Adapalene-loaded poly

Adapalene (ADAP) is an important drug widely used in the topical treatment of acne. It is a third-generation retinoid and provides keratolytic, anti-inflammatory, and antiseborrhoic action. However, some topical adverse effects such as erythema, dryness, and scaling have been reported with its comme...

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Bibliographic Details
Published in:PloS one 2019-03, Vol.14 (3), p.e0213625
Main Authors: Novatski, Andressa, Dias, Daniele Toniolo, Padilha de Paula, Josiane, Farago, Paulo Vitor, Lyra, Amanda, Nadal, Jessica Mendes, dos Anjos Camargo, Guilherme, Barboza, Fernanda Malaquias, Macenhan, William Roger, Roik, João Ricardo, Somer, Aloisi
Format: Article
Language:English
Subjects:
Acne
Adapalene
Anti-inflammatory agents
Antiacne agents
Bonds (Securities)
Caprolactone
Chemical properties
Dermatologic agents
Dosage and administration
Drug delivery systems
Drug therapy
Erythema
Microencapsulation
Photoacoustic spectroscopy
Polymer industry
Polymers
Polyols
Spectra
Spectroscopy
Transdermal drug delivery systems
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Summary:Adapalene (ADAP) is an important drug widely used in the topical treatment of acne. It is a third-generation retinoid and provides keratolytic, anti-inflammatory, and antiseborrhoic action. However, some topical adverse effects such as erythema, dryness, and scaling have been reported with its commercial formula. In this sense, the microencapsulation of this drug using polyesters can circumvent its topical side effects and can lead to the enhancement of drug delivery into sebaceous glands. The goal of this work was to obtain ADAP-loaded poly([epsilon]-caprolactone) (PCL) microparticles prepared by a simple emulsion/solvent evaporation method. Formulations containing 10 and 20% of ADAP were successfully obtained and characterized by morphological, spectroscopic, and thermal studies. Microparticles presented encapsulation efficiency of ADAP above 98% and showed a smooth surface and spherical shape. Fourier transform infrared spectroscopy (FTIR) results presented no drug-polymer chemical bond, and a differential scanning calorimetry (DSC) technique showed a partial amorphization of the drug. ADAP permeation in the Strat-M membrane for transdermal diffusion testing was evaluated by photoacoustic spectroscopy (PAS) in the spectral region between 225 and 400 nm after 15 min and 3 h from the application of ADAP-loaded PCL formulations. PAS was successfully used for investigating the penetration of polymeric microparticles. In addition, microencapsulation decreased the in vitro transmembrane diffusion of ADAP.
ISSN:1932-6203
1932-6203