Controlled Ocular Delivery of Acyclovir through Rate Controlling Ocular Insert of Eudragit: A Technical Note

Khan, Shagufta; Ali, Asgar; Singhavi, Dilesh J.; Yeole, Pramod

doi:10.1208/s12249-008-9032-1

Cited by 17 publications

(15 citation statements)

References 11 publications

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“…One milliliter of the filtrate was diluted up to ten milliliters; the drug content was measured by analyzing the diluted solution with UV-visible spectrophotometer. (24,25) The mean and standard deviation were calculated. The dosage uniformity meets the requirements stated in the USP when the first ten units have an acceptance value less than or equal to 15% (26) .…”

Section: Content Uniformitymentioning

confidence: 99%

Preparation and Evaluation of Rebamipide Film using Casting Technique for Local Action

Radhi

Ghareeb

2019

IJPS

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The aim of this study is to prepare and evaluate an extended release rebamipide ocular insert using hydroxypropyl methylcellulose as the main components of this drug delivery system for dry eye syndrome management, to have the advantage of both rebamipide inducing mucin secretion and hydroxypropyl methylcellulose lubricating properties. Solvent casting technique was used to prepare the inserts; the amino acid L-arginine was used to solubilize the drug, hydroxypropyl methylcellulose grades (HPMC E5 and K15M) and poly ethylene glycol 200 were used as excipients. The inserts were evaluated for their physical and mechanical properties, moisture loss% and absorption %, surface pH, and in-vitro drug release. The use of L-arginine exhibited an enhancement of rebamipide solubility in both deionized water and phosphate buffer (pH 7.4) by approximately 274 and 2.8 folds, respectively. The formulae showed uniform weight, thickness and drug content except for formula (F1) that composed mostly of HPMC E5: HPMC K15M at ratio of 1: 0.17 and had no plasticizer (poly ethylene glycol 200) in its composition; it showed haziness in its appearance and brittleness of the insert. While formula (F3) which contained mainly HPMC E5: HPMC K15M at ratio of 1: 0.4 with poly ethylene glycol 200 showed good physical and mechanical properties thus was selected for in vitro release and was compared to the marketed brand Mucosta ® ophthalmic suspension unit dose 2%w/v; F3 showed significant larger T50% and T80% (p-values 0.034 and 0.015) compared to those of the reference marketed brand and similarity factor value was (f2 = 37.27). The results of this study showed that rebamipide ocular inserts have good potential for futuristic rebamipide extended release ocular delivery system.

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Section: Content Uniformitymentioning

confidence: 99%

Preparation and Evaluation of Rebamipide Film using Casting Technique for Local Action

Radhi

Ghareeb

2019

IJPS

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“…[26] An implant containing 2.5% sodium alginate with 3.5:1.5 ratio of Eudragit RL 100 and RS 100 in vivo showed the presence of 1.7 µg/ml of ACV in the aqueous humor after 8 h, which remained up to 5 days and also supported with high IVIVC. [27] ACV incorporated as a binary system with β-cyclodextrin and dispersed into HPMC, was made as the reservoir for the implant, and the release was controlled up to 20 h with non-Fickian diffusion behavior and high IVIVC in release rate studies. [28] Controlled drug release was achieved by soluble ocular insert containing the combination of natural hydrophilic and hydrophobic polymers.…”

Section: Modified Release Tabletsmentioning

confidence: 99%

Drug delivery approaches of an antiviral drug: A comprehensive review

Durai¹

2015

Asian J Pharm

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T he guanine derivative antiviral drug acyclovir (ACV) is one of the oldest molecules laying successful market until date, being commercially available in various dosage forms for oral, topical and parenteral administrations. Clinical application of this drug is superior to new antiviral agents due to its potential values such as suppression of recurrence, safety profile, minimal drug interactions, and being inexpensive. ACV is slightly water-soluble, less permeable and poorly bioavailable, yet more potential antiviral molecule, the physicochemical modifications and novel dosage form approaches resulted with more than 100 research works within a decade. The survey of literature showed enormous reports on ACV formulation development, which includes modified tablets, particulate drug delivery, vesicular drug delivery, polymeric nanoparticles, bioadhesive systems, floating dosage forms, in situ gelling systems, transdermal delivery, implantable systems, emulsified dosage forms, polymeric films/patches, etc. As the drug could be administered via multiple routes for effective site targeted action at various doses, and attracted the attention of many researches, the review of the current approaches for the delivery of ACV could be more beneficial for the new scientists. This paper is a review of recent researches highlighting the development of newer techniques and novel dosage forms of ACV for better therapeutic efficacy, which were aimed at enhancing its solubility, permeability and bioavailability.Durai: Recent formulation designs of acyclovir How to cite this article: Durai RD. Drug delivery approaches of an antiviral drug: A comprehensive review. Asian J Pharm 2015;9:1-12.

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“…A basic concept in ophthalmic research and development is that the therapeutic efficiency of an ophthalmic drug can be greatly improved by prolonging its contact with the corneal surface ophthalmic inserts offer many advantages over conventional dosages forms, like increased ocular residence, possibility of releasing drug at a slow and constant rate, accurate dosing, exclusion of preservatives and increased shelf life 4 .…”

Section: Issn: 0975-8232mentioning

confidence: 99%

Untitled

2012

IJPSR

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Goal of the present investigation was to formulate ocular inserts of dorzolamide hydrochloride and timolol maleate for the treatment of glaucoma. Ocular inserts of dorzolamide hydrochloride and timolol maleate were prepared using different polymers ethylcellulose, Eudragit RL 100, and Eudragit RS100 by solvent casting method with an objective to increasing the contact time, achieving controlled release, reducing in frequency of administration, and improving therapeutic efficacy. The drug-excipients interaction was studied by Fourier transform infrared spectroscopy (FTIR) studies. Prepared ocular inserts were evaluated for their physicochemical properties such as uniformity of thickness, weight uniformity, tensile strength, percentage elongation, drug content, moisture loss, moisture absorption. The in vitro diffusion of drug from the inserts was studied using the classical biochemical donor -receptor compartment model fabricated in the laboratory and the formulation that showed better release profile was subjected to in vivo studies on albino-rabbits. Ocular irritation study was performed using healthy albino rabbits and confirmed that there was no irritation in the rabbit eyes. All the inserts were found to be uniform thickness and uniform weight. The inserts possessed good tensile strength and percentage elongation. All the formulations followed a first order release pattern. Optimized formulation RSRL3 showed high correlation coefficient (R = 0.996 & 0.995 respectively for dorzolamide HCl & timolol maleate) between in vitro and in vivo release. Stability study was carried out on RSRL3 formulation and showed no significant changes in the drug content as well as physical characteristics of the film.

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Controlled Ocular Delivery of Acyclovir through Rate Controlling Ocular Insert of Eudragit: A Technical Note

Cited by 17 publications

References 11 publications

Preparation and Evaluation of Rebamipide Film using Casting Technique for Local Action

Preparation and Evaluation of Rebamipide Film using Casting Technique for Local Action

Drug delivery approaches of an antiviral drug: A comprehensive review

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