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Mater Sci Eng C Mater Biol Appl. 2019 Oct;103:109730. doi: 10.1016/j.msec.2019.05.015.
Epub 2019 May 10.

Bimatoprost loaded nanovesicular long-acting sub-conjunctival

in-situ gelling implant: In vitro and in vivo evaluation

Monika Yadav 1 , Ana Guzman‐Aranguez 2 , Maria J Perez de Lara 2 , Mandeep Singh 1 ,

Joga Singh 1 , Indu Pal Kaur 3

Affiliations expand

PMID: 31349399
DOI: 10.1016/j.msec.2019.05.015

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Abstract
Primary treatment for glaucoma relies on chronic instillation ﴾daily﴿ of intraocular pressure ﴾IOP﴿
lowering eye drops. Present study tends to develop and assess a novel sustained release
bimatoprost loaded nanovesicular ﴾BMT‐NV﴿ ‐ thermosensitive in‐situ gelling implant ﴾BMT‐NV‐
GEL‐IM﴿, for subconjunctival delivery. BMT‐NVs developed using novel composition and method
of preparation, ﴾IPA/700/DEL/2014﴿ and industrially viable methodology were characterized and
evaluated comprehensively for ocular suitability. Their incorporation into an in‐situ gelling
formula was safe ﴾in vitro and in vivo﴿ and stable upon sterilization. Autoclavability was an
important consideration, as a preservative‐free, single‐use BMT‐NV‐GEL‐IM will avoid side‐
effects associated with repetitive application of drops containing preservatives like
benzalkonium chloride ﴾BAK﴿. An extended in vitro release of BMT ﴾80.23%﴿ was observed for 10
days while the IOP lowering effect extended over 2 months with single subconjunctival injection
of BMT‐NV‐GEL‐IM in rats. No clinical signs of irritation, inflammation, or infection were
observed in any injected eye, throughout the study, as also confirmed by histology.
Furthermore, single administration of BMT‐NV‐GEL as topical drop lowered the IOP over 5 days.
Presence of significant diffuse fluorescence in confocal microscopy of internal eye tissues post‐
in vivo application, as subconjunctival implant, even after 2 month and eye drops upto1 week
provide direct evidence of successful sustained delivery. We thus provide an improved modality
for antiglaucoma medication in patients who are challenged to adhere to a regimen of daily eye
drops.

Keywords: Cytotoxicity; Fluorescence; Glaucoma; Nanomedicine; Ocular; Sustained delivery.

Copyright © 2019 Elsevier B.V. All rights reserved.

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MeSH terms
Animals
Bimatoprost* / chemistry
Bimatoprost* / pharmacokinetics
Bimatoprost* / pharmacology
Drug Evaluation, Preclinical
Drug Implants
Glaucoma* / drug therapy
Glaucoma* / metabolism
Glaucoma* / pathology
Male
Nanostructures* / chemistry
Nanostructures* / therapeutic use
Rats
Rats, Wistar

Substances
Drug Implants
Bimatoprost

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PubChem Compound ﴾MeSH Keyword﴿

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