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Cited by 119Advancements in Transdermal Drug DeliveryAdvanced Drug Delivery SystemsNanoparticle-Based Drug Delivery

The DOI matches its Crossref record; 28 of the 28 references it cites were found in a registry or an index.

Formation of ion pairing as an alternative to improve encapsulation and stability and to reduce skin irritation of retinoic acid loaded in solid lipid nanoparticles

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Castro, Gisele A., Coelho, Anna Luíza L.R., Oliveira, Cleida A., Mahecha, Germán A.B., Oréfice, Rodrigo L., Ferreira, Lucas A.M.·2009·International Journal of Pharmaceutics
DOI 10.1016/j.ijpharm.2009.07.025
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Abstract

This work aims to investigate the influence of the formation of ion pairing between all-trans retinoic acid (RA) and a lipophilic amine (stearylamine; STE) on the drug encapsulation efficiency (EE) and stability of solid lipid nanoparticles (SLNs). The SLNs were characterized for EE and size. The EE and particle size were significantly improved and reduced, respectively, when the surfactant or co-surfactant concentration increased. However, while the formulation without STE allowed only 13% of RA encapsulation, the EE for RA-STE-loaded SLNs was 94%. The stability studies showed a significant decrease in EE for the SLNs without STE, while, for SLNs loaded with RA and STE, the EE remained constant after 360 days. The interactions among ion pairing components and the lipid matrix were investigated through small-angle X-ray scattering (SAXS). The SAXS analysis revealed the presence of RA in the crystalline form in SLNs without ion pairing, while crystalline RA was not observed in SLNs loaded with RA/amine. Skin irritation studies showed that the SLNs loaded with the ion pairing were significantly less irritating when compared to the marketed RA-cream. This novel SLN formulation represents a promising alternative for topical treatment of acne with RA.

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Research works printed but not linked: 2

  1. Kayali, 1991, Interactions of retinoic acid with a model of stratum corneum lipids, J. Dermal. Clin. Eval. Soc., 2, 7
  2. US Pharmacopoeia 26, 2003. US Pharmacopoeial Convention, Rockville, MD, pp. 1861–1862.

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Metadata

Authors
Castro, G. A., Coelho, A. L. L. R., Oliveira, C. A., Mahecha, G. A. B., Oréfice, R. L., & Ferreira, L. A. M.
Affiliations
Universidade Federal de Minas Gerais (BR)
Corresponding author
Ferreira, Lucas A.M.
ORCID
Venue
International Journal of Pharmaceutics
Publisher
Elsevier BV
Published
2009-10
Volume
381
Issue
1
Pages
77-83
ISSN
0378-5173 (ISSN-L)
DOI
10.1016/j.ijpharm.2009.07.025
OpenAlex
W2005760281
Cited by
119
References
28
Citations by year
2025: 6 · 2024: 8 · 2023: 3 · 2022: 4 · 2021: 14 · 2020: 10 · 2019: 9 · 2018: 5 · 2017: 7 · 2016: 8 · 2015: 11 · 2014: 6 · 2013: 9 · 2012: 8
FWCI
4.28
Type
journal article
Language
en
Open access
Licence
Locations
  • International Journal of Pharmaceutics (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • Conselho Nacional de Desenvolvimento Científico e Tecnológico
  • Fundação de Amparo à Pesquisa do Estado de Minas Gerais
  • Universidade Federal de Minas Gerais
  • Laboratório Nacional de Luz Síncrotron
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Keywords
ion pairing, all-trans retinoic acid, solid lipid nanoparticles, octadecylamine, encapsulation efficiency, nanoparticle stability, skin irritation, topical retinoids, acne treatment
MeSH terms
Acne Vulgaris, Administration, Cutaneous, Amines, Animals, Chemistry, Pharmaceutical, Drug Stability, Emulsions, Exanthema, Excipients, Female, Mice, Hairless, Particle Size, Surface Properties, Surface-Active Agents, Tretinoin, X-Ray Diffraction, Drug Delivery Systems, Phase Transition, Mice, Nanoparticles, Scattering, Small Angle, Electrochemical Techniques

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