The potential of lipid emulsion for ocular delivery of lipophilic drugs

Shunmugaperumal, Tamilvanan; Benita, Simon

doi:10.1016/j.ejpb.2004.03.033

Cited by 139 publications

(73 citation statements)

References 57 publications

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“…Undiluted triacetin has no or only minor effect on the rabbit eye (34,35). On the other hand, Transcutol P and the amphoteric surfactant, Miranol C2M conc NP, are known as common emulsion excipients suitable for dissolving or dispersing lipophilic drugs in ocular preparations (42).…”

Section: Construction Of Pseudoternary-phase Diagramsmentioning

confidence: 99%

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: 99%

Nanoemulsion as a Potential Ophthalmic Delivery System for Dorzolamide Hydrochloride

et al. 2009

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“…Each formulation was tested on three albino rabbits; the experiment was performed by a single instillation (50 μl) of the niosomal preparation under test into the conjunctival sac of one eye, whilst the contralateral eye served as control. Both eyes of the rabbits under test were examined for any irritation signs, such as conjunctival: corneal edema and/or hyperemia on the basis of direct visual observation using a slit lamp, before treatment, and 1, 24 and 48 h after instillation (31,32). The animal experiments were conducted in full compliance with local, national, ethical and regulatory principles for animal care and was approved by the Cairo University Animal Care Committee…”

Section: Ocular Irritancy Test Of Niosome-encapsulated Gentamicinmentioning

confidence: 99%

Niosome-Encapsulated Gentamicin for Ophthalmic Controlled Delivery

2008

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Abstract. The objective of the present research was to investigate the feasibility of using non-ionic surfactant vesicles (niosomes) as carriers for the ophthalmic controlled delivery of a water soluble local antibiotic; gentamicin sulphate. Niosomal formulations were prepared using various surfactants (Tween 60, Tween 80 or Brij 35), in the presence of cholesterol and a negative charge inducer dicetyl phosphate (DCP) in different molar ratios and by employing a thin film hydration technique. The ability of these vesicles to entrap the studied drug was evaluated by determining the entrapment efficiency %EE after centrifugation and separation of the formed vesicles. Photomicroscopy and transmission electron microscopy as well as particle size analysis were used to study the formation, morphology and size of the drug loaded niosomes. Results showed a substantial change in the release rate and an alteration in the %EE of gentamicin sulphate from niosomal formulations upon varying type of surfactant, cholesterol content and presence or absence of DCP. In-vitro drug release results confirmed that niosomal formulations have exhibited a high retention of gentamicin sulphate inside the vesicles such that their in vitro release was slower compared to the drug solution. A preparation with 1:1:0.1 molar ratio of Tween 60, cholesterol and DCP gave the most advantageous entrapment (92.02%±1.43) and release results (Q 8h =66.29%±1.33) as compared to other compositions. Ocular irritancy test performed on albino rabbits, showed no sign of irritation for all tested niosomal formulations.

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“…LETT. 440 [12,13]. Direct contact of the drug with body fluids and tissues can be avoided, which means a minimization or significant decrease in side effects.…”

Section: Introductionmentioning

confidence: 99%

Emulsions of oil from Adenanthera pavonina L. seeds and their protective effect

Jaromin

Żarnowski

Kozubek

2006

Cellular and Molecular Biology Letters

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Abstract:In our previous study, we developed very stable formulations of submicron oil-in-water emulsions from Adenanthera pavonina L. (family Leguminosae, subfamily Mimosoideae) seed oil, stabilised with soybean lecithin (SPC). Continuing our research, we introduced an additional co-emulsifier, Tween 80, to those formulations in order to decrease the size of the emulsion particles and improve their stability. Formulations with a mean particle size ranging from 43.6 to 306.5 nm and a negative surface charge from -45.3 to -28.5 mV were obtained. Our stability experiments also revealed that most of the tested formulations had a very good degree of stability over a 3-month storage period, both at 4ºC and at room temperature. Since many intravenous injectable drugs exhibit lytic activity against erythrocytes, we examined this activity for the emulsion form of cardol, a natural compound with already proven hemolytic properties. The incorporation of this agent into the emulsion caused an evident decrease in hemolytic activity (97-99%). This highly protective effect, observed against sheep erythrocytes, was independent of both the composition and the particle size of the emulsions used. Our studies suggest that nonionic surfactant/phospholipid-based emulsions containing this edible oil of A. pavonina L. may be useful as an alternative formulation matrix for pharmaceutical, nutritional or cosmetic applications of otherwise membrane-acting components.

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The potential of lipid emulsion for ocular delivery of lipophilic drugs

Cited by 139 publications

References 57 publications

Nanoemulsion as a Potential Ophthalmic Delivery System for Dorzolamide Hydrochloride

Nanoemulsion as a Potential Ophthalmic Delivery System for Dorzolamide Hydrochloride

Niosome-Encapsulated Gentamicin for Ophthalmic Controlled Delivery

Emulsions of oil from Adenanthera pavonina L. seeds and their protective effect

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