Cited by 79Advanced Drug Delivery SystemsAdvancements in Transdermal Drug DeliveryDrug Solubulity and Delivery Systems

A grafted copolymer-based nanomicelles for topical ocular delivery of everolimus: formulation, characterization, ex-vivo permeation, in-vitro ocular toxicity, and stability study

Mehra, Nikita, Aqil, Mohd., Sultana, Yasmin·2021·European Journal of Pharmaceutical Sciences

Abstract

Treatment of posterior uveitis via topical route is desirable but cannot be achieved by conventional drug delivery strategies. Therefore, the aim of this study is to develop a topical nanomicellar formulation of an immunosuppressant drug, everolimus using Soluplus®, a grafted copolymer of polyvinyl caprolactam-polyvinylalcohol-polyethyleneglycol (PVCL-PVA-PEG) for improved permeation through ocular epithelia with minimal or no irritation resulting in enhanced ocular bioavailability at the posterior segments of the eye for the treatment of uveitis. Soluplus-everolimus nano micelles were found to have a low CMC (7.2 µg/ml) and 65.55 nm in size. The prepared nanomicelles were characterized for surface morphology by TEM, SEM, and AFM and found to have spherical particles with a smooth surface. The nanomicelles were found to have high encapsulation efficiency and result in sustained release of everolimus when compared with everolimus suspension. The everolimus nanomicelles showed significantly higher permeation across goat cornea than everolimus suspension (p<0.001). CLSM of prepared nanomicelles confirmed the deeper permeation through the goat cornea. These results indicated the significantly higher accessibility and improved drug bioavailability thus, everolimus nanomicelles could be considered a promising topical drug delivery nanocarrier for treating uveitis.

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Crossref · 10.1016/j.ejps.2021.105735

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Authors
Mehra, N., Aqil, M., & Sultana, Y.
Affiliations
Jamia Hamdard (IN)
Corresponding author
Sultana, Yasmin
Venue
European Journal of Pharmaceutical Sciences
Publisher
Elsevier BV
Published
2021-04
Volume
159
Pages
105735
ISSN
0928-0987 (ISSN-L)
OpenAlex
W3128065936
Cited by
79
References
52
Citations by year
2026: 5 · 2025: 11 · 2024: 16 · 2023: 24 · 2022: 14 · 2021: 9
FWCI
6.36
Type
journal article
Language
en
Open access
closed
Locations
  • European Journal of Pharmaceutical Sciences (publishedVersion)
  • PubMed (publishedVersion)
Funders
University Grants Commission
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
Keywords
everolimus, nanomicelles, topical ocular drug delivery, posterior uveitis, Soluplus, corneal permeation, ocular toxicity, sustained drug release, ocular bioavailability, immunosuppressants
MeSH terms
Everolimus, Toxic Optic Neuropathy, Humans, Micelles, Solubility, Nanoparticles, Administration, Ophthalmic

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