DESIGN, DEVELOPMENT AND EVALUATION OF CATIONIC GUAR AND HYDROXYPROPYL GUAR BASED IN SITU GELS FOR OPHTHALMIC DRUG DELIVERY

The poor bioavailability and therapeutic response exhibited by the conventional eye drops due to rapid corneal loss is overcome by the use of ion-activated gel forming systems that are instilled as drops;these undergo gelation in cul-de-sac mode. The present study describes the design, development and evaluation of in situ ophthalmic drug delivery of antibacterial agent, linezolid, based on ion-activated guar gum derivatives. Novel polymers such as Cationic guar with hydroxypropyl guar are being used as gelling as well as viscosity enhancing agents. Differential scanning calorimetric studies have revealed that linezolid is compatible with all the excipients in the formulation. The study also aims at rheological characterization, effect of sterilization (moist heat) and effect of aging on the viscosity of in situ gels by calculating consistency index (K), flow behaviour index (n value) using power law model. The in vitro drug diffusion study for the developed formulations has also been carried out. The formulation CGHPG2,exhibiting good physical stability subsequent to sterilization and storage and further retaining the consistency index (K) and flow behavior index (n value), was chosen as the optimized formulation. The gel formed in situ revealed the sustained release of the drug for up to 12 hrs. Stability data recorded over a period of 6 months at elevated temperature conditions revealed the formulation to be stable. In vivo ocular toxicity studies revealed non irritant and non toxic nature of the formulation. Therefore, the developed guar gum derivative based ophthalmic in situ gel by virtue of its prolonged corneal residence time and sustained drug release could be considered a viable alternative to the conventional eye drop formulation in achieving enhanced bioavailability.

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Gel-Based Materials for Ophthalmic Drug Delivery

Gels ◽

10.3390/gels7030130 ◽

2021 ◽

Vol 7 (3) ◽

pp. 130

Author(s):

Roberta Cassano ◽

Maria Luisa Di Gioia ◽

Sonia Trombino

Keyword(s):

Drug Delivery ◽

Side Effects ◽

Contact Lenses ◽

Prolonged Release ◽

Eye Drops ◽

Non Invasive ◽

Ophthalmic Drug Delivery ◽

Ophthalmic Drug ◽

In Situ Gelling

The most common route of administration of ophthalmic drugs is the topical route because it is convenient, non-invasive, and accessible to all patients. Unfortunately, drugs administered topically are not able to reach effective concentrations. Moreover, their bioavailability must be improved to decrease the frequency of administrations and their side effects, and to increase their therapeutic efficiency. For this purpose, in recent decades, particular attention has been given to the possibility of developing prolonged-release forms that are able to increase the precorneal residence time and decrease the loss of the drug due to tearing. Among these forms, gel-based materials have been studied as an ideal delivery system because they are an extremely versatile class with numerous prospective applications in ophthalmology. These materials are used in gel eye drops, in situ gelling formulations, intravitreal injections, and therapeutic contact lenses. This review is intended to describe gel-based materials and their main applications in ophthalmology.

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An Insight into Ophthalmic Drug Delivery System

International Journal of Pharmaceutical Sciences and Drug Research ◽

10.25004/ijpsdr.2009.010101 ◽

2009 ◽

Vol 1 (01) ◽

Cited By ~ 1

Author(s):

Rathore K. S. ◽

Nema R. K.

Keyword(s):

Drug Delivery ◽

Topical Administration ◽

Eye Drops ◽

In Situ Gel ◽

Ophthalmic Drug Delivery ◽

Ophthalmic Drug ◽

Ophthalmic Therapy ◽

Ocular Therapy ◽

Insight Into

Promising management of eye ailments take off effective concentration of drug at the eye for sufficient period of time. Dosage forms are administered directly to eye for localized ophthalmic therapy. Most of the treatments call for the topical administration of ophthalmic active drugs to the tissues around the ocular cavity. Conventional ophthalmic drug delivery systems including eye drops, ophthalmic ointments, are no longer sufficient to encounter eye diseases. This article reviews the constraints with conventional ocular therapy and explores various novel approaches like in-situ gel, ocular films or ocuserts, nanosuspension, collagen shields, latex systems, nanoparticles, liposomes, niosomes, iontophorosis, eye implants, etc to improve the ophthalmic bioavailability of drugs to the anterior chamber of the eye.

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Effect of xanthan gum and guar gum on in situ gelling ophthalmic drug delivery system based on poloxamer-407

International Journal of Biological Macromolecules ◽

10.1016/j.ijbiomac.2013.08.024 ◽

2013 ◽

Vol 62 ◽

pp. 117-123 ◽

Cited By ~ 55

Author(s):

Manas Bhowmik ◽

Puja Kumari ◽

Gunjan Sarkar ◽

Mrinal Kanti Bain ◽

Biplab Bhowmick ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Xanthan Gum ◽

Guar Gum ◽

Poloxamer 407 ◽

Ophthalmic Drug Delivery ◽

Ophthalmic Drug ◽

In Situ Gelling

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pH Triggered In-situ Gelling Ophthalmic Drug Delivery System

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v8i01.11900 ◽

2018 ◽

Vol 8 (01) ◽

Author(s):

Kurniawansyah I S ◽

Rahmi F ◽

Sopyan I

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

The Body ◽

Eye Drops ◽

Ophthalmic Drug Delivery ◽

Short Period ◽

Ophthalmic Drug ◽

In Situ Gelling

Eyes are delicate and most vital organs of the body whose defence mechanism restricts entry of exogenous substance. Conventional drug delivery systems get washed off within a short period of time that usually cause poor bioavailability and therapeutic responses because high tear fluid turnover and dynamics cause rapid elimination of the drug from the eye. In-situ gelling ophthalmic drug delivery system is one of the new methods that is developed to overcome this bioavailability problems. In-situ gelling systems are viscous polymerbased liquids that exhibit sol-to-gel phase transition on the ocular surface due to a change in a specific physicochemical parameter like temperature, ionic strength, or pH triggered in-situ systems. Using this formulation of pH triggered in-situ gel systems, the release of drug can be sustained for longer periods of time, therapeutically more efficacious, non-irritant and stable than conventional eye drops.

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DEVELOPMENT, EVALUATION AND CHARACTERISTICS OF OPHTHALMIC IN SITU GEL SYSTEM: A REVIEW

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2019v11i4.34949 ◽

2019 ◽

pp. 47-53 ◽

Cited By ~ 1

Author(s):

MRINMOY DEKA ◽

ABDUL BAQUEE AHMED ◽

JASHOBIR CHAKRABORTY

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Temperature Modulation ◽

Duration Of Action ◽

In Situ Gel ◽

Ophthalmic Drug Delivery ◽

Sensitive Organ ◽

Ophthalmic Drug

Eye is a sensitive organ and is easily injured and infected. Delivery of drugs into eye is complicated due to removal mechanism of precorneal area results decrease in therapeutic response. Conventional ocular delivery systems like solution, suspension, ointment shows some disadvantages such as rapid corneal elimination, repeated instillation of drug and short duration of action. In situ polymeric delivery system will help to achieve optimal concentration of drug at the target site, thereby helps to achieve the desired therapeutic concentration. There are various novel ocular drug delivery systems such as In-situ gel, dendrimers, niosomes, nanoparticulate system, collagen shield, ocular iontophoresis suspension and ocusert etc. In situ gelling systems are liquid upon instillation and undergo a phase transition to form gel due to some stimuli responses such as temperature modulation, change in pH and presence of ions. Various attempts have been made towards the development of stable sustained release in-situ gels. Newer research in ophthalmic drug delivery systems is directed towards an incorporation of several drug delivery technologies, that includes to build up systems which is not only extend the contact time of the vehicle at the ocular surface, but which at the same time slow down the removal of the drug. This is a review based on ocular in situ gels, characteristization, techniques and evaluation of in situ ophthalmic drug delivery systems,

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The Effect of Photoinitiator Concentration on the Physicochemical Properties of Hydrogel Contact Lenses

Applied Mechanics and Materials ◽

10.4028/www.scientific.net/amm.679.118 ◽

2014 ◽

Vol 679 ◽

pp. 118-127 ◽

Cited By ~ 2

Author(s):

Deirdre M. McElroy ◽

Luke M. Geever ◽

Clement L. Higginbotham ◽

Sinead M. Devery

Keyword(s):

Drug Delivery ◽

Physicochemical Properties ◽

Contact Lens ◽

Contact Lenses ◽

Delivery Systems ◽

Eye Drops ◽

Soft Contact ◽

Soft Contact Lenses ◽

Ophthalmic Drug Delivery ◽

Ophthalmic Drug

Hydrogel soft contact lenses have been investigated as delivery systems for ophthalmic drug products in response to the need for more efficient ophthalmic drug delivery systems. Ocular drugs delivered via eye drops have a low residence time in the eye resulting in as low as 5% bioavailability of the therapeutic agent. This study investigates the effect of varying concentrations of the photoinitiator diphenyl (2,4,6-trimethylbenzoyl)-phosphine oxide (TPO) on the physicochemical properties of hydrogel soft contact lenses for ophthalmic drug delivery purposes. Contact lens samples were synthesised via photopolymerisation with a range of initiator concentration. Gel fraction and swelling results indicated that increasing the photoinitiator concentration increased the efficiency of the gel network and reduced the water content of contact lens samples. Fourier transform infra-red spectroscopy (FTIR) analysis was employed to confirm polymerisation of the lenses and also indicated the presence of residual photoinitiator in lenses with higher TPO concentrations.

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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

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2019.118734 ◽

2020 ◽

Vol 574 ◽

pp. 118734 ◽

Cited By ~ 2

Author(s):

Pierre-Louis Destruel ◽

Ni Zeng ◽

Johanne Seguin ◽

Sophie Douat ◽

Frédéric Rosa ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Retention Time ◽

Rheological Characterization ◽

Ophthalmic Drug Delivery ◽

Ophthalmic Drug ◽

In Situ Gelling

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FORMULATION, OPTIMIZATION, AND EVALUATION OF IN-SITU GEL OF MOXIFLOXACIN HYDROCHLORIDE FOR OPHTHALMIC DRUG DELIVERY

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i4.30388 ◽

2019 ◽

pp. 147-158

Author(s):

Chitra Gupta ◽

VIJAY JUYAL ◽

Upendra Nagaich

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Influential Factors ◽

Drug Formulation ◽

In Situ Gel ◽

Formulation Optimization ◽

Ophthalmic Drug Delivery ◽

Ophthalmic Drug

Objective: The present study emphasizes the synthesis, optimization, and evaluation of ocular in-situ gel for ophthalmic drug delivery against conjunctivitis. Methods: Pre-formulation studies on the drug and polymers were carried out, which included the study of various physicochemical properties of the drug and drug-polymer compatibility studies. The 12 different formulations were further pre-optimised by Taguchi method for determining the number of influential factors. Furthermore, the formulation optimization was done by using ‘Box–Behnken’ design (BBD) (Design expert 10 software) for assessing the effect of formulation variables on product characteristics viz. viscosity, gelation temperature (GT), and mean release time (MRT). About 13 suggested runs of the experiment were carried out and formulations were optimised. Finally, three batches of the optimised formulation were prepared and evaluated for in vitro drug release, isotonicity of formulation, anti-microbial potential, ocular irritancy, and accelerated stability testing. Results: Pre-formulation study confirmed the purity, solubility, and compatibility of drug measured by λmax, partition coefficient, stability study, and Fourier-transform infrared spectroscopy (FTIR) analysis. Taguchi screening method suggested about 12 different formulations and 3 most prominent influential factors including viscosity, GT, and drug release. 13 different formulations designed based on ‘BBD’ method were further optimised by considering the most influential factors suggested by Taguchi screening. The in vitro evaluation of the optimised formulation gave satisfactory results in terms of drug release, and anti-microbial activity. It was found to be isotonic with no ocular irritancy. Further, the preparation immediately transformed from sol to gel upon administration into cul-de-sac region of the eye due to multi-dimensional approaches utilised for in-situ gel formation namely temperature change Pluronic, ion sensitivity due to Gellan-gum, pH sensitivity because of Carbopol. Conclusion: The optimised in-situ gelling ocular drug formulation showed promising potency for ophthalmic drug delivery with no irritancy due to the multifactorial mechanism.

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