Formulation and ex vivo–in vivo evaluation of pH-triggered brimonidine tartrate in situ gel for the glaucoma treatment using application of 32 factorial design

Barse, Rohan; Tagalpallewar, Amol; Kokare, Chandrakant; Sharma, Jyoti; Sharma, Pankaj Kumar

doi:10.1080/03639045.2017.1414229

Cited by 29 publications

(27 citation statements)

References 32 publications

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“…Brimonidine tartrate (BRT) is a hydrophilic drug used for treatment of glaucoma, its pharmacological classification is α 2 adrenergic agonist acts by dual mechanisms, decreasing aqueous humor production and increasing the uveoscleral outflow as it promotes prostaglandins synthesis, it has a neuroprotective action and decrease the ischemia-induced optic nerve damage (Saylor et al., 2009; Barse et al., 2018). Moreover, it has the advantage of being effective in normal tension glaucoma (Gandolfi et al., 2003), where IOP measurements are below 21 mm Hg but characteristic glaucomatous structural and functional optic nerve defects are present (Razeghinejad & Lee, 2019).…”

Section: Introductionmentioning

confidence: 99%

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

2019

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Brimonidine tartrate (BRT) is a hydrophilic a 2 adrenergic agonist used for the treatment of glaucoma. Glaucoma is an ocular disease affecting the anterior segment of the eye requiring lifetime treatment. Owing to the obstacles facing ocular delivery systems and hydrophilicity of BRT, frequent administration of the eye drops is required. Niosomes have been widely used to improve the ocular bioavailability of the topically applied drugs and to enhance the ocular residence time. However, they have drawbacks as physical instability, aggregation, and loss of the entrapped drug. For this reason, BRT proniosomes were prepared to overcome niosomal instability issues. A D-optimal design was utilized to determine the optimum conditions for preparation of the proniosomal gels. Independent variables were amount of surfactant, surfactant:cholesterol ratio, and type of surfactant used. The dependent variables were entrapment efficiency (EE%), particle size, percentage of drug released after 2 h (Q 2h), and percentage of drug released after 24 h (Q 24h). The optimum formula was suggested with desirability 0.732 and the composition of 540 mg Span 60 and 10:1 surfactant:cholesterol ratio. The results obtained after reconstitution were; EE% of 79.23 ± 1.12% particle size of 810.95 ± 16.758 nm, polydispersity index (PDI) 0.6785 ± 0.213, zeta potential 59.1 ± 0.99 mV, Q 2h 40.98 ± 1.29%, Q 8h 63.35 ± 6.07%, and Q 24h ¼ 91.11 ± 1.76%. Transmission electron microscope imaging of the formula showed the typical spherical shape of niosomes. In-vivo pharmacodynamic study assured the improved ocular bioavailability of BRT selected formula when compared with Alphagan V R P with relative AUC 0-24 of 5.024 and 7.90 folds increase in the mean residence time (MRT). Lack of ocular irritation of the formula was assured by Draize test.

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Section: Introductionmentioning

confidence: 99%

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

2019

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“…Both in vitro and in vivo tests indicated that the hybrid hydrogel displayed the superior precorneal retention of drugs over the Carbopol or Pluronic aqueous solution alone. A similar ophthalmic drug delivery system was also reported by Barse and coworkers, who used Carbopol in combination with hydroxypropyl methylcellulose (HPMC) for topical glaucoma treatment . Experimental results demonstrated that the optimized hybrid hydrogel could provide a relatively long‐term duration of drug action and improve IOP reduction activity compared to marketed eye drops in the in vivo study.…”

Section: Ophthalmic Hydrogel Systemmentioning

confidence: 60%

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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“…It was observed after administration of marketed eye drop formulation, the rapid reduction in intraocular pressure upto 3 h, but due to liquid nature of formulation it had no ability to retain in cul de sac region. The results showed that after 3 h % decrease in IOP again decrease in case of marketed formulation due to its liquid nature [47,[48][49][50].…”

Section: G In Vivo Studiesmentioning

confidence: 99%

A Review on Poloxamer and Hydroxy Propyl Methyl Cellulose Combination as Thermoresponsive Polymers in Novel Ophthalmic in Situ Gel Formulation and Their Characterization

et al. 2021

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Poor bioavailability is one of the most significant problems in the delivery of the ocular drug system. Ophthalmic ointments, solutions and suspensions are the most frequently used dosage forms to treat ocular disease, and their effectiveness as a drug are compromised by several limitations that lead to poor ocular bioavailability. In situ gel is one of the most promising strategy and solutions to improve the ocular bioavailability of drugs. The purpose of this review is to discuss the formulation and characterization of in situ gel. This review is written based on the data or information obtained by using several search engines and several scientific journals, focused on Poloxamer 407 and Hydroxy Propyl Methyl Cellulose (HPMC) bases combination. Active ingredients to treat ocular disease such as Ciprofloxacin, Fluconazole and Ofloxacin can be formulated with the combination of Poloxamer 407 as polymer gelling agent and HPMC as viscosity enhancer to produce good quality in situ gel dosage forms. The in situ gel dosage forms can be a promising alternate solution for the ophthalmic delivery system.

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Formulation and ex vivo–in vivo evaluation of pH-triggered brimonidine tartrate in situ gel for the glaucoma treatment using application of 3² factorial design

Abstract: The developed in situ gelling system as a promising ophthalmic formulation to prolong the drug lowering effect on the intraocular pressure.

Cited by 29 publications

References 32 publications

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

Stimulus‐Responsive Hydrogel for Ophthalmic Drug Delivery

A Review on Poloxamer and Hydroxy Propyl Methyl Cellulose Combination as Thermoresponsive Polymers in Novel Ophthalmic in Situ Gel Formulation and Their Characterization

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