Ion Pair Strategy in Solid Lipid Nanoparticles: a Targeted Approach to Improve Epidermal Targeting with Controlled Adapa
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RESEARCH PAPER
Ion Pair Strategy in Solid Lipid Nanoparticles: a Targeted Approach to Improve Epidermal Targeting with Controlled Adapalene Release, Resulting Reduced Skin Irritation Linna B. O. Rodrigues 1 & Flávia A. Lima 1 & Camila P. B. Alves 1 & Elisângela Martins-Santos 2 & Marta M. G. Aguiar 1 & Cleida A. Oliveira 2 & Rodrigo L. Oréfice 3 & Lucas A. M. Ferreira 1 & Gisele A. C. Goulart 1 Received: 24 February 2020 / Accepted: 24 June 2020 # Springer Science+Business Media, LLC, part of Springer Nature 2020
ABSTRACT 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.
KEY WORDS adapalene . epidermal targeting . ion pair .
skin irritation . SLN
ABBREVIATIONS AD DCChol®
* Gisele A. C. Goulart [email protected]; [email protected]
Rodrigo L. Oréfice [email protected]
Linna B. O. Rodrigues [email protected]
Lucas A. M. Ferreira [email protected]
Flávia A. Lima [email protected] Camila P. B. Alves [email protected] Elisângela Martins-Santos [email protected]
1
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
2
Department of Morphology, Institute of Biological Sciences, UFMG, Belo Horizonte, MG CEP 31270-901, Brazil
3
Department of Metallurgical and Materials Engineering, UFMG, Belo Horizonte, MG CEP 31270-901, Brazil
Marta M. G. Aguiar [email protected] Cleida A. Oliveira [email protected]
Adapalene 3β-[N-(Dimethylaminoethane)carbamoyl] cholesterol
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DSC EE FTIR HPLC MH PBS PDI PU RA SA SAXS SLN TEM XRD
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Differential scanning calorimetry Encapsulation efficiency Fourier-transform infrared spectroscopy High performance liquid chromatogr
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