4.7 Article

Isotretinoin-Delonix polymeric nanoparticles: Potentials for skin follicular targeting in acne treatment

Journal

INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 610, Issue -, Pages -

Publisher

ELSEVIER
DOI: 10.1016/j.ijpharm.2021.121217

Keywords

Acne vulgaris; Delonix nanoparticles; Skin follicular targeting; Isotretinoin

Funding

  1. Sao Paulo Research Foundation (FAPESP) [2014/22451-7]
  2. World Academy of Science (TWAS)
  3. Brazilian National Council for Scientific and Technological Development (CNPq) (TWAS-CNPq) [190007/2013-3]
  4. National Institute of Science and Technology in Pharmaceutical Nanotechnology -INCT NANOFARMA (FAPESP) [2014/50928-2]
  5. National Institute of Science and Technology in Pharmaceutical Nanotechnology -INCT NANOFARMA (CNPq) [465687/2014-8]
  6. Coordination for the Improvement of Higher Education Personnel -CAPES [001]

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IST-DLX nanoparticles were developed for acne treatment with small particle size, negative zeta potential, and high encapsulation efficiency. These nanoparticles showed enhanced delivery of IST to hair follicles, modulation of inflammation, and reduced irritation, indicating their potential for effective acne management.
In acne management, oral isotretinoin (IST) is associated with various untoward systemic effects, while its topical formulation has irritation side effects. Delonix (DLX) is a natural galactomannan derived from Delonix regia seed that can fabricate nanoparticles for topical skin delivery. This study aims to develop IST-DLX nanoparticles and assess their prospects for acne treatment. Fluorescent-DLX nanoparticles (made with a lipophilic BODIPY dye) or IST-DLX nanoparticles were prepared and characterized. BODIPY-DLX nanoparticles' skin distribution and ISTDLX nanoparticles' in-vitro targeting were assessed in pig ear skin, inflammatory modulation was assessed in AMJ-2 macrophage cells, while skin penetration and irritation were assessed in Wistar rats. IST-DLX nanoparticles had approximate to 230 nm, negative zeta potential, and approximate to 30% encapsulation efficiency. Confocal showed BODIPY in DLX nanoparticles accumulated in hair follicles as compared to BODIPY solution. IST-DLX nanoparticles released approximate to 37% IST over 48 h and increased IST 3-fold in hair follicles compared to IST solution. IST-DLX nanoparticles suppressed IL-6 expression in cells and reduced photo-irritation in Wistar rats compared to IST solution. In conclusion, IST-DLX nanoparticles may target and deliver adequate IST to skin layers associated with acne, avoid systemic penetration, modulate inflammatory pathogenic acne stage and prevent IST topical photo-irritation.

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