize patient adherence to treatment.
Databáze: MEDLINE
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