Characterization and in vivo evaluation of ocular minitablets prepared with different bioadhesive Carbopol–starch components

Weyenberg, Wim; Bozdağ, Sibel; Foreman, P; Remon, Jean Paul; Ludwig, Annick

doi:10.1016/j.ejpb.2005.08.003

Cited by 21 publications

(13 citation statements)

References 14 publications

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“…However, despite the positive findings, some limitations are present. For instance, it was reported that in some cases the mini‐tablets displayed a tendency to move around in or fall out of the eye . This could hinder the drug release process and cause discomfort for the subject.…”

Section: Developments and Future Outlookmentioning

confidence: 99%

A review of topically administered mini-tablets for drug delivery to the anterior segment of the eye

Moosa

Choonara

Toit

et al. 2014

Journal of Pharmacy and Pharmacology

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Objectives The human eye is a unique and intricate structure which has made drug delivery to the eye a formidable undertaking. Anterior-segment eye diseases are ubiquitous, especially among elderly patients, and conventional eye drops, although a first-choice dosage form, are not always an efficient treatment option. The development of novel drug delivery systems for improved treatment is therefore imperative. Key findings In an attempt to circumvent the obstacles presented by the structure of the eye, advanced systems such as ocular mini-tablets have been developed. In this review, a concerted effort has been made to provide a detailed overview of topically administered ocular mini-tablets and other solid devices for drug delivery to the anterior segment of the eye. These mini-tablets have been shown in vitro and in vivo to have significant advantages in comparison with liquid preparations. This is a step toward attaining better patient convenience and compliance, which are critical factors. Summary Solid ophthalmic dosage forms have several advantages that can contribute to assisting with patient compliance and, ultimately, effective disease treatment. In addition to the challenges associated with topical ocular drug delivery, the shortcomings of conventional eye drops, advantages of mini-tablets, and improvements to date to these systems are discussed. The requirement for further advancements in the ocular field is also emphasized.

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Section: Developments and Future Outlookmentioning

confidence: 99%

A review of topically administered mini-tablets for drug delivery to the anterior segment of the eye

Moosa

Choonara

Toit

et al. 2014

Journal of Pharmacy and Pharmacology

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“…These inserts could help to overcome the ocular drug delivery limitations and enhance the ocular bioavailability of drugs by improving the precorneal residence time of drugs and also decrease the non-productive drug loss-related systemic toxicities [8,9]. Dosing of drug using the ocular inserts is more accurate with a low risk of systemic adverse effects as the drug does not drain into the nasolacrimal passage.…”

Section: Introductionmentioning

confidence: 99%

Sustained release ocular inserts of brimonidine tartrate for better treatment in open-angle glaucoma

Bhagav

Trivedi

Shah

et al. 2011

Drug Deliv. and Transl. Res.

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Pathology of eye, especially in the case of glaucoma, requires optimal therapeutically effective concentration of the drug in the ocular tissues for prolonged period of time with decreased dosing frequency and improved patient compliance. In the present study, brimonidine tartrate (BRT) ocular inserts were designed based on hydrophilic and/or inert/zwitterionic polymer matrix to design mucoadhesive and extended release ocular inserts. Designed inserts were evaluated for their physicochemical properties such as crushing strength/hardness, friability, drug content and mucoadhesion, and erosion and in vitro drug release characteristics. The selected optimised formulations were compared with marketed preparation for in vivo ocular irritation in healthy rabbits and for in vivo pharmacodynamic efficacy on alpha-chymotrypsin-induced glaucomatous rabbits. The developed formulations showed good physicochemical properties and mucoadhesive strength, and a good correlation was seen between rate of erosion or swelling with drug release rate in case of formulations with higher proportion of polyethylene oxide (PEO). Modulation of drug release was achieved by incorporating Eudragit in PEO matrix. Addition of Eudragit resulted in shifting of drug release mechanism from erosion-controlled to diffusion-controlled mechanism. In vivo ocular irritation studies confirmed the absence of any irritation upon administration in rabbits. Intraocular pressure (IOP) measurement studies showed an improved IOP-lowering ability of ocular insert of BRT in comparison to eye drops.

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“…Spray-dried polymeric delivery systems also have been recommended as a possible way to enhance the low bioavailability displayed by standard ophthalmic vehicles [11,12]. A modifiedrelease ocular insert system of CFX-HCl was previously reported [13].…”

Section: Introductionmentioning

confidence: 99%

In Vivo Study of Promising Formulated Ocular Bio-Adhesive Inserts of Ciprofloxacin Hydrochloride Combination With Xanthan Gum and Carbopol

Alshawwa

Obaidat

Sallam³

et al. 2016

Int J Pharm Pharm Sci

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Objective: To study the in vivo behaviour and irritant properties of different ocular bio-adhesive inserts of ciprofloxacin hydrochloride (CFX-HCl) prepared using a spray dried (SD2) matrix system consisting of xanthan gum, carbopol, and propylene glycol.Methods: CFX-HCl in aqueous humor samples was analysed using HPLC method. Applying a mobile phase of 0.01M sodium acetate: methanol (70:30 v/v) with pH around 3.00, and using Purosphere star 100RP-18 column (125 mm × 4.6 mm × 5 µm). The in vivo behaviour and irritant properties of ocular inserts was studied on rabbits. Twelve rabbits were used for the study and were divided into four groups. After placing the insert in the eye 100 µl of the aqueous humor was withdrawn at different time intervals in order to measure the concentration profile of CFX-HCl. The tested formulae R, F1, F2, and F3 were all containing 6.25 mg of CFX-HCl. Results:The method was well validated according to linearity, recovery, and precision. Where the calibration curve was linear over a concentration range of (2.500-7.826) µg/ml, with an average recovery of 99.76%. The presence of the matrix system enhances the absorption of CFX-HCl and sustains its release up to four days leading to increasing its bioavailability. Also, the ocular inserts of F2 and F3 have better biocompatibility compared with R and F1. Conclusion:The analysis method was found sensitive, accurate and precise and could be used to assess the in vivo behaviour of CFX-HCl. The ratio of the free drug to the matrix system controlled the rate of drug release.

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Characterization and in vivo evaluation of ocular minitablets prepared with different bioadhesive Carbopol–starch components

Cited by 21 publications

References 14 publications

A review of topically administered mini-tablets for drug delivery to the anterior segment of the eye

A review of topically administered mini-tablets for drug delivery to the anterior segment of the eye

Sustained release ocular inserts of brimonidine tartrate for better treatment in open-angle glaucoma

In Vivo Study of Promising Formulated Ocular Bio-Adhesive Inserts of Ciprofloxacin Hydrochloride Combination With Xanthan Gum and Carbopol

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