Cited by 128Advanced Drug Delivery SystemsDrug Solubulity and Delivery SystemsNanoparticle-Based Drug Delivery

α-Lipoic acid in soluplus(®) polymeric nanomicelles for ocular treatment of diabetes-associated corneal diseases

Alvarez-Rivera, Fernando, Fernández-Villanueva, David, Concheiro, Angel, Alvarez-Lorenzo, Carmen·2016·Journal of Pharmaceutical Sciences

Abstract

α-Lipoic acid (ALA) is a powerful antioxidant valuable for prevention and treatment of ophthalmic complications such as diabetic keratopathy and retinopathy. The aim of this work was to develop micelle-based formulations that can enhance the solubility, stability, and corneal permeability of ALA. Compared to a conventional surfactant (sodium dioctylsulfosuccinate), Soluplus(®) (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol copolymer) led to smaller micelles (70-80 vs. 240-528 nm) with improved ability to solubilize ALA, maintaining ocular compatibility (Hens Egg Test on the Chorio-Allantoic Membrane). Soluplus nanomicelles enhanced more than 10-fold ALA solubility compared to common eye drops and withstood strong dilution in lachrymal fluid, filtration through sterilizing membranes, and freeze-drying. Interestingly, Soluplus nanomicelle formulation prepared with 1 or 2 mM block copolymer concentration exhibited in situ gelling capability and transformed into weak gels at 35°C, which is expected to increase corneal residence time. Bovine corneal permeability revealed that Soluplus nanomicelles notably enhanced ALA accumulation into the cornea as well as flux of drug toward the receptor chamber. Overall, these findings point out Soluplus nanomicelles as suitable carriers of ALA that may exhibit improved performance compared to currently available eye drop solutions.

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Crossref · 10.1016/j.xphs.2016.03.006

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  • Soluplus nanomicelles demonstrated a tenfold enhancement in ALA solubility compared with conventional eye drops while withstanding strong dilution in the lachrymal fluid.

    “Soluplus nanomicelles demonstrated a tenfold enhancement in ALA solubility compared with conventional eye drops while withstanding strong dilution in the lachrymal fluid.”

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Authors
Alvarez-Rivera, F., Fernández-Villanueva, D., Concheiro, A., & Alvarez-Lorenzo, C.
Affiliations
Universidade de Santiago de Compostela (ES)
Venue
Journal of Pharmaceutical Sciences
Publisher
Elsevier BV
Published
2016-09
Volume
105
Issue
9
Pages
2855-2863
ISSN
0022-3549 (ISSN-L)
OpenAlex
W2341154678
Cited by
127
References
44
Citations by year
2026: 7 · 2025: 16 · 2024: 9 · 2023: 13 · 2022: 17 · 2021: 11 · 2020: 21 · 2019: 13 · 2018: 10 · 2017: 8 · 2016: 2
FWCI
6.27
Type
journal article
Language
en
Open access
closed
Locations
  • Journal of Pharmaceutical Sciences (publishedVersion)
  • PubMed (publishedVersion)
Funders
Fundación BBVA
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Keywords
alpha-lipoic acid, Soluplus, polymeric micelles, ocular drug delivery, diabetic keratopathy, corneal permeability, drug solubilization, in situ gelling, sodium dioctylsulfosuccinate, bovine cornea, freeze-drying stability
MeSH terms
Animals, Antioxidants, Cattle, Cornea, Corneal Diseases, Drug Compounding, Freeze Drying, Thioctic Acid, Micelles, Permeability, Polyethylene Glycols, Polymers, Polyvinyls, Solubility, Diabetes Complications, Chorioallantoic Membrane, Nanoparticles, Administration, Ophthalmic

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