Bimatoprost loaded nanovesicular long-acting sub-conjunctival in-situ gelling implant: In vitro and in vivo evaluation

Yadav, Monika; Guzmán-Aránguez, Ana; Lara, María J Pérez de; Singh, Mandeep; Singh, J. S.; Kaur, Indu Pal

doi:10.1016/j.msec.2019.05.015

Cited by 16 publications

(12 citation statements)

References 61 publications

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“…It is challenging to ensure drug delivery into posterior segment ocular tissues following topical eye drops instillation because of the above-mentioned barriers. The solutions to overcoming these bioavailability issues may emerge with the development of advanced ophthalmic gel formulations; also sub-conjunctival application could be tested when formulations with extended delivery are available [ 27 ].…”

Section: Discussionmentioning

confidence: 99%

Recent large-scale philophthalmosis outbreak in Portugal: inefficacy of common antihelminthic agents

Heneberg

Casero²

2022

Parasites Vectors

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Background Parasitic conjunctivitis caused by Philophthalmus spp. is a common ophthalmic disease in birds, with localized outbreaks occurring worldwide. There is no consensus on treating this disease; mechanical removal is considered a standard recommendation, but is associated with disease relapses within days or weeks. Methods From 2015 to 2020, we examined 4295 Larus michahellis and Larus fuscus gulls in southern Portugal for the presence of Philophthalmus spp. Due to the need to treat dozens of infected gulls in the rescue station, we tested three treatment regimens aimed at targeting Philophthalmus lucipetus in the infected gulls: (I) the ophthalmic application of levamisole; (II) the oral application of milbemycin in combination with praziquantel; and (III) the subcutaneous application of ivermectin. Results The outbreak of philophthalmosis in gulls in southern Portugal has been ongoing since the first cases were reported in 2015–2016. The prevalence of philophthalmosis has fluctuated annually, peaking a maximum of 10.3% in L. fuscus in 2017 and at 2.1% in L. michahellis in 2016. The infection intensity peaked at a median of 11.5 eye-flukes per host bird in L. fuscus in 2016 and a median of six eye-flukes per host bird in L. michahellis in 2017. Nine gulls were infected with >50 eye-flukes. None of the treatment options were effective at treating P. lucipetus infections: the numbers of eye-flukes in the infected birds did not decrease, and the clinical signs of the disease did not change. Conclusions An outbreak of philophthalmosis in southern Portugal has massively affected two species of gulls in the region. Two previously suggested philophthalmosis treatments (ocular levamisole and praziquantel given orally), as well as a third mode of treatment with a previously failed compound (ivermectin administered subcutaneously) were used. However, the treatments did not affect the numbers of P. lucipetus in the eyes of the treated gulls. Further research should address ophthalmic gel formulations or sub-conjunctival delivery mode for antihelminthic drugs that are effective against Philophthalmus spp. in vitro. Graphical abstract

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Section: Discussionmentioning

confidence: 99%

Recent large-scale philophthalmosis outbreak in Portugal: inefficacy of common antihelminthic agents

Heneberg

Casero²

2022

Parasites Vectors

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“…The pH of the Bimatoprost formulation is 7.2 which indicates the Bimatoprost formulation meets the requirements [36].…”

Section: Bimatoprostmentioning

confidence: 99%

A Comprehensive Chemical Characterization of in Situ Ophthalmic Gel

et al. 2021

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In situ ophthalmic gel is a gel preparation that is initially in the form of ophthalmic solution that dripped into the eye and then the solution turns into a gel after contact with the surface of the eye. In situ gel will undergo phase change to gel due to pH, electrolyte and temperature conditions. So that the preparation of ophthalmic in situ gel is required characterization to make sure that the prepared preparations meet the standards and are safe when used. Chemical evaluation includes pH, concentration, chemical bonds, crystallization and drug and polymer interactions. The purpose of this review is to discuss the evaluation methods used in preparations, and to see whether the pH of in situ ophthalmic gel formulation that provided can met the ideal pH requirements of the eye, so that the ophthalmic in situ gel preparation would not causing irritation and liquid tear production.

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“…Moreover, no irritation, inflammation, or infection was observed in the study. 392 Additionally, a biodegradable implant (Bimatoprost SR) was designed that employed a biodegradable Novadur (Allergan plc) platform to provide a slow release of bimatoprost over time. 393 In phase 1/2 clinical trials, it was found that Bimatoprost SR implant and bimatoprost administered topically (0.03%) induced similar IOP-lowering effects in humans.…”

Section: Odd Nanowafermentioning

confidence: 99%

“…The results revealed favorable outcomes, such as extended in vitro release of bimatoprost (80.23%) for 10 days and an extension of the IOP-lowering effect over 2 months with single subconjunctival injection of bimatoprost loaded nanovesicular-thermosensitive in situ gelling implant in rats. Moreover, no irritation, inflammation, or infection was observed in the study …”

Section: Ocular Drug Delivery (Odd)mentioning

confidence: 99%

Ocular Disease Therapeutics: Design and Delivery of Drugs for Diseases of the Eye

et al. 2020

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The ocular drug discovery field has evidenced significant advancement in the past decade. The FDA approvals of Rhopressa, Vyzulta, and Roclatan for glaucoma, Brolucizumab for wet age-related macular degeneration (wet AMD), Luxturna for retinitis pigmentosa, Dextenza (0.4 mg dexamethasone intracanalicular insert) for ocular inflammation, ReSure sealant to seal corneal incisions, and Lifitegrast for dry eye represent some of the major developments in the field of ocular therapeutics. A literature survey also indicates that gene therapy, stem cell therapy, and target discovery through genomic research represent significant promise as potential strategies to achieve tissue repair or regeneration and to attain therapeutic benefits in ocular diseases. Overall, the emergence of new technologies coupled with first-in-class entries in ophthalmology are highly anticipated to restructure and boost the future trends in the field of ophthalmic drug discovery. This perspective focuses on various aspects of ocular drug discovery and the recent advances therein. Recent medicinal chemistry campaigns along with a brief overview of the structure–activity relationships of the diverse chemical classes and developments in ocular drug delivery (ODD) are presented.

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Bimatoprost loaded nanovesicular long-acting sub-conjunctival in-situ gelling implant: In vitro and in vivo evaluation

Cited by 16 publications

References 61 publications

Recent large-scale philophthalmosis outbreak in Portugal: inefficacy of common antihelminthic agents

Recent large-scale philophthalmosis outbreak in Portugal: inefficacy of common antihelminthic agents

A Comprehensive Chemical Characterization of in Situ Ophthalmic Gel

Ocular Disease Therapeutics: Design and Delivery of Drugs for Diseases of the Eye

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