New vehicle based on a microemulsion for topical ocular administration of dexamethasone

Fialho, Sílvia Ligório; Silva-Cunha, Armando

doi:10.1111/j.1442-9071.2004.00914.x

Cited by 150 publications

(84 citation statements)

References 20 publications

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“…The magnetic stirring speed was 100 rpm. At predetermined time points (2,4,6,8,10,12,24, and 36 h), 1 mL of each sample was withdrawn and immediately replaced with an equal volume of fresh Ringer's solution. The amount of drug released by L/NPs was determined by the HPLC method as described in the "Analysis of drug-loading efficiency and capacity" section.…”

Section: In Vitro Drug Release Testmentioning

confidence: 99%

“…Three methods are used for drug delivery to the posterior segment and fundus in clinical settings ( Figure 1). [1][2][3][4][5][6][7] The first method has been applied to the treatment of posterior segment disease and involves injection or implantation of the drug into the vitreous humor via the flat part of the ciliary body. The second method targets the subconjunctival fascia by implantation or injection, with the drug eventually becoming concentrated in the choroid, retinal pigment epithelium, retina, etc.…”

Section: Introductionmentioning

confidence: 99%

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Corneal permeation properties of a charged lipid nanoparticle carrier containing dexamethasone

Ban¹,

Zhang²,

Huang³

et al. 2017

IJN

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Drug delivery carriers can maintain effective therapeutic concentrations in the eye. To this end, we developed lipid nanoparticles (L/NPs) in which the surface was modified with positively charged chitosan, which engaged in hydrogen bonding with the phospholipid membrane. We evaluated in vitro corneal permeability and release characteristics, ocular irritation, and drug dynamics of modified and unmodified L/NPs in aqueous humor. The size of L/NPs was uniform and showed a narrow distribution. Corneal permeation was altered by the presence of chitosan and was dependent on particle size; the apparent permeability coefficient of dexamethasone increased by 2.7 and 1.8 times for chitosan-modified and unmodified L/NPs, respectively. In conclusion, a chitosan-modified system could be a promising method for increasing the ocular bioavailability of unmodified L/NPs by enhancing their retention time and permeation into the cornea. These findings provide a theoretical basis for the development of effective drug delivery systems in the treatment of ocular disease.

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Section: In Vitro Drug Release Testmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Corneal permeation properties of a charged lipid nanoparticle carrier containing dexamethasone

Ban¹,

Zhang²,

Huang³

et al. 2017

IJN

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“…Microemulsions (MEs) have a single optically isotropic, thermodynamically stable composites with a droplet diameter size usually within the range of 10 -100 nm (19). Microemulsions have very low surface tension and small droplet size, which lead to high absorption and permeation.…”

Section: Introductionmentioning

confidence: 99%

A Novel Microemulsion System for Ocular Delivery of Azithromycin: Design, Characterization and Ex-Vivo Rabbit Corneal Permeability

Salimi

Panahi-Bazaz

2017

Jundishapur J Nat Pharm Prod

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Background: The poor bioavailability of ophthalmic drops is mainly due to the rapid nasolacrimal drainage of the drug and very low permeability of corneal epithelium. Hence, there is an interest to find an effective system to improve drug permeability and bioavailability. Objectives: The aim of the present study was to design and characterize a novel microemulsion system as an ocular delivery system for Azithromycin and evaluate its physicochemical characteristics and rabbit corneal permeability in order to enhance the penetration of the drug. Methods: The prepared microemulsions (MEs) were assessed for their viscosity, pH, particle size, surface tension, DSC, stability, in vitro drug release, and corneal rabbit permeability. In this study, a full factorial design was employed with 3 variables at 2 levels for preparing 8 formulations and data analysis. Results:The results showed that the average droplet size of ME formulations was in the range of 6.78 to 26.65 nm while pH values were 5.1 to 5.7 and viscosity range was 115 -361 cps. Drug release profile revealed that 79.066% of the drug released in 24 hours of the experiment. The maximum and minimum percentages of drug permeated through rabbit cornea were observed in MEA-7 (12.87%) and MEA-2 (0.909%), respectively. All ME formulations with different compositions and properties significantly increased partitioning, flux, and permeability coefficient from rabbit cornea. Dapp and Papp parameters in MEA-1 and MEA-7 formulations were 0.00882 cm 2 h -1 and 2.391 cmh -1 , which were 17.65, 35.17 times higher than those of control (AZ suspension, 1%), respectively. The

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“…63 The instillation of dexamethasone-containing microemulsions in the eyes of rabbits has been shown to result in enhanced intraocular permeability. 64 Because sterilization is normally performed by autoclaving, microemulsions are unsuitable when the drug is water-soluble or insoluble (does not dissolve in water or oil), thermolabile, or if the drug should appear transparent externally. In comparison with microspheres and liposomes, microemulsions are also unsuitable for long-term sustained drug release.…”

Section: Other Nanocarriers Microemulsionsmentioning

confidence: 99%

Liposomes and nanotechnology in drug development: focus on ocular targets

Honda¹,

Asai²,

Oku³

et al. 2013

IJN

126

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Abstract:Poor drug delivery to lesions in patients' eyes is a major obstacle to the treatment of ocular diseases. The accessibility of these areas to drugs is highly restricted by the presence of barriers, including the corneal barrier, aqueous barrier, and the inner and outer blood-retinal barriers. In particular, the posterior segment is difficult to reach for drugs because of its structural peculiarities. This review discusses various barriers to drug delivery and provides comprehensive information for designing nanoparticle-mediated drug delivery systems for the treatment of ocular diseases. Nanoparticles can be designed to improve penetration, controlled release, and drug targeting. As highlighted in this review, the therapeutic efficacy of drugs in ocular diseases has been reported to be enhanced by the use of nanoparticles such as liposomes, micro/ nanospheres, microemulsions, and dendrimers. Our recent data show that intravitreal injection of targeted liposomes encapsulating an angiogenesis inhibitor caused significantly greater suppression of choroidal neovascularization than did the injection of free drug. Recent progress in ocular drug delivery systems research has provided new insights into drug development, and the use of nanoparticles for drug delivery is thus a promising approach for advanced therapy of ocular diseases.

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New vehicle based on a microemulsion for topical ocular administration of dexamethasone

Cited by 150 publications

References 20 publications

Corneal permeation properties of a charged lipid nanoparticle carrier containing dexamethasone

Corneal permeation properties of a charged lipid nanoparticle carrier containing dexamethasone

A Novel Microemulsion System for Ocular Delivery of Azithromycin: Design, Characterization and Ex-Vivo Rabbit Corneal Permeability

Liposomes and nanotechnology in drug development: focus on ocular targets

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