Comparison of Efficacy and Safety Evaluation of Latanoprost Formulations with and without Benzalkonium Chloride

Kasai, Hiroyoshi; Aoyama, Yumiko; Kurasawa, Takashi; Imamura, Tomoyo; Tsuruma, Kazuhiro; Hara, Hideaki; Hirata, Haruhisa; Yamamoto, Tetsuya

doi:10.4236/pp.2013.44054

Cited by 4 publications

(6 citation statements)

References 31 publications

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“…On one hand, beta-blockers are contraindicated for patients with asthma or with a history of cardiac disease. On the other hand, prostaglandin analogues rely on preservatives, such as benzalkonium chloride (BAK) or polyquaternium, for their solubilization which can cause redness of the eye as well as corneal inflammation upon repeated administration [7,[9][10][11][12][13][14]. The choice of treatment in the first intention is left to the practitioner, often leading to the use of prostaglandin analogues [8,15].…”

Section: Introductionmentioning

confidence: 99%

“…With current packaging technologies, such as single-dose or preservative-free eye drops (PFED) in multidose bottles, the use of preservatives is outdated. In terms of efficacy, PFED formulations are not inferior to formulas containing BAK [13]. Therefore, prostaglandin analogues are reformulated without the use of preservatives as stabilizers and solubilizers [10,16], often using ricin oil or propylene glycol as cosolvent [12].…”

Section: Introductionmentioning

confidence: 99%

“…Therefore, prostaglandin analogues are reformulated without the use of preservatives as stabilizers and solubilizers [10,16], often using ricin oil or propylene glycol as cosolvent [12]. Indeed, PFED formulations were shown to have a better ocular tolerance, especially regarding surface parameters such as an increased tear break-up time or less burning/stinging sensation upon instillation [11][12][13]. Better ocular tolerance is particularly important as it will lead to a better patient adherence and a more successful management of the IOP, hence delaying onset of irreversible symptoms such as vision loss.…”

Section: Introductionmentioning

confidence: 99%

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New Preservative-Free Formulation for the Enhanced Ocular Bioavailability of Prostaglandin Analogues in Glaucoma

Alviset

Corvis

Hammad³

et al. 2022

Pharmaceutics

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Glaucoma is a wide-spread eye disease caused by elevated intraocular pressure. Uncontrolled, this pressure may lead to damages to the optic nerve. Prostaglandin analogues, such as latanoprost and travoprost (which are water-insoluble active substances), are the most used class of active pharmaceutical ingredient. To administer them as eye drops, preservatives, such as benzalkonium chloride, are used as solubilizers. The latter is known to cause a local inflammation when used chronically and is not recommended for patients with ocular surface disorders. In this work, we sought to use polysorbate 80 (PS80) as a solubilizing agent simultaneously with sodium hyaluronate (NaHA) as a thickener and cytoprotective agent for the corneal surface. The first part of this study assessed the compatibility of the excipients with the active substance, using physicochemical methods such as spectra fluorescence and differential scanning calorimetry (DSC), as well as the solubilization mechanism of PS80 regarding prostaglandin analogues using nuclear magnetic resonance (NMR). The second part evaluated the stability of a formula candidate, its viscosity upon instillation, and its pharmacokinetic profile in rabbits as compared to the commercially approved medicine Travatan®. The results show that sodium hyaluronate is inert with respect to travoprost, while PS80 successfully solubilizes it, meaning that benzalkonium chloride is no longer required. Moreover, the pharmacokinetic profiles of the rabbits showed that the original formula described in the present study enhanced the ocular bioavailability of the drug, making it a promising product to control intraocular pressure with a potential reduced dosage of travoprost, therefore minimizing its related side effects.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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New Preservative-Free Formulation for the Enhanced Ocular Bioavailability of Prostaglandin Analogues in Glaucoma

Alviset

Corvis

Hammad³

et al. 2022

Pharmaceutics

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“…Although the majority of patients have elevated IOP, at least one-sixth of patients with POAG have IOP levels below 21 mm Hg, which is called normal-tension glaucoma (NTG). 2 , 6 …”

Section: Introductionmentioning

confidence: 99%

Intraocular Pressure Reduction Effect of 0.005% Latanoprost Eye Drops in a Hyaluronic Acid-Chitosan Nanoparticle Drug Delivery System in Albino Rabbits

Rubenicia

Cubillan

Sicam

et al. 2021

Trans. Vis. Sci. Tech.

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Purpose The purpose of this study was to evaluate the intraocular pressure (IOP) reduction efficiency of hyaluronic acid-chitosan-latanoprost link nanoparticle (HA-CS-latanoprost link NP) formulated eye drops. Methods The IOP reduction study was performed in 24 normotensive albino rabbits. The test animals were randomized and grouped accordingly to treatment namely, HA-CS-latanoprost link NP, plain latanoprost, and the commercially available Xalatan eye drop, all were formulated with 0.005% latanoprost. The 9 days of the experiment were divided into baseline period (days 1–2), treatment period (days 3–6), and recovery period (days 7–9). A wireless noncontact tonometer was used to measure IOP at a time interval of 2 hours for 12 hours per day with 5 readings each. Results The highest mean daily IOP reduction during the treatment period was 24% for plain latanoprost, 23% for Xalatan, and 29% for HA-CS-latanoprost link NP. The maximum reduction in IOP for plain latanoprost and Xalatan all occurred at the sixth hour with the peak effects of 4.85 mm Hg (37%) and 4.8 mm Hg (36%), respectively. Although HA-CS-latanoprost link NP had peak effects of 5.75 mm Hg (43%) at the sixth hour and 5.22 mm Hg (39%) at the eighth hour. Daily mean IOP measurements of each treatment group showed that HA-CS-latanoprost link NP has a greater IOP reduction effect compared with the other two treatments ( P < 0.001). Conclusions The results showed that the formulation of latanoprost with CS and HA is more effective in reducing the IOP than by drug alone. Translational Relevance The results provide evidence from animal experiment that HA-CS-latanoprost link NP formulation could improve and sustain drug concentration in the anterior segment of the eye. The improved reduction in IOP with that HA-CS-latanoprost link NP formulation can serve as a basis that latanoprost eye drops can be formulated with decreased concentration of benzalkonium HCl, an irritant preservative and penetration enhancer.

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“…Ocular drug delivery is one of the most appealing and arduous endeavours facing by the pharmaceutical scientist. The primitive ophthalmic solutions, suspensions and ointment dosage forms are unquestionably no longer satisfactory to combat some current virulent diseases 2,3 . An analysis write-up proclaims that almost 90% of ready for use ophthalmic formulations in the US, and an equivalent percentage is still supposedly valid for the present international trade.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Tafluprost Ophthalmic Solution

kumar¹,

Kumar²,

Rao³

2019

J. Drug Delivery Ther.

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The aim of the present study was to formulate, develop and evaluate ophthalmic solution containing Tafluprost. The selected prostaglandin analogue belongs to BCS - II. So to increase the solubility of the Tafluprost in WFI Beta Cyclodextrin was used by performing various trials variables of the experiments procedure Stirring time and speed were optimized to enhance the solubility. From the experimental procedure with different trails 20mg/mL of Cyclodextrins was fixed for the optimized formula. The product were characterized for appearance, physical state, colour and odour of the drug characteristics. The prepared formulations were evaluated for pH, osmolality and assay and found to be in acceptable ranges. Stability study was carried out for optimized formulation at 40°C±2°C /NMT 25%RH and 30°C ±2°C/ 65%±5% RH for 3 months, were evaluated for pH ,osmolality ,assay found to be within acceptable limits. Finally it can be concluded that the in house product Tafluprost ophthalmic solution was met with in the specification.

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Comparison of Efficacy and Safety Evaluation of Latanoprost Formulations with and without Benzalkonium Chloride

Cited by 4 publications

References 31 publications

New Preservative-Free Formulation for the Enhanced Ocular Bioavailability of Prostaglandin Analogues in Glaucoma

New Preservative-Free Formulation for the Enhanced Ocular Bioavailability of Prostaglandin Analogues in Glaucoma

Intraocular Pressure Reduction Effect of 0.005% Latanoprost Eye Drops in a Hyaluronic Acid-Chitosan Nanoparticle Drug Delivery System in Albino Rabbits

Formulation and Evaluation of Tafluprost Ophthalmic Solution

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