Preservatives for Topical Ocular Drug Formulations

Velpandian, Thirumurthy

doi:10.1007/978-3-319-25498-2_16

Cited by 2 publications

(3 citation statements)

References 39 publications

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“…For the purpose of the study, batch size was 1 L for both formulations. Cetrimide at a concentration of 0.01% was chosen because it is a preservative commonly used for the antimicrobial preservation of ophthalmic solutions, with an efficacy similar to benzalkonium chloride [ 31 , 32 ].…”

Section: Methodsmentioning

confidence: 99%

Stability of Ophthalmic Atropine Solutions for Child Myopia Control

et al. 2020

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Myopia is an ophthalmic condition affecting more than 1/5th of the world population, especially children. Low-dose atropine eyedrops have been shown to limit myopia evolution during treatment. However, there are currently no commercial industrial forms available and there is little data published concerning the stability of medications prepared by compounding pharmacies. The objective of this study was to evaluate the stability of two 0.1 mg/mL atropine formulations (with and without antimicrobiobial preservatives) for 6 months in two different low-density polyethylene (LDPE) multidose eyedroppers. Analyses used were the following: visual inspection, turbidity, chromaticity measurements, osmolality and pH measurements, atropine quantification by a stability-indicating liquid chromatography method, breakdown product research, and sterility assay. In an in-use study, atropine quantification was also performed on the drops emitted from the multidose eyedroppers. All tested parameters remained stable during the 6 months period, with atropine concentrations above 94.7% of initial concentration. A breakdown product (tropic acid) did increase slowly over time but remained well below usually admitted concentrations. Atropine concentrations remained stable during the in-use study. Both formulations of 0.1 mg/mL of atropine (with and without antimicrobial preservative) were proved to be physicochemically stable for 6 months at 25 °C when stored in LDPE bottles, with an identical microbial shelf-life.

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Section: Methodsmentioning

confidence: 99%

Stability of Ophthalmic Atropine Solutions for Child Myopia Control

et al. 2020

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“…Preservatives exert important effects, including prevention of the microbial growth that can occur after opening a container of multidose eye medication, keeping the formulation free from contaminants, and improving the safety of the product. However, the majority of preservatives are associated with adverse effects, inducing toxicity to the ocular cells or hypersensitivity, 1 and have the potential to cause clinically relevant chronic or irreversible damage and ocular hyper-reactivity when used for long periods. [1][2][3] Microglycine (sodium hydroxymethylglycinate) is a small, pale-yellow, water-soluble compound, available commercially as an aqueous solution (mwater™) with buffering properties and known antimicrobial effect.…”

Section: Introductionmentioning

confidence: 99%

“…However, the majority of preservatives are associated with adverse effects, inducing toxicity to the ocular cells or hypersensitivity, 1 and have the potential to cause clinically relevant chronic or irreversible damage and ocular hyper-reactivity when used for long periods. [1][2][3] Microglycine (sodium hydroxymethylglycinate) is a small, pale-yellow, water-soluble compound, available commercially as an aqueous solution (mwater™) with buffering properties and known antimicrobial effect. 4 It is a derivative of the amino acid glycine and has broad-spectrum antimicrobial activity against both Gram-negative and Gram-positive bacteria, yeasts and moulds.…”

Section: Introductionmentioning

confidence: 99%

<p>Eye Irritation Potential of Microglycine and Microglycine-Containing Ointments: An in vitro Study on Reconstructed Human Corneal Epithelium</p>

Ceriotti¹,

Balzaretti²,

Barone³

et al. 2020

OPTH

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To assess the eye tolerability of a buffered ophthalmic solution containing microglycine (sodium hydroxymethylglycinate, mwater TM ) in an in vitro model. Materials and Methods: A multiple endpoint analysis (MEA) approach was applied to the reconstructed human corneal epithelium (HCE) model. Sodium hydroxymethylglycinate solution (0.04%) and two ophthalmic ointments containing microglycine (Protectorial, containing 0.02% of sodium hydroxymethylglycinate, and Edenight, containing 0.04% of sodium hydroxymethylglycinate) were investigated. The buffered solution and the ointments were tested on HCE after acute (one application in 24 hrs, followed or not by 16 hrs of recovery) or repeated (one application per day for three consecutive days) exposures; benzalkonium chloride (BAK) 0.01% and saline isotonic solution were used as positive and negative controls, respectively. Cellular viability, trans-epithelial electrical resistance (TEER), lactate dehydrogenase (LDH) release and histo-morphology were evaluated. Results: BAK 0.01% toxicity in HCE was confirmed for the 24+16 hrs acute and repeated exposure protocols, while, after 24-hours acute treatment, only modifications of the superficial cell layer were visible compared with the negative control. Sodium hydroxymethylglycinate had a very good tolerability profile and a neutral impact on the corneal surface after acute or repeated exposure. The Protectorial and Edenight ointments preserved cell viability in the different exposure protocols, suggesting a good local tolerability profile. Modifications of the superficial layers were observed on histo-morphological analysis and confirmed by increased release of LDH after 24+16 hrs acute exposure (+65% and +76% for Protectorial and Edenight, respectively) and TEER values after 24+16 hrs and 72 hrs exposure protocols. These results were dependent on the ointments' accumulation on the corneal epithelium due to their physical form (semi-solid) and lipophilic properties. Conclusion: Sodium hydroxymethylglycinate, alone or as part of eye ointments, was found to be non-toxic after acute or repeated exposure in the reconstructed HCE model.

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Preservatives for Topical Ocular Drug Formulations

Cited by 2 publications

References 39 publications

Stability of Ophthalmic Atropine Solutions for Child Myopia Control

Stability of Ophthalmic Atropine Solutions for Child Myopia Control

<p>Eye Irritation Potential of Microglycine and Microglycine-Containing Ointments: An in vitro Study on Reconstructed Human Corneal Epithelium</p>

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