Gelrite®: A novel, ion-activated, in-situ gelling polymer for ophthalmic vehicles. Effect on bioavailability of timolol

Rozier, Annouk; Mazuel, Claude; Grove, Jeffrey; Plazonnet, Bernard

doi:10.1016/0378-5173(89)90305-0

Cited by 248 publications

(93 citation statements)

References 8 publications

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“…In vitro release of timolol from GG gelled solutions was retarded and controlled by drug diffusion in the gel. Accordingly, in vivo the formation of the gel prolonged the precorneal residence time, and therefore, it increased the ocular bioavailability of timolol in the cornea, aqueous humor and iris+ciliary body of rabbits (Rozier et al, 1989). A similar in situ-gelling behaviour and in vitro release of the antibacterial agent pefloxacin was reported of a 0.6% GG solution.…”

Section: Gellan Gumsupporting

confidence: 51%

Polysaccharides as Excipients for Ocular Topical Formulations

Zambito¹,

Colo²

2011

Biomaterials Applications for Nanomedicine

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Section: Gellan Gumsupporting

confidence: 51%

Polysaccharides as Excipients for Ocular Topical Formulations

Zambito¹,

Colo²

2011

Biomaterials Applications for Nanomedicine

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“…This problem can be overcome using in situ gel-forming drug delivery systems prepared from polymers that exhibit sol-to-gel phase transitions due to a change in a specific physicochemical parameter in the cul-de-sac (7). In the past few years, an impressive number of pH (e.g., cellulose acetate phthalate and Carbopol), temperature (e.g., Poloxamer), and ion (e.g., gellan gum and alginate) induced in situ forming systems have been reported to sustain ophthalmic drug delivery (8)(9)(10)(11). These in situ gel-forming systems could prolong the precorneal residence time of a drug (12)(13)(14)(15)(16) and improve ocular bioavailability (17).…”

Section: Introductionmentioning

confidence: 99%

“…Deacetylated gellan gum (an exocellular polysaccharide of microbial origin, commercially available as Gelrite ® ) is an interesting in situ gelling polymer that has been tested since it seems to perform very well in humans (10,18). Preparations of Gelrite are dropped into eyes; gel formation takes place, induced by the electrolytes of the tear fluid (19).…”

Section: Introductionmentioning

confidence: 99%

In Situ Gelling Gelrite/Alginate Formulations as Vehicles for Ophthalmic Drug Delivery

et al. 2010

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Abstract. The objective of this study was to develop an ion-activated in situ gelling vehicle for ophthalmic delivery of matrine. The rheological properties of polymer solutions, including Gelrite, alginate, and Gelrite/alginate solution, were evaluated. In addition, the effect of formulation characteristics on in vitro release and in vivo precorneal drug kinetic of matrine was investigated. It was found that the optimum concentration of Gelrite solution for the in situ gel-forming delivery systems was 0.3% (w/w) and that for alginate solution was 1.4% (w/w). The mixture of 0.2% Gelrite and 0.6% alginate solutions showed a significant enhancement in gel strength at physiological condition. On the basis of the in vitro results, the Gelrite formulations of matrine-containing alginate released the drug most slowly. For each tested polymer solution, the concentration of matrine in the precorneal area was higher than that of matrinecontaining simulated tear fluid (STF) almost at each time point (p<0.05). The area under the curve of formulation 16 (0.2%Gelrite/0.6%alginate) was 4.65 times greater than that of containing matrine STF. Both the in vitro release and in vivo pharmacological studies indicated that the Gelrite/alginate solution had the better ability to retain drug than the Gelrite or alginate solutions alone. The tested formulation was found to be almost non-irritant in the ocular irritancy test. The overall results of this study revealed that the Gelrite/alginate mixture can be used as an in situ gelling vehicle to enhance ocular retention.

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“…Microparticles display per se a prolonged residence time on mucosal membranes compared to single-unit dosage forms (Rozier et al, 1989). This residence time at mucosal membranes is even further improved when they exhibit mucoadhesive properties.…”

Section: Introductionmentioning

confidence: 95%

Insulin delivery through nasal route using thiolated microspheres

Nema

Jain

et al. 2013

Drug Delivery

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The aim of the present study was to investigate the potential of developed thiolated microspheres for insulin delivery through nasal route. In the present study, cysteine was immobilized on carbopol using EDAC. A total of 269.93 mmol free thiol groups per gram polymer were determined. The prepared nonthiolated and thiolated microspheres were studied for particle shape, size, drug content, swellability, mucoadhesion and in vitro insulin release. The thiolated microspheres exhibited higher mucoadhesion due to formation of covalent bonds via disulfide bridges with the mucus gel layer. Drug permeation through goat nasal mucosa of nonthiolated and thiolated microspheres were found as 52.62 AE 2.4% and 78.85 AE 3.1% in 6 h, respectively. Thiolated microspheres bearing insulin showed better reduction in blood glucose level (BGL) in comparison to nonthiolated microspheres as 31.23 AE 2.12% and 75.25 AE 0.93% blood glucose of initial BGL were observed at 6 h after nasal delivery of thiolated and nonthiolated microspheres in streptozotocin-induced diabetic rabbits.

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Gelrite®: A novel, ion-activated, in-situ gelling polymer for ophthalmic vehicles. Effect on bioavailability of timolol

Cited by 248 publications

References 8 publications

Polysaccharides as Excipients for Ocular Topical Formulations

Polysaccharides as Excipients for Ocular Topical Formulations

In Situ Gelling Gelrite/Alginate Formulations as Vehicles for Ophthalmic Drug Delivery

Insulin delivery through nasal route using thiolated microspheres

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