Cited by 1Advanced Drug Delivery SystemsDrug Solubulity and Delivery SystemsAdvancements in Transdermal Drug Delivery

A nanomicelles platform delivery system for water-insoluble corticosteroid to treat anterior uveitis

Sathe, Priyadarshini, Kameshwari, Srujana Mosalikanti Sai, Nirmal, Jayabalan·2025·The AAPS Journal

Abstract

Difluprednate is marketed as an emulsion due to its poor aqueous solubility. Emulsions are known to cause ocular discomfort and require frequent dosing to show therapeutic activity. Nanomicelles are well known to improve the solubility and permeation of water-insoluble drugs. Therefore, to enhance the water solubility and reduce the dosing frequency by improving difluprednate permeation across the cornea, we formulated nanomicelles. Difluprednate loaded nanomicelles (Dicel) was prepared by thin film hydration method and optimized using Box-Behnken design. The Dicel formulated had a particle size, polydispersity index, zeta potential and entrapment efficiency of 21.9 nm, 0.15, -7.55 mV and 75.4%, respectively. Transmission electron microscopy analysis showed spherical nanomicelles. The Dicel showed a sustained release profile for 48 h. The difluprednate permeation across the cornea from Dicel was enhanced by twofold compared to commercially available emulsion. Also, it was found to be stable upon dilution with simulated tear fluid and was biocompatible. Further, Dicel improved the anti-inflammatory activity of difluprednate at one and two times a day administration compared to four times a day administration of difluprednate emulsion. The present study highlights the role of topical nanomicelles in delivering difluprednate, which is better than the existing marketed emulsion in the management of ocular inflammation.

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Crossref · 10.1208/s12248-025-01103-z

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  • Topical nanomicelles represent a promising novel delivery system for anterior uveitis treatment with reduced dosing frequency.

    “With favorable stability and biocompatibility, these findings confirm that topical nanomicelles represent a promising novel delivery system for anterior uveitis treatment with reduced dosing frequency [175].”

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Authors
Sathe, P., Kameshwari, S. M. S., & Nirmal, J.
Affiliations
Birla Institute of Technology and Science - Hyderabad Campus (IN)
Corresponding author
Nirmal, Jayabalan
Venue
The AAPS Journal
Published
2025-07-22
Volume
27
Issue
5
Pages
122-122
ISSN
1550-7416 (ISSN-L)
OpenAlex
W4412567128
Cited by
1
References
50
Citations by year
2025: 1
FWCI
0.42
Type
journal article
Language
en
Open access
closed
Locations
  • The AAPS Journal (publishedVersion)
  • PubMed (publishedVersion)
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
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
Keywords
difluprednate, nanomicelles, anterior uveitis, ocular drug delivery, corneal permeation, topical ocular formulations, thin-film hydration, sustained drug release, anti-inflammatory activity, ocular inflammation, Box-Behnken design
MeSH terms
Animals, Cornea, Emulsions, Fluprednisolone, Glucocorticoids, Humans, Micelles, Particle Size, Rabbits, Solubility, Uveitis, Anterior, Water, Drug Delivery Systems, Nanoparticles, Administration, Ophthalmic, Drug Liberation

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