Novel in situ gelling ophthalmic drug delivery system based on gellan gum and hydroxyethylcellulose: Innovative rheological characterization, in vitro and in vivo evidence of a sustained precorneal retention time

Destruel, Pierre-Louis; Zeng, Ni; Séguin, Johanne; Douat, Sophie; Rosa, Frédéric; Brignole‐Baudouin, Françoise; Dufaÿ, Sophie; Dufaÿ-Wojcicki, Amélie; Maury, Marc; Mignet, Nathalie; Boudy, Vincent

doi:10.1016/j.ijpharm.2019.118734

Cited by 41 publications

(36 citation statements)

References 53 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The ease of administration in case of a highly viscous solution and gel forms retard its use and patient compliance. The blurred vision and the lachrymation are associated with the dosage form involving hydrogel (Destruel et al, 2020). The clarity of the developed in situ gels followed by visual observation in the black and white background was satisfactory and in the desirable limits.…”

Section: Resultsmentioning

confidence: 99%

In vitro–in vivo evaluation of tetrahydrozoline‐loaded ocular in situ gels on rabbits for allergic conjunctivitis management

Okur

Yozgatlı

Okur

2020

Drug Development Research

View full text Add to dashboard Cite

Ocular allergy is one of the most common disorders of the eye surface. The conventional eye drops lack of therapeutic efficacy due to low ocular bioavailability and decreased drug residence time on eye surface. Hence, the present research work aimed to formulate, optimize, and evaluate the in situ gel for ophthalmic drug delivery. The prepared in situ gel formulations were evaluated for clarity, pH, gelling capacity, viscosity, osmolality, in vitro release study, and kinetic evaluation. ex vivo corneal permeation/penetration study using goat and in vivo studies on rabbits were also performed. Fourier‐transformed infrared spectroscopy was also applied to study possible interactions between drug and polymers. The formulations found to be stable, nonirritant, and showed sustained release of the drug for a period of up to 24 hr with no ocular damage. The developed in situ gels loaded with tetrahydrozoline are alternative and promising ocular candidates for the treatment of allergic conjunctivitis.

show abstract

Section: Resultsmentioning

confidence: 99%

In vitro–in vivo evaluation of tetrahydrozoline‐loaded ocular in situ gels on rabbits for allergic conjunctivitis management

Okur

Yozgatlı

Okur

2020

Drug Development Research

View full text Add to dashboard Cite

show abstract

“…In a previous work [13], the physico-chemical, rheological and mucoadhesive properties of the in situ gelling delivery systems were characterized. The three formulations exhibited suitable pH (6.4 to 6.6), osmolality (429 to 443 mOsm/kg), and transmittance (>90%) for ophthalmic use.…”

Section: Resultsmentioning

confidence: 99%

“…The hydrogels were prepared as in our previous work [13]. Final concentrations are reminded in Table 1.…”

Section: In Situ Gelling Formulationsmentioning

confidence: 99%

“…To overcome the drawbacks of existing dosage forms and meet an important need of clinicians and patients, a novel mydriatic in situ gelling delivery system was developed [13]. Many investigators have considered the use of in situ gelling delivery systems as a promising way to achieve efficient topical ophthalmic drug delivery [14].…”

Section: Introductionmentioning

confidence: 99%

“…In a previous work [13], three formulations of in situ gelling delivery systems were developed and characterized rheologically. Their extended retention time was then assessed in vivo.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

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

Self Cite

View full text Add to dashboard Cite

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.

show abstract

Biopolymer‐Based Scaffolds for Bone and Tissue Engineering

Sweety¹,

Selvasudha²,

Dhanalekshmi³

et al. 2021

Nanoengineering of Biomaterials

View full text Add to dashboard Cite

Novel in situ gelling ophthalmic drug delivery system based on gellan gum and hydroxyethylcellulose: Innovative rheological characterization, in vitro and in vivo evidence of a sustained precorneal retention time

Cited by 41 publications

References 53 publications

In vitro–in vivo evaluation of tetrahydrozoline‐loaded ocular in situ gels on rabbits for allergic conjunctivitis management

In vitro–in vivo evaluation of tetrahydrozoline‐loaded ocular in situ gels on rabbits for allergic conjunctivitis management

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

Biopolymer‐Based Scaffolds for Bone and Tissue Engineering

Contact Info

Product

Resources

About