Design and development of a novel pH triggered nanoemulsifiedin-situophthalmic gel of fluconazole:Ex-vivotranscorneal permeation, corneal toxicity and irritation testing

Pathak, Mukesh Kumar; Chhabra, Gulshan; Pathak, Kamla

doi:10.3109/03639045.2012.707203

Cited by 71 publications

(40 citation statements)

References 35 publications

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“…The LE-loaded nanoemulsion were formulated as per the experimental design employing a two-factor, three-level (3 2 ) factorial design by selecting the percentage of oil Capryol 90 (X 1 ) and S mix (X 2 ) as independent variables, while mean globule size are measured in nm (Y 1 ) and polydispersity index (Y 2 ) as responses (Ammar et al, 2010;Pathak et al, 2012). To recognize the significance of different independent variables on the experimental responses, response surface analyses were carried out.…”

Section: Formulation Of the Le-loaded Nanoemulsionmentioning

confidence: 99%

Development of loteprednol etabonate-loaded cationic nanoemulsified in-situ ophthalmic gel for sustained delivery and enhanced ocular bioavailability

et al. 2016

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A novel cationic nanoemulsified in-situ ophthalmic gel of loteprednol etabonate (LE) was developed to improve the permeability and retention time of formulations for overall improvement of drug's ocular bioavability. Capryol 90 (oil phase), tween 80 (surfactant) and transcutol P (cosurfactant) was selected as formulation excipients to construct pseudoternary phase diagrams and nanoemulsion region was recognized from diagrams. Spontaneous emulsification method was used to manufacture LE nanoemulsion and it was optimized using 3 2 factorial design by considering the amount of oil and the ratio of surfactant to cosurfactant (S mix ) as independent variables and evaluated for various physicochemical properties. Optimized NE was dispersed in Poloxamer 407 and 188 solution to form nanoemulsified sols that were predictable to transform into in-situ gels at corneal temperature. Drug pharmacokinetics of sterilized optimized in situ NE gel, NE-ISG2 [0.69% w/w Capryol 90, 0.99%w/w S mix (3:1), 13% Poloxamer 407, 4% w/w Poloxamer 188] and marketed formulation were assessed in rabbit aqueous humor. The in-situ gels were clear, shear thinning in nature and displayed zeroorder drug release kinetics. NE-ISG2 showed the minimum ocular irritation potential and significantly (p50.01) higher C max and AUC (0-10 h) , delayed T max , extended mean residence time and improved (2.54-fold times) bioavailability compared to marketed formulation. KeywordsLoteprednol etabonate, ocular cationic nanoemulsion, in-situ gel, ex vivo transcorneal permeation, pharmacokinetic study History

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Section: Formulation Of the Le-loaded Nanoemulsionmentioning

confidence: 99%

Development of loteprednol etabonate-loaded cationic nanoemulsified in-situ ophthalmic gel for sustained delivery and enhanced ocular bioavailability

et al. 2016

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“…Developed formulation did not damage ocular tissue and were nonirritating to ocular surface showed by HET-CAM test. The results showed higher in vitro efficacy, safety and patient compliance with higher permeation and precorneal residence time for treatment of fungal infection [65].…”

Section: Nanoemulsified In Situ Gelsmentioning

confidence: 97%

“…For ophthalmic delivery of fluconazole (FLZ), Pathak et al [65], developed a novel pH triggered nanoemulsified in situ gel (NE-ISG) for ocular delivery with enhanced residence time and permeation across ocular barrier for fungal infection. Optimized nanoemulsion (NE4) was prepared by spontaneous emulsification then nanoemulsified sol (NE-ISG1-NE-ISG5) were prepared by dispersing it in Carbopol 934 solution.…”

Section: Nanoemulsified In Situ Gelsmentioning

confidence: 99%

Newer Trends in In Situ Gelling Systems for Controlled Ocular Drug Delivery

Jain¹,

Kumar²,

Singh³

et al. 2016

JAPLR

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In situ -gelling systems has the great potential in the wide areas of drug delivery. The application areas of such systems are broad and these systems can be formulated not only as gels but also as in situ gelling nanospheres, microspheres and liposomes. To overcome the drawbacks associated with conventional drug delivery systems and take advantages of both solutions and gels, such as accurate dosing, ease of administration of the former and longer precorneal residence of the latter, a newer concept of in situ gelling drug delivery systems was came in light for the first time in the early 1980s. In situ gelling systems are the polymeric solutions which can be administered in solution form and immediately undergoes sol-gel phase transition in to a viscoelastic gel upon exposure to physiological conditions (e.g. pH, temperature and ionic concentration) or application of external triggers. In situ gelling systems seems to have wide applications in ocular therapy. A lot of research is going on in this area proves the fact that in situ gelling systems can be advantageous in the ocular drug delivery. In the present review we will discuss recent researches involving application of in situ gelling polymers, their applications in the various domains of drug delivery and marketed formulations based on in situ gelling systems.

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“…The shear stress of the sample solutions was measured at different shear rates (6,12,20,30,40, 60 rpm) under physiological conditions (35±0.1°C) and non-physiological conditions (25±0.1°C). To simulate the physiological eye environment of the gels, the thermosensitive gels were diluted with artificial tears (STF) at a ratio of 40 : 7 before the rheological studies were conducted at 35±0.1°C.…”

Section: Experimental Materialsmentioning

confidence: 99%

“…Hence, the absorption of the ophthalmic drug is severely limited, resulting in poor ocular bioavailability. 6) Moreover, a small amount of the drug passes from the nasolacrimal duct into the gastrointestinal tract causing systemic toxicity. 7) Thus, frequent application of the eye drops is necessary to maintain therapeutic ocular bioavailability; but the frequent use of high concentration solutions may induce both ocular and systemic side effects.…”

mentioning

confidence: 99%

Design and Evaluation of a Brinzolamide Drug–Resin in Situ Thermosensitive Gelling System for Sustained Ophthalmic Drug Delivery

Hua

Liu

et al. 2014

Chem. Pharm. Bull.

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In this study a brinzolamide drug-resin ophthalmic thermosensitive in situ gelling system was developed and evaluated. Brinzolamide was combined with ion exchange resins to prolong the retention time of drugs in the eye and to reduce ocular and systemic side effects. Poloxamer F127 was used as gelling vehicle in combination with carbopol 934P, which acted as a viscosity-enhancing agent. They were prepared using the cold method. The optimized formulation exhibited a sol-gel transition at 33.2 1.1°C with pseudoplastic flow behavior. This formulation was stable and nonirritant to rabbit eyes. In vitro release studies demonstrated diffusion-controlled release of brinzolamide from the combined solutions over a period of 8 h. In vivo evaluation (the elimination of brinzolamide through tears and absorption of brinzolamide in aqueous humor) indicated that the solution combination was better able to retain the drug than commercial preparations. Thus this formulation is safe for ophthalmic use and significantly increases brinzolamide bioavailability in aqueous humor.

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Design and development of a novel pH triggered nanoemulsifiedin-situophthalmic gel of fluconazole:Ex-vivotranscorneal permeation, corneal toxicity and irritation testing

Cited by 71 publications

References 35 publications

Development of loteprednol etabonate-loaded cationic nanoemulsified in-situ ophthalmic gel for sustained delivery and enhanced ocular bioavailability

Development of loteprednol etabonate-loaded cationic nanoemulsified in-situ ophthalmic gel for sustained delivery and enhanced ocular bioavailability

Newer Trends in In Situ Gelling Systems for Controlled Ocular Drug Delivery

Design and Evaluation of a Brinzolamide Drug–Resin <i>in Situ</i> Thermosensitive Gelling System for Sustained Ophthalmic Drug Delivery

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