Effects of Benzalkonium Chloride in Ophthalmic Eyedrop Medications on Corneal Epithelium

Seino, Satoshi; Takada, Yukihisa; Saika, Shizuya

doi:10.1248/yakushi.20-00177-1

Cited by 6 publications

(3 citation statements)

References 21 publications

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“…When engineered into nanoparticles, hyaluronate can serve as an effective vehicle for drug delivery, capable of encapsulating a wide array of anti-cancer agents. These nanoparticles can preferentially home in on osteosarcoma cells, exploiting the enhanced permeability and retention (EPR) effect commonly observed in tumor vasculature to facilitate selective drug accumulation at the tumor site [ 134 , 135 ]. Once at the tumor site, the nanoparticles are internalized by the cancer cells, where the encapsulated drugs are released to exert their therapeutic effects, thereby inhibiting the growth and metastasis of osteosarcoma cells.…”

Section: Resultsmentioning

confidence: 99%

Nano-Based Drug Delivery Systems: Potential Developments in the Therapy of Metastatic Osteosarcoma—A Narrative Review

Luo,

Sun,

Tan

et al. 2023

Pharmaceutics

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Osteosarcoma, a predominant malignant bone tumor, poses significant challenges due to its high metastatic and recurrent nature. Although various therapeutic strategies are currently in use, they often inadequately target osteosarcoma metastasis. This review focuses on the potential of nanoscale drug delivery systems to bridge this clinical gap. It begins with an overview of the molecular mechanisms underlying metastatic osteosarcoma, highlighting the limitations of existing treatments. The review then transitions to an in-depth examination of nanoscale drug delivery technologies, emphasizing their potential to enhance drug bioavailability and reduce systemic toxicity. Central to this review is a discussion of recent advancements in utilizing nanotechnology for the potential intervention of metastatic osteosarcoma, with a critical analysis of several preclinical studies. This review aims to provide insights into the potential applications of nanotechnology in metastatic osteosarcoma therapy, setting the stage for future clinical breakthroughs and innovative cancer treatments.

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Section: Resultsmentioning

confidence: 99%

Nano-Based Drug Delivery Systems: Potential Developments in the Therapy of Metastatic Osteosarcoma—A Narrative Review

Luo,

Sun,

Tan

et al. 2023

Pharmaceutics

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“…Hence, patients such as those with glaucoma and dry eye syndrome, who require the chronic administration of ophthalmic solutions, may suffer from BAC-induced damage of their corneal epithelium. [3][4][5] To avoid this, ophthalmic solutions not containing BAC are desired. Currently, some containers are used to negate the need for BAC in ophthalmic solutions.…”

Section: Introductionmentioning

confidence: 99%

New Candidate Preservative in Ophthalmic Solution Instead of Benzalkonium Chloride: 1,3-Didecyl-2-methyl Imidazolium Chloride

Iwasaki

Uchiyama

Nosaka

2023

CHEMICAL & PHARMACEUTICAL BULLETIN

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Benzalkonium chloride (BAC) is a useful preservative for ophthalmic solutions but has some disadvantageous effects on corneal epithelium, especially keratinocytes. Therefore, patients requiring the chronic administration of ophthalmic solutions may suffer from damage due to BAC, and ophthalmic solutions with a new preservative instead of BAC are desired. To resolve the above situation, we focused on 1,3-didecyl-2-methyl imidazolium chloride (DiMI). As a preservative for ophthalmic solutions, we evaluated the physical and chemical properties (absorption to a sterile filter, solubility, heat stress stability, and light/UV stress stability), and also the anti-microbial activity. The results indicated that DiMI was soluble enough to prepare ophthalmic solutions, and was stable under severe heat and light/UV conditions. In addition, the antimicrobial effect of DiMI as a preservative was considered to be stronger than BAC. Moreover, our in vitro toxicity tests suggested that DiMI is safer to humans than BAC. Considering the test results, DiMI may be an excellent candidate for a new preservative to replace BAC. If we can overcome manufacturing process issues (soluble time and flushing volume) and the insufficiency of toxicological information, DiMI may be widely adopted as a safe preservative, and immediately contribute to the increased well-being of all patients.

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“…The eye is a complex organ with highly specialized constituent tissues derived from different primordial cell lineages ( Hayashi, 2021 ). Currently, several corneal epithelial disorders such as oedema, blepharitis, glaucoma or the dry eye syndrome, represent the most common ophthalmic epithelial disorders ( Seino et al, 2021 ). Different corneal infections are reported worldwide, mainly caused by bacteria but also by viruses and, as the most recent pathogenic microorganisms, opportunistic free living protozoa such as Acanthamoeba spp.…”

Section: Introductionmentioning

confidence: 99%

In vitro amoebicidal effects of arabinogalactan-based ophthalmic solution

Reyes-Batllé

Rodríguez-Talavera

Sifaoui

et al. 2021

International Journal for Parasitology: Drugs and Drug Resistan

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The main corneal infections reported worldwide are caused by bacteria and viruses but, recently, the number of Acanthamoeba keratitis (AK) cases has increased. Acanthamoeba genus is an opportunistic free living protozoa widely distributed in environmental and clinical sources, with two life-cycle stages: the trophozoite and the cyst. AK presents as primary symptoms eye redness, epithelial defects, photophobia and intense pain. An early diagnosis and an effective treatment are crucial to avoid blindness or eye removal but, so far, there is no established treatment to this corneal infection. Diverse research studies have reported the efficacy of commercialized eye drops and ophthalmic solutions against the two life cycle stages of Acanthamoeba strains, that usually present preservatives such as Propylene Glycol of Benzalkonium chloride (BAK). These compounds present toxic effects in corneal cells, favouring the inflammatory response in the so sensitive eye tissue. In the present work we have evaluated the efficacy of nine proprietary ophthalmic solutions with and without preservatives (ASDA Dry Eyes Eyedrops, Miren®, ODM5®, Ectodol®, Systane® Complete, Ocudox®, Matrix Ocular®, Alins® and Coqun®) against the two life cycle stages of three Acanthamoeba strains. Our work has demonstrated the high anti- Acanthamoeba activity of Matrix Ocular®, which induces the programmed cell death mechanisms in Acanthamoeba spp. trophozoites. The high efficacy and the absence of ocular toxic effects of Matrix Ocular®, evidences the use of the Arabinogalactan derivatives as a new source of anti-AK compounds.

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Effects of Benzalkonium Chloride in Ophthalmic Eyedrop Medications on Corneal Epithelium

Cited by 6 publications

References 21 publications

Nano-Based Drug Delivery Systems: Potential Developments in the Therapy of Metastatic Osteosarcoma—A Narrative Review

Nano-Based Drug Delivery Systems: Potential Developments in the Therapy of Metastatic Osteosarcoma—A Narrative Review

New Candidate Preservative in Ophthalmic Solution Instead of Benzalkonium Chloride: 1,3-Didecyl-2-methyl Imidazolium Chloride

In vitro amoebicidal effects of arabinogalactan-based ophthalmic solution

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