Updates on drug bioavailability and delivery to posterior segment of eye

Gupta, Himanshu

doi:10.4103/0975-7406.116792

Cited by 9 publications

(4 citation statements)

References 32 publications

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“…The conventional ocular delivery systems like solutions, suspensions and ointments show drawbacks such as increased precorneal elimination, high variability in efficiency and blurred vision, respectively. [ 3 4 ] The major problem encountered with solution is the rapid and extensive elimination of drugs from the precorneal lachrymal fluid by solution drainage, lachrymation, and nonproductive absorption by the conjunctiva, which may lead to undesirable side-effects. It must be noted that this high drainage rate is due to the tendency of the eye to maintain its residence volume at 7-10 μl permanently, whereas volumes topically instilled range from 20 to 50 μl.…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of stimuli-sensitive hydrogels of timolol maleate and brimonidine tartrate for the treatment of glaucoma

Dubey

Prabhu²

2014

Int J Pharma Investig

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Background:Stimuli-sensitive hydrogels are hydrophilic, three-dimensional, polymeric network structure capable of imbibing large amounts of water or biological fluids on stimulation, such as pH, temperature, and ionic change. Owing to the drawback of conventional therapy for ocular delivery, and to provide additive effect on intraocular pressure (IOP) reduction, stimuli sensitive hydrogel membranes containing a combination of timolol maleate and brimonidine tartrate were formulated for the treatment of glaucoma.Materials and Methods:Stimuli-sensitive hydrogel were formulated by timolol maleate and brimonidine tartrate. Poly acrylic acid (carbopol C 934p) is used as a gelling agent, hydroxylpropyl methylcellulose as viscolizer, sodium chloride as tonicity agent. Bezalkonium chloride as preservative. White rabbits of both sexes, weighing between 2 and 3 kg were used for the study. Stirring of ingredients in pH 4 phosphate buffers at high speed was carried out.Result:Viscosity of the prepared hydrogels lies in the optimum range that is, 25-55 cps. Infrared spectroscopy studies show that there is no interaction between the drug and polymer. Drug released up to 90% at the end of 8 h. The hydrogel membranes were found to be sterile, nonirritant to the eye. Marketed formulation showed a decrease in IOP up to 14 mmHg at the end of 5 h and then elimination of drug, F2 and F6 maintain the sustained effect up to 12 h.Conclusion:Stimuli-sensitive hydrogels was successfully formulated and evaluated for rheological studies, drug release studies, drug interaction studies, sterility studies, ocular irritation studies, and in vivo studies. IOP lowering activity of the combination of timolol maleate and brimonidine tartrate in stimuli-sensitive hydrogel was better when compared with alone medication, which shows the additive effect of combination medication.

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Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of stimuli-sensitive hydrogels of timolol maleate and brimonidine tartrate for the treatment of glaucoma

Dubey

Prabhu²

2014

Int J Pharma Investig

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“…Only 2.3% of injuries require hospitalization but noteworthy is that over 10% of them lose useful vision [3]. Despite anatomical and physiological protection, injuries to the eyes are common with poor prognosis due to vulnerable tissues, infection and meager amount of drug reaching ocular tissues [4].…”

Section: Introductionmentioning

confidence: 99%

A Clinical Study of Ocular Trauma: Etiology, Pattern, Management and Visual Outcome

Bhim¹,

Sahai²,

Gangwal³

et al. 2022

Act Sci Oph

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“…Angiotensin converting enzyme (ACE) inhibitors and angiotensin II receptor blocker‐class drugs, such as candesartan and irbesartan, have been shown to be effective in preventing the damage caused by diabetic retinopathy (Moss et al, ; Sjølie, Dodson, & Hobbs, ; Virk, Donaghue, Wong, & Craig, ; Wang et al, ). However, it is difficult to reach a therapeutically relevant concentration of these therapeutics in the posterior segment of the eye, where the retina is located (Gupta, ). To achieve that, high concentrations of the therapeutics would be required in the systemic circulation.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous quantification of candesartan and irbesartan in rabbit eye tissues by liquid chromatography–tandem mass spectrometry

Tan

Gui

Wong

et al. 2020

Biomedical Chromatography

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Diabetic retinopathy is a major cause of vision loss in adults. Novel eye-drop formulations of candesartan and irbesartan are being developed for its cure or treatment. To support a preclinical trial in rabbits, it was critical to develop and validate a new LC-MS/MS method for simultaneous quantification of candesartan and irbesartan in rabbit eye tissues (cornea, aqueous humor, vitreous body and retina/choroid). Eye tissue samples were first homogenized in H 2 O-diluted rabbit plasma. The candesartan and irbesartan in the supernatants together with their respective internal standards (candesartan-d 4 and irbesartan-d 4 ) were extracted by solid-phase extraction. The extracted samples were injected onto a C 18 column for gradient separation. The MS detection was in the positive electrospray ionization mode using the multiple reaction monitoring transitions of m/z 441 ! 263, 445 ! 267, 429 ! 207, and 433 ! 211 for candesartan, candesartan-d 4 , irbesartan and irbesartan-d 4 , respectively. For the validated concentration ranges (2-2000 and 5-5000 ng/g for candesartan and irbesartan, respectively), the within-run and between-run accuracies (% bias) were within the range of −8.0-10.0. The percentage CV ranged from 0.6 to 7.3. There was no significant matrix interference nor matrix effect from different eye tissues and different rabbits. The validated method was successfully used in the Good Laboratory Practice (GLP) study of rabbits. K E Y W O R D S candesartan, eye tissue, irbesartan, LC-MS, rabbit

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Updates on drug bioavailability and delivery to posterior segment of eye

Cited by 9 publications

References 32 publications

Formulation and evaluation of stimuli-sensitive hydrogels of timolol maleate and brimonidine tartrate for the treatment of glaucoma

Formulation and evaluation of stimuli-sensitive hydrogels of timolol maleate and brimonidine tartrate for the treatment of glaucoma

A Clinical Study of Ocular Trauma: Etiology, Pattern, Management and Visual Outcome

Simultaneous quantification of candesartan and irbesartan in rabbit eye tissues by liquid chromatography–tandem mass spectrometry

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