Cited by 53Advanced Drug Delivery SystemsOcular Surface and Contact LensAdvancements in Transdermal Drug Delivery

Assembling surfactants-mucoadhesive polymer nanomicelles (ASMP-Nano) for ocular delivery of Cyclosporine-A

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Terreni, Eleonora, Chetoni, Patrizia, Tampucci, Silvia, Burgalassi, Susi, Al-kinani, Ali, Alany, Raid, Monti, Daniela·2020·Pharmaceutics

Abstract

The physiological protective mechanisms of the eye reduce the bioavailability of topically administered drugs above all for those with high molecular weight and /or lipophilic characteristics, such as Cyclosporine A (CyA). The combined strategy based on the association of nanomicelles and mucoadhesive polymer seems promising since a limited number of commercial products containing CyA have been recently approved. The scope of this investigation was the design of Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano), based on a binary system of two surfactants in combination with hyaluronic acid, and their biopharmaceutical evaluation. The optimisation of the ASMP-Nano in term of the amount of surfactants, CyA-loading and size determined the selection of the clear and stable Nano1HAB-CyA formulation containing 0.105% w/w CyA loaded-nanomicelles with a size of 14.41 nm. The nanostructured system had a protective effect towards epithelial corneal cells with a cell viability of more than 80%. It interacted with cellular barriers favouring the uptake and the accumulation of CyA into the cells as evidenced by fluorescent probe distribution, by hindering CyA permeation through reconstituted corneal epithelial tissue. In pharmacokinetics study on rabbits, the nanomicellar carrier prolonged the CyA retention time in the precorneal area mainly in presence of hyaluronic acid (HA), a mucoadhesive polymer.

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Crossref · 10.3390/pharmaceutics12030253

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  • Terreni et al. demonstrated that ASMP-Nano mainly prolonged CyA retention time in the anterior corneal region in the presence of HA in rabbits.

    “Eleonora Terreni et al. have demonstrated that ASMP-Nano mainly prolonged the CyA retention time in the anterior corneal region in the presence of HA (a mucosal adhesion polymer) in the pharmacokinetic study of rabbits [18].”

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Authors
Terreni, E., Chetoni, P., Tampucci, S., Burgalassi, S., Al-kinani, A., Alany, R., & Monti, D.
Affiliations
  • University of Pisa (IT)
  • Kingston University London (GB)
  • University of Auckland (NZ)
Corresponding author
Monti, Daniela
Venue
Pharmaceutics
Publisher
MDPI AG
Published
2020-03-11
Volume
12
Issue
3
Pages
253
ISSN
1999-4923 (ISSN-L)
OpenAlex
W3010915761
Cited by
53
References
57
Citations by year
2026: 3 · 2025: 9 · 2024: 7 · 2023: 11 · 2022: 9 · 2021: 8 · 2020: 6
FWCI
3.30
Type
journal article
Language
en
Open access
Locations
  • Pharmaceutics (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • Research Repository (Kingston University London) (acceptedVersion)
  • CINECA IRIS Institutial research information system (University of Pisa) (submittedVersion, other-oa)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Funders
Università di Pisa (PRA 2018_18)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Ocular Surface and Contact Lens
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
Keywords
cyclosporine, ocular drug delivery, nanomicelles, hyaluronic acid, mucoadhesive polymers, corneal epithelial cells, precorneal retention, pharmacokinetics, topical ocular formulations, corneal permeation

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