Propylenglycol a new osmotic agent for ophthalmic uses

Bietti, G. B.; Virno, M; Pecori-Giraldi, J

doi:10.1007/bf00151798

Cited by 9 publications

(10 citation statements)

References 5 publications

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“…Solutions of up to 50% propylene glycol caused no irritations to the rabbit eye, whereas the undiluted application was associated with a weak conjunctival redness (40,41). Triacetin, as reported by Hughes (33), is well tolerated by the rabbit eye.…”

Section: Construction Of Pseudoternary-phase Diagramsmentioning

confidence: 59%

Nanoemulsion as a Potential Ophthalmic Delivery System for Dorzolamide Hydrochloride

et al. 2009

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Abstract. Dilutable nanoemulsions are potent drug delivery vehicles for ophthalmic use due to their numerous advantages as sustained effect and high ability of drug penetration into the deeper layers of the ocular structure and the aqueous humor. The aim of this article was to formulate the antiglaucoma drug dorzolamide hydrochloride as ocular nanoemulsion of high therapeutic efficacy and prolonged effect. Thirty-six systems consisting of different oils, surfactants, and cosurfactants were prepared and their pseudoternary-phase diagrams were constructed by water titration method. Seventeen dorzolamide hydrochloride nanoemulsions were prepared and evaluated for their physicochemical and drug release properties. These nanoemulsions showed acceptable physicochemical properties and exhibited slow drug release. Draize rabbit eye irritation test and histological examination were carried out for those preparations exhibiting superior properties and revealed that they were nonirritant. Biological evaluation of dorzolamide hydrochloride nanoemulsions on normotensive albino rabbits indicated that these products had higher therapeutic efficacy, faster onset of action, and prolonged effect relative to either drug solution or the market product. Formulation of dorzolamide hydrochloride in a nanoemulsion form offers, thus, a more intensive treatment of glaucoma, a decrease in the number of applications per day, and a better patient compliance compared to conventional eye drops.

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Section: Construction Of Pseudoternary-phase Diagramsmentioning

confidence: 59%

Nanoemulsion as a Potential Ophthalmic Delivery System for Dorzolamide Hydrochloride

et al. 2009

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“…Fialho et al used Cremophor EL at a concentration of 15% in their ophthalmic ME formulation as a safe administration of dexamethasone to the eye . Also, they stated that according to the information provided by the manufacturer, Cremophor EL at a concentration up to 30% does not have any irritant effect on the eye. , Furthermore, a solution of propylene glycol is safe and causes no irritations to the rabbit eye at a concentration up to 50%, whereas undiluted propylene glycol only associated with a weak conjunctival redness. ,, Similarly, Liu et al reported that Labrasol at a concentration of 5% produced a slight ocular irritation when used as ophthalmic penetration enhancer for their drug (baicalin) . Despite using Labrasol as a surfactant in our ME at a concentration above the limit that was previously reported, our results demonstrate that it does not produce any ocular irritation at all.…”

Section: Resultsmentioning

confidence: 99%

“…43,44 Furthermore, a solution of propylene glycol is safe and causes no irritations to the rabbit eye at a concentration up to 50%, whereas undiluted propylene glycol only associated with a weak conjunctival redness. 42,45,46 Similarly, Liu et al reported that Labrasol at a concentration of 5% produced a slight ocular irritation when used as ophthalmic penetration enhancer for their drug (baicalin). 47 Despite using Labrasol as a surfactant in our ME at a concentration above the limit that was previously reported, our results demonstrate that it does not produce any ocular irritation at all.…”

Section: Ternary and Pseudo-ternary Phase Diagrams And Preparation Of Multiple W/o/w Me Eye Dropsmentioning

confidence: 99%

Once Daily Pregabalin Eye Drops for Management of Glaucoma

et al. 2019

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Elevated intraocular pressure (IOP) is the most significant risk factor contributing to visual field loss in glaucoma. Unfortunately, the deficiencies associated with current therapies have resulted in reduced efficacy, several daily dosings, and poor patient compliance. Previously, we identified the calcium voltage-gated channel auxiliary subunit alpha2delta 1 gene (Cacna2d1) as a modulator of IOP and demonstrated that pregabalin, a drug with high affinity and selectivity for CACNA2D1, lowered IOP in a dose-dependent manner. Unfortunately, IOP returned to baseline at 6 h after dosing. In the current study, we develop a once daily topical pregabalin-loaded multiple water-inoil-in-water microemulsion formulation to improve drug efficacy. We characterize our formulations using multiple in vitro and in vivo evaluations. Our lead formulation provides continuous release of pregabalin for up to 24 h. Because of its miniscule droplet size (<20 nm), our microemulsion has a transparent appearance and should not blur vision. It is also stable at one month of storage at temperatures ranging from 5 to 40 °C. Our formulation is nontoxic, as illustrated by a cell toxicity study and slit-lamp biomicroscopic exams. CACNA2D1 is highly expressed in both the ciliary body and the trabecular meshwork, where it functions to modulate IOP. A single drop of our lead pregabalin formulation reduces IOP by greater than 40%, which does not return to baseline until >30 h post-application. Although there were no significant differences in the amplitude of IOP reduction between the formulations we tested, a significant difference was clearly observed in their duration of action. Our multilayered microemulsion is a promising carrier that sustains the release and prolongs the duration of action of pregabalin, a proposed glaucoma therapeutic.

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“…The ophthalmologic tolerance of these substances (except for water and everolimus) has been demonstrated. [13][14][15][16][17][18][19][20] Currently, there is no topical eye-applicable formulation available for use on patients that contains one of the new immunosuppressants.…”

Section: Introductionmentioning

confidence: 99%