Abstract
<p class="Default"><strong>Objective: </strong>To study the <em>in vivo</em> 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.</p><p class="Default"><strong>Methods: </strong>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 <em>in vivo</em> 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 After placing the insert in the eye 100 µl of the aqueous humor was withdrawn at different time intervals in order to measure the concentration profile of CFX-HCl.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.</p><p class="Default"><strong>Results: </strong>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.</p><strong>Conclusion: </strong>The analysis method was found sensitive, accurate and precise and could be used to assess the <em>in vivo</em>behaviour of CFX-HCl. The ratio of the free drug to the matrix system controlled the rate of drug release.<p class="Default"> </p><p> </p>
Highlights
Ciprofloxacin hydrochloride is 1-cyclopropyl-6-fluoro-4-oxo-7-(piperazin1-yl)-quinoline-3-carboxylic acid, monohydrochloride, monohydrate with the chemical structure shown in, it is a commercially available antibiotic used to treat bacterial infections in different parts of the body [1]
Ciprofloxacin hydrochloride CFX-HCl has short elimination half-life, if it is used for treating eye illnesses, it must be given as 34 drops at least three times a day in order to maintain a continuous sustained level of medication, which gives the eye a massive and unpredictable dose, and as the drug concentration of the eye drop solution increases more amount of it will be lost through lacrimal-nasal drainage system, and subsequent absorption of this drained drug may result in having undesirable systemic side effects [5]
The controlled drug delivery system has an upper edge over eye drops and ointments, because the drug is delivered at the site of action, less amount of the drug is required, constant drug supply is maintained over a predetermined time, so patient compliance and efficacy of ciprofloxacin hydrochloride could be improved by the use of a drug delivery system promoting prolonged release of drug and increasing its application intervals [2, 3]
Summary
Ciprofloxacin hydrochloride is 1-cyclopropyl-6-fluoro-4-oxo-7-(piperazin1-yl)-quinoline-3-carboxylic acid, monohydrochloride, monohydrate with the chemical structure shown in (fig. 1), it is a commercially available antibiotic used to treat bacterial infections in different parts of the body [1]. 1), it is a commercially available antibiotic used to treat bacterial infections in different parts of the body [1] It is used for the treatment of infectious types of keratitis and conjunctivitis caused by gram-negative bacteria. A basic concept shared by most scientists in ophthalmic research and development is that the therapeutic efficacy of an ophthalmic drug can be greatly improved by prolonging its contact with the corneal tissue and/or conjunctiva epithelium [6] For achieving this purpose, viscosity-enhancing agents, such as methyl cellulose, were added to eye drop preparations, they did not yield a constant drug bioavailability as originally hoped repeated medications were still required throughout the day [6]. The controlled drug delivery system has an upper edge over eye drops and ointments, because the drug is delivered at the site of action, less amount of the drug is required, constant drug supply is maintained over a predetermined time, so patient compliance and efficacy of ciprofloxacin hydrochloride could be improved by the use of a drug delivery system promoting prolonged release of drug and increasing its application intervals [2, 3]
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