In situ ophthalmic gel of ciprofloxacin hydrochloride for once a day sustained delivery.
ABSTRACT This article focuses on preparation and evaluation of a once a day ophthalmic delivery system for ciprofloxacin hydrochloride based on the concept of pH-triggered in situ gelation. The in situ gelling system involves the use of polyacrylic acid (Carbopol 980NF) as a phase transition polymer, hydroxypropyl methylcellulose (Methocel K100LV) as a release retardant, and ion exchange resin as a complexing agent. Ciprofloxacin hydrochloride was complexed with ion exchange resin to avoid incompatibility between drug and polyacrylic acid. The developed formulation was stable, and nonirritant to rabbit eyes and in vitro drug release was found to be around 98% over a period of 24 hours.
- SourceAvailable from: Manas Bhowmik[Show abstract] [Hide abstract]
ABSTRACT: The aim of this investigation was to develop a novel in-situ gelling formulation based on poloxamer-407 (PM) for the sustained release of an ophthalmic drug. In an attempt to reduce the concentration of PM without compromising the in-situ gelling capability and also to increase the drug release time, xanthan gum (XG) and guar gum (GG) were added into PM to develop different formulations. At concentrations of 18% and above, the PM was able to undergo sol-gel transition below body temperature. It was found that XG and GG at a weight ratio of 3:7 were able to convert PM solution into gel below body temperature at PM concentrations below 18%. Both the in-vitro and in-vivo studies indicated that the PM with an XG-GG combination had a better ability to retain the drug than PM itself. The results indicated that the developed in-situ gelling formulations containing PM with XG-GG may be a better alternative than a conventional eye drop.International journal of biological macromolecules 08/2013; · 2.37 Impact Factor
- [Show abstract] [Hide abstract]
ABSTRACT: Introduction: Topical fluoroquinolones are used in ophthalmology to treat ocular infections. They are bactericidal and inhibit bacterial DNA replication by inhibiting DNA gyrase and topoisomerase. Fluoroquinolones possess two ionizable groups: a carboxylic group (pKa(1) = 5.5 - 6.34) and a heterocyclic group (pKa(2) = 7.6 - 9.3), in the nucleus, which acquire charge at pH above and below the isoelectric point (pI = 6.75 - 7.78). At isoelectric point, fluoroquinolones remain unionized and show enhanced corneal penetration but exhibit reduced aqueous solubility and the drug may precipitate from aqueous solution. Aqueous ophthalmic solutions of fluoroquinolones are obtained by using hydrochloride or mesylate salt which is acidic and irritating to the eyes. Hence, pH of the solution is kept between 5 and 7 to ensure aqueous solubility and minimum ocular irritation. Areas covered: This review gives an overview of various physicochemical and formulation factors affecting the ocular delivery of fluoroquinolones and strategies for getting higher ocular bioavailability for ocular delivery of fluoroquinolones. These strategies could be employed to improve efficacy of fluoroquinolones in eye preparation. Expert opinion: Broad-spectrum antibacterials, such as the ophthalmic fluoroquinolones, are powerful weapons for treating and preventing potentially sight-threatening infections. The fourth-generation fluoroquinolones have quickly assumed an outstanding place in the ophthalmic applications. Especially valuable for their broad-spectrum coverage against Gram-positive and Gram-negative organisms, these agents have become the anti-infective of preference for many ophthalmologists. Moxifloxacin seems to be a promising powerful molecule among all fluoroquinolones for treatment of bacterial infections.Expert Opinion on Drug Delivery 02/2013; · 4.87 Impact Factor
- [Show abstract] [Hide abstract]
ABSTRACT: PURPOSE: The aim of the present study was to develop and optimize sinomenine hydrochloride (SIN) in situ gel for uveitis treatment. METHODS: Carbopol 940 was used as the gelling agent in combination with hydroxypropyl methylcellulose (HPMC), which acts as a viscosity enhancer. The formulations were prepared using various concentrations of Carbopol 940 and HPMC. The prepared in situ gels were evaluated for gellation, drug release, ocular irritation, elimination time and pharmacokinetic studies. Furthermore, the effect of SIN on the development of experimental autoimmune anterior uveitis (EAAU) was assessed. RESULTS: The optimum concentration of Carbopol was 0.1% (w/v), and that for HPMC was 0.4% (w/v). Which showed a significant enhancement in gel strength in the physiological condition while free flowing at non-physiological condition. Optimum formula F2-3 consisting of 0.5% SIN was prepared and kept as gel group, and 0.5% SIN solution was prepared and kept as control group. Gel group provided sustained release of the drug over a period of 480min. No evidence of overt toxicity and irritation was observed in any study. The elimination time of control group and gel group was completed within 10min and 25min, respectively. The area under the aqueous humor concentration vs. time curve (AUC0-t) and maximum concentration (Cmax) values of gel group was 2.70-fold and 1.79-fold higher than that of control group. Additionally, clinical examination showed that SIN suppressed inflammation in EAAU. CONCLUSIONS: These results support the potential applications of SIN in situ gel for uveitis treatment.International immunopharmacology 06/2013; · 2.21 Impact Factor