Ophthalmic drug delivery systems—Recent advances

Bourlais, Chrystèle Le; Acar, L.; Zia, Hossein; Sado, P. A.; Needham, Thomas E.; Leverge, R.

doi:10.1016/s1350-9462(97)00002-5

Cited by 627 publications

(355 citation statements)

References 125 publications

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“…The cornea is a significant mechanical and chemical obstacle and its main task is the safeguard of the intraocular tissues of the eye. The cornea is depicted by lipophilic and hydrophilic structures and reflects an effectual obstacle to the absorption of both hydrophilic and lipophilic molecules (2,3). Because of the tightness of the corneal barrier and quick loss of the instilled drug solution from the precorneal area, the bioavailability lessens.…”

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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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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“…For better ocular drug delivery, the drug should be both hydrophilic and lipophilic in nature. [150][151][152] Cyclodextrins complexes increase the aqueous solubility of some lipophilic drugs without altering the molecular structure and increase the ability to permeate through the biological membranes. Hydrophilic cyclodextrins, especially 2-hydroxypropyl-β-cyclodextrin and sulfobutyl-β-cyclodextrin, are nontoxic to the eye and are well tolerated in aqueous eye drop formulations.…”

Section: Cyclodextrin In Ocular Drug Deliverymentioning

confidence: 99%

Untitled

Budhwar¹

2018

AJP

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Inclusion complexes have various applications in different fields of drug delivery and pharmaceutical industry due to their ability of complexation with guest molecules and enhancement of the physicochemical properties of guest molecules. Cyclodextrins and their derivatives have the ability to encapsulate the bioactive compounds into its cavity and protect these from the environmental conditions, improve the solubility, bioavailability, and other properties also. The aim of this review is to highlight the advantages of cyclodextrins in the enhancement of physicochemical properties of drugs (such as solubility, stability, bioavailability, permeability, and others), different methods for production and various characterization techniques used for evaluation of complexes. Applications of cyclodextrin complexes in pharmaceutical and other fields are also explained here with examples. Thus cyclodextrins, because of their continuing ability to find several novel applications in drug delivery, are expected to solve many problems accompanied with the delivery of different novel drugs through various delivery routes.

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“…Já para o tratamento de doenças intraoculares, as diversas barreiras que o fármaco deve ultrapassar dificultam a obtenção de doses terapêuticas no tecido alvo, especialmente na retina e no vítreo. Estima-se que a absorção intraocular na câmara anterior seja entre 1 e 5% da dose administrada (4,6) . A drenagem do filme lacrimal, o reflexo de lacrimejamento e piscar no ato de instilar o colírio e o limitado volume da solução capaz de se manter no fundo do saco conjuntival eliminam rapidamente a maior parte da droga administrada.…”

Section: Via Tópica De Administração De Fármacos Para a Retina E Vítreounclassified

“…Géis oftálmicos são compostos hidrofílicos disponíveis em nosso meio como lubrificantes, pilocarpina e xilocaína. Os géis prolongam seu contato com a córnea por propriedades mucoadesivas decorrentes de sua elevada viscosidade e liberam o medicamento por difusão após erosão do polímero que se hidrolisa (4) . Os polímeros incluem ésteres de celulose, álcool polivinílico, carbopol, poliacrilamida, ácido hialurô-nico e ácido plurônico (2) .…”

Section: Via Tópica De Administração De Fármacos Para a Retina E Vítreounclassified

“…Além disso, medicamentos biológicos recentemente apresentados para os oftalmologistas possuem particularidades que precisam ser consideradas. A farmacologia ocular também lida com dificuldades específicas, seja em se obter amostras de tecidos ou fluidos intraoculares para determinação de concentrações de medicamentos administrados, seja para avaliar a toxicidade desses medicamentos quando administrados diretamente sobre a retina ou a necessidade de não interferir com as propriedades ópticas do olho (2)(3)(4) . O objetivo desse trabalho é fornecer uma atualização sobre farmacologia ocular, as principais medicações e suas vias de administração para o tratamento de doenças que acometem o segmento posterior do olho.…”

Section: Resumo Introduçãounclassified

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