Development and evaluation of a pH triggered in situ ocular gel of brimonidine tartrate

Bharath, S.; Karuppaiah, Arjunan; Karthik, S.; Hariharan, Sivaram; Santhanam, Ramasamy

doi:10.35333/jrp.2020.164

Cited by 5 publications

(5 citation statements)

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“…The sterility test was conducted on the mixture, and it successfully passed the test, indicating the absence of any microorganisms. Furthermore, the mixture was found to exhibit stability when stored at room temperature for a period of 60 days [ 26 ].…”

Section: Discussionmentioning

confidence: 99%

Comparative Study of In Situ Gel Formulation Based on the Physico-Chemical Aspect: Systematic Review

Kurniawansyah,

Rusdiana,

Sopyan

et al. 2023

Gels

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In recent years, in situ gel delivery systems have received a great deal of attention among pharmacists. The in situ gelation mechanism has several advantages over ointments, the most notable being the ability to provide regular and continuous drug delivery with no impact on visual clarity. Bioavailability, penetration, duration, and maximum medication efficacy are all improved by this mechanism. Our review systematically synthesizes and discusses comparisons between three types of in situ gelling system according to their phase change performance based on the physicochemical aspect from publications indexed in the Pubmed, ResearchGate, Scopus, Elsevier, and Google Scholar databases. An optimal temperature-sensitive in situ gelling solution must have a phase change temperature greater than ambient temperature (25 °C) to be able to be readily delivered to the eye; hence, it was fabricated at 35 °C, which is the precorneal temperature. In a pH-sensitive gelling system, a gel develops immediately when the bio-stimuli come into contact with it. An in situ gelling system with ionic strength-triggered medication can also perhaps be used in optical drug-delivery mechanisms. In studies about the release behavior of drugs from in situ gels, different models have been used such as zero-order kinetics, first-order kinetics, the Higuchi model, and the Korsmeyer-Peppas, Peppas-Sahlin and Weibull models. In conclusion, the optimum triggering approach for forming gels in situ is determined by a certain therapeutic delivery application combined with the physico-chemical qualities sought.

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Section: Discussionmentioning

confidence: 99%

Comparative Study of In Situ Gel Formulation Based on the Physico-Chemical Aspect: Systematic Review

Kurniawansyah,

Rusdiana,

Sopyan

et al. 2023

Gels

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“…The formulations were exposed to determine the kinetics of drug release. The in vitro drug release data were analyzed by fitting them into different kinetic models, namely zero-order, first-order, Higuchi, and Korsmeyer-Peppas, to investigate the release mechanism of natamycin from the formulation [23,24].…”

Section: (F) Kinetic Modelingmentioning

confidence: 99%

“…The stability studies of in situ gel of Natamycin was stored at 25°C ± 2°C / 60% RH ± 5% and 40°C ± 2°C / 75% RH ± 5 % for 3 months. The gel was analysed for physiochemical parameters like color change, clarity, visual appearance, gelling capacity, drug content, and pH for three months [24,27].…”

Section: (H) Stability Study Of Prepared Ocular Gelmentioning

confidence: 99%

Preparation and Characterization of Natamycin Loaded Bioadhesive inSituOphthalmic Gel for Enhanced Bioavailability

Verma

Gupta

Manigauha

2022

JSMPM

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Natamycin, an antifungal agent that has been approved in the management of exteriorfungal infectionsof the oculus such asfungal keratitis,blepharitis, and conjunctivitis. The ophthalmic preparation needs frequent installation into the eye due to the quickprecorneldrugloss which may lead to poor bioavailability. The present investigation aimed at formulation development and characterization of in situophthalmic gel of natamycin by using a blend polymer of sodium alginate, ethylcellulose, and Xanthan gum for better residence time to improvethe bioavailability of the drug. The six different formulations (F1 to F6) of natamycin in situgel were prepared. All the formulations were evaluated for clarity, visual appearance, pH, gelling capacity, drug content, drug release, release kinetic, ocular irritancy, and in vitro stability. The results were found to have complied with the pharmacopoeial specification. The in vitrodrug releases of F3 formulation established maximum drug release for 8 h as compared to other formulations in sustained manner.Further, the F3 formulation was found to be stable, safe and innocuous. The studies suggested that prepared in situophthalmic gel of natamycin will be a valuable alternative to conventional eye drops to counter the precorneal loss.

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“…As explained, the carbomer is able to gel and interacts with the mucin layer of the corneal via hydrogen interaction, resulting in a thin film that is able to resist the blinking forces and the tears washout of the eyes [ 79 ]. Likewise, Karuppaiah et al also developed brimonidine in situ gel with Carbopol 940 that could release brimonidine 3 h longer than the marketed ophthalmic eye drops [ 60 ]. Burst released from the formulation was hardly observed throughout the study, while that being said, it usually happened when the drug was not fully entrapped in the gel matrix.…”

Section: Smart Ocular Delivery Using Stimuli-responsive In Situ Gel Platformmentioning

confidence: 99%

Potential of Stimuli-Responsive In Situ Gel System for Sustained Ocular Drug Delivery: Recent Progress and Contemporary Research

et al. 2021

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Eyesight is one of the most well-deserved blessings, amid all the five senses in the human body. It captures the raw signals from the outside world to create detailed visual images, granting the ability to witness and gain knowledge about the world. Eyes are exposed directly to the external environment; they are susceptible to the vicissitudes of diseases. The World Health Organization has predicted that the number of individuals affected by eye diseases will rise enormously in the next decades. However, the physical barriers of the eyes and the problems associated with conventional ocular formulations are significant challenges in ophthalmic drug development. This has generated the demand for a sustained ocular drug delivery system, which serves to deliver effective drug concentration at a reduced frequency for consistent therapeutic effect and better patient treatment adherence. Recent advancement in pharmaceutical dosage design has demonstrated that a stimuli-responsive in situ gel system exhibits the favorable characteristics for providing sustained ocular drug delivery and enhanced ocular bioavailability. Stimuli-responsive in situ gels undergo a phase transition (solution–gelation) in response to the ocular environmental temperature, pH, and ions. These stimuli transform the formulation into a gel at the cul de sac to overcome the shortcomings of conventional eye drops, such as rapid nasolacrimal drainage and short contact time with the ocular surface This review highlights the recent successful research outcomes of stimuli-responsive in situ gelling systems in treating in vivo models with glaucoma and various ocular infections. Additionally, it also presents the mechanism, recent development, and safety considerations of stimuli-sensitive in situ gel as the potential sustained ocular delivery system for treating common eye disorders.

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Development and evaluation of a pH triggered in situ ocular gel of brimonidine tartrate

Cited by 5 publications

References 0 publications

Comparative Study of In Situ Gel Formulation Based on the Physico-Chemical Aspect: Systematic Review

Comparative Study of In Situ Gel Formulation Based on the Physico-Chemical Aspect: Systematic Review

Preparation and Characterization of Natamycin Loaded Bioadhesive inSituOphthalmic Gel for Enhanced Bioavailability

Potential of Stimuli-Responsive In Situ Gel System for Sustained Ocular Drug Delivery: Recent Progress and Contemporary Research

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