In vitro and in vivo evaluation of in situ gelling systems for sustained topical ophthalmic delivery: state of the art and beyond

Destruel, Pierre-Louis; Zeng, Ni; Maury, Marc; Mignet, Nathalie; Boudy, Vincent

doi:10.1016/j.drudis.2016.12.008

Cited by 62 publications

(38 citation statements)

References 155 publications

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“…The sol–gel transition of in situ gelling polymers depends on one or a combination of different environmental triggers, such as changes in pH, temperature, and the presence of ions, that all influence polymer–polymer and polymer–solvent interactions . The development of in situ gel systems has received considerable attention over the past 25 years, sparked by the numerous advantages of such delivery systems. These include ease and reduced frequency of administration leading to improved patient compliance…”

Section: Introductionmentioning

confidence: 99%

Behavior of In Situ Cross‐Linked Hydrogels with Rapid Gelation Kinetics on Contact with Physiological Fluids

Diryak

Kontogiorgos

Ghori

et al. 2018

Macro Chemistry & Physics

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The impact of different physiological fluids on the rheological properties of gellan gum is investigated using a commercially available rheometer with a modified lower plate. The power of this method is demonstrated by measuring in real time, the rapid gelation kinetics, and gel strength of gellan gum exposed to simulated gastric fluid, lacrimal fluid, saliva, and wound fluid (all having a different ionic composition), highlighting potential use in the intelligent design of in situ gelling delivery systems. Changes in rheological behavior are examined in situ, gelation kinetics are modeled, and microstructure analyzed in the different simulated physiological environments.

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Section: Introductionmentioning

confidence: 99%

Behavior of In Situ Cross‐Linked Hydrogels with Rapid Gelation Kinetics on Contact with Physiological Fluids

Diryak

Kontogiorgos

Ghori

et al. 2018

Macro Chemistry & Physics

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“…Drug release from semi-solid dosage forms is complex, various mechanisms are involved (i.e., diffusion and erosion) and numerous evaluation methods have been described and developed to study these parameters [19,35]. The results below showed that in standard flow-through cells, on an FDA-approved USP 4 apparatus, in situ gelling delivery systems exhibited a fast but prolonged release over time ( Figure 1).…”

Section: In Vitro Drug Release Evaluation Using the Standard Flow-thrmentioning

confidence: 99%

In Situ Gelling Ophthalmic Drug Delivery System for the Optimization of Diagnostic and Preoperative Mydriasis: In Vitro Drug Release, Cytotoxicity and Mydriasis Pharmacodynamics

Destruel

Zeng²,

Brignole-Baudouin

et al. 2020

Pharmaceutics

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Mydriasis is required prior to many eye examinations and ophthalmic surgeries. Nowadays, phenylephrine hydrochloride (PHE) and tropicamide (TPC) are extensively used to induce mydriasis. Several pharmaceutic dosage forms of these two active ingredients have been described. However, no optimal therapeutic strategy has reached the market. The present work focuses on the formulation and evaluation of a mucoadhesive ion-activated in situ gelling delivery system based on gellan gum and hydroxyethylcellulose (HEC) for the delivery of phenylephrine and tropicamide. First, in vitro drug release was studied to assess appropriate sustained drug delivery on the ocular surface region. Drug release mechanisms were explored and explained using mathematical modeling. Then, in situ gelling delivery systems were visualized using scanning electron microscopy illustrating the drug release phenomena involved. Afterward, cytotoxicity of the developed formulations was studied and compared with those of commercially available eye drops. Human epithelial corneal cells were used. Finally, mydriasis intensity and kinetic was investigated in vivo. Mydriasis pharmacodynamics was studied by non-invasive optical imaging on vigilant rabbits, allowing eye blinking and nasolacrimal drainage to occur physiologically. In situ gelling delivery systems mydriasis profiles exhibited a significant increase of intensity and duration compared with those of conventional eye drops. Efficient mydriasis was achieved following the administration of a single drop of in situ gel reducing the required amount of administered active ingredients by four-to eight-fold compared with classic eye drop regimen.

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“…Simultaneously, Carbopol has excellent mucoadhesive properties and hence has been widely investigated for mucoadhesive ophthalmic drug delivery. [39][40][41] The mucoadhesive character of Carbopol is likely attributed to its ability to form strong hydrogen bonding, hydrophobic interactions, and electrostatic attractions with mucin present in the mucosal layer. [42,43] Currently, there are several commercial ophthalmic formulations based on Carbopol, including tear substitutes such as Lacrinorm, Lacrigel, or formulations containing the therapeutic agents Iduviran and Pilopine.…”

Section: Ph-sensitive Hydrogel For Ophthalmic Drug Deliverymentioning

confidence: 99%

Stimulus‐Responsive Hydrogel for Ophthalmic Drug Delivery

Lin

Lei

Shi

et al. 2019

Macromolecular Bioscience

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Blindness and vision impairment are major global health problems. Effective ophthalmic drug delivery poses a significant challenge because of protective physiological barriers and various biological clearance mechanisms that result in extremely low ocular bioavailability. Over the past several decades, several safe and effective ophthalmic drug delivery approaches have been promoted to combat these problems and to improve ocular bioavailability. Among these approaches, the stimulus‐responsive hydrogel for topical drug delivery has gained increasing attention because of its prolonged drug retention at the local site and enhanced ocular bioavailability. This review summarizes and presents recent advances and perspectives of a stimulus‐responsive hydrogel for ophthalmic drug delivery.

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In vitro and in vivo evaluation of in situ gelling systems for sustained topical ophthalmic delivery: state of the art and beyond

Cited by 62 publications

References 155 publications

Behavior of In Situ Cross‐Linked Hydrogels with Rapid Gelation Kinetics on Contact with Physiological Fluids

Behavior of In Situ Cross‐Linked Hydrogels with Rapid Gelation Kinetics on Contact with Physiological Fluids

In Situ Gelling Ophthalmic Drug Delivery System for the Optimization of Diagnostic and Preoperative Mydriasis: In Vitro Drug Release, Cytotoxicity and Mydriasis Pharmacodynamics

Stimulus‐Responsive Hydrogel for Ophthalmic Drug Delivery

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