Topical semi-solid drug delivery: kinetics and tolerance of ophthalmic hydrogels

Zignani, M.; Tabatabay, C.; Gurny, Robert

doi:10.1016/0169-409x(95)00015-y

Cited by 104 publications

(44 citation statements)

References 64 publications

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“…Systems with low viscosity allow good tolerance with little blinking pain. In contrast, systems with enhanced viscosity, although less tolerant, induce an increase in ocular contact time by reducing the drainage rate and, as a consequence, improve bioavailability (55). Viscosity of eyedrops is required to be not higher than 20.0 mPa s (56).…”

Section: Rheological Measurementsmentioning

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: Rheological Measurementsmentioning

confidence: 99%

Nanoemulsion as a Potential Ophthalmic Delivery System for Dorzolamide Hydrochloride

et al. 2009

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“…13 Realistically however, strategies such as reducing administered volume, increasing drug dosage and frequency of application and related strategies, although capable of improving drug effectiveness are difficult to achieve in practice. 2,5,7,14,15 Several attempts have been made to harness specific properties of macromolecules (viscosity modification, mucoadhesion and in-situ gelling 11,[16][17][18][19] ) to enhance interaction and retention of the drug with the anterior eye. The marked effect of viscosity increase 5 (0.9% saline < 1% methyl cellulose < 1.4% poly(vinyl alcohol) < petrolatum oil) on the reduction of tear film drainage is illustrated in Figure 1b.…”

Section: Introductionmentioning

confidence: 99%

The design of contact lens based ocular drug delivery systems for single-day use: Part (I) Structural factors, surrogate ophthalmic dyes and passive diffusion studies

Mahomed

Tighe

2014

J Biomater Appl

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The poor retention and efficacy of instilled drops as a means of delivering drugs to the ophthalmic environment is well-recognised. The potential value of contact lenses as a means of ophthalmic drug delivery and consequent improvement of pre-corneal retention is one obvious route to the development of a more effective ocular delivery system. Furthermore, the increasing availability and clinical use of daily disposable contact lenses provides the platform for the development of viable single-day use drug delivery devices based on existing materials and lenses. In order to provide a basis for the effective design of such devices, a systematic understanding of the factors affecting the interaction of individual drugs with the lens matrix is required. Because a large number of potential structural variables are involved it is necessary to achieve some rationalisation of the parameters and physicochemical properties (such as molecular weight, charge, partition coefficients) that influence drug interactions. Ophthalmic dyes and structurally related compounds based on the same core structure were used to investigate these various factors and the way in which they can be used in concert to design effective release systems for structurally different drugs. Initial studies of passive diffusional release form a necessary precursor to the investigation of the features of the ocular environment that over-ride this simple behaviour. Commercially available contact lenses of differing structural classifications were used to study factors affecting the uptake of the surrogate actives and their release under "passive" conditions. The interaction between active and lens material shows considerable and complex structure dependence which is not simply related to equilibrium water content (EWC). The structure of the polymer matrix itself was found to have the dominant controlling influence on active uptake; hydrophobic interaction with the ophthalmic dye playing a major role.3

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“…Because tears gave a pseudoplastic behavior, pseudoplastic vahicles would be more suitable as compare to Newtonian formulations, which have constant viscosity independent of the shear rate, whereas pseudoplastic solution exhibit decreased viscosity with increasing shear rate, therefore offering lowered viscosity during blinking and stability of the tear film during fixation. [18,19] Drug release from hydrogels [20] As discussed in the previous sections, hydrogels have a unique combination of characteristics that make them usefull in drug delivery applications. Due to their hydrophilicity, hydrogels…”

Section: In Situ Hydrogelsmentioning

confidence: 99%

Formulation and Evaluation of in Situ Ocular Gel for Dry Eye Syndrome

Kasliwal¹

2017

WJPR

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Ophthalmic drug delivery must be able to sustained the drug release and to remain in the vicinity in front of the eye for prolong period of time. The topical application of drugs is the method of choice under most circumstance because of its convenience and safety for ophthalmic chemotherapy. To develop the in situ ocular gel of a polymixin B sulphate which release the drug in sustained manner by using high esterified pure pectin, guar gum and hydroxyl propyl methylcellulose. Ocular in situ gel was prepared by dispersion method.In the present research work it can be shown that polymixin B sulphate, an antibacterial agent used in the treatment of dry eye syndrome was successfully formulated as an ion-activated in situ forming ophthalmic solution using pectin, guar gum in combination with HPMC as a viscosity enhancer. The in situ gel was subjected to content uniformity and was found to be between 97% to 98%. The developed formulation is a viable alternative of conventional eye drop due its ability to enhance bioavailability through its longer precorneal residence time and ability to sustain release drug.

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Topical semi-solid drug delivery: kinetics and tolerance of ophthalmic hydrogels

Cited by 104 publications

References 64 publications

Nanoemulsion as a Potential Ophthalmic Delivery System for Dorzolamide Hydrochloride

Nanoemulsion as a Potential Ophthalmic Delivery System for Dorzolamide Hydrochloride

The design of contact lens based ocular drug delivery systems for single-day use: Part (I) Structural factors, surrogate ophthalmic dyes and passive diffusion studies

Formulation and Evaluation of in Situ Ocular Gel for Dry Eye Syndrome

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