Ophthalmic controlled release in situ gelling systems for ciprofloxacin based on polymeric carriers

Al‐Kassas, Raida; ELKHATIB, MONA M.

doi:10.1080/10717540802689008

Cited by 40 publications

(19 citation statements)

References 23 publications

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“…This consideration accounts for why HPMC solution was used as a vehicle. It acts as a viscosity enhancer and is expected to increase both the residence time of the S-nitrosothiols in the cul-de-sac and their bioavailability on the pre corneal tear film (36)(37)(38) . Moreover, the low amount of S-nitrosothiols decomposition in the HPMC matrix indicates that this vehicle is appropriate for ocular drug delivery.…”

Section: Discussionmentioning

confidence: 99%

Assessment of ocular surface toxicity after topical instillation of nitric oxide donors

Cariello¹,

Souza²,

Lowen³

et al. 2013

Arq. Bras. Oftalmol.

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Ethic committee from UNIFESP: number 1573/08. ABSTRACTPurpose: To evaluate the ocular surface toxicity of two nitric oxide donors in ex vivo and in vivo animal models: S-nitrosoglutathione (GSNO) and S-nitroso-Nace tylcysteine (SNAC) in a hydroxypropyl methylcellulose (HPMC) matrix at final concentrations 1.0 and 10.0 mM. Methods: Ex vivo GSNO and SNAC toxicities were clinically and histologically ana lyzed using freshly excised pig eyeballs. In vivo experiments were performed with 20 albino rabbits which were randomized into 4 groups (5 animals each): Groups 1 and 2 received instillations of 150 µL of aqueous HPMC solution containing GSNO 1.0 and 10.0 mM, respectively, in one of the eyes; Groups 3 and 4 received instillations of 150 µL of aqueous HPMC solution-containing SNAC 1.0 and 10.0 mM, respectively, in one of the eyes. The contralateral eyes in each group received aqueous HPMC as a control. All animals underwent clinical evaluation on a slit lamp and the eyes were scored according to a modified Draize eye test and were histologically analyzed. Results: Pig eyeballs showed no signs of perforation, erosion, corneal opacity or other gross damage. These findings were confirmed by histological analysis. The re was no difference between control and treated rabbit eyes according to the Draize eye test score in all groups (p>0.05). All formulations showed a mean score under 1 and were classified as "non-irritating". There was no evidence of tissue toxicity in the histological analysis in all animals. Conclusion: Aqueous HPMC solutions containing GSNO and SNAC at concentrations up to 10.0 mM do not induce ocular irritation.

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Section: Discussionmentioning

confidence: 99%

Assessment of ocular surface toxicity after topical instillation of nitric oxide donors

Cariello¹,

Souza²,

Lowen³

et al. 2013

Arq. Bras. Oftalmol.

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“…The feasibility of the in situ gelling system as an ocular drug delivery should be a free flowing liquid with low viscosity at non-physiological condition to allow reproducible administration into the eye as drops; it should also undergo in situ sol-to-gel phase transition at physiological condition to form gel capable of enduring shear forces expected in the eye during and between blinking and facilitate sustained drug release (Lin and Sung, 2000;Kalam et al, 2008;Al-Kassas and El-Khatib, 2009;Liu et al, 2010). Therefore, the gelling capacity, viscosity, in vitro release study and the mucoadhesive properties of the prepared Mox ophthalmic formulations were evaluated.…”

Section: Evaluation Of Formulationsmentioning

confidence: 99%

Moxifloxacin-gelrite In Situ ophthalmic gelling system against photodynamic therapy for treatment of bacterial corneal inflammation

et al. 2011

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In this study, six in situ gelling formulations based on Gelrite were prepared and evaluated for the retained ophthalmic delivery of Moxifloxacin (Mox). The effectiveness of the best developed formula G5 was compared with photodynamic therapy (PDT), the recent expanding approach for the treatment of ophthalmologic disorders after the assessment of optimum photodynamic inactivation parameters that permit efficient pathogens eradication. It was found that, Staphylococcus aureus (S. aureus) (Gram-positive) was more susceptible to effective lethal photosensitization that reaches 93.5% reduction in viable count than Escherichia coli (E. coli) (Gramnegative) of 76.1% using 3 mg/mL Hematoporphyrin (HP), illuminated by 630 nm Light Emitting Diode (LED) at 9 J/cm(2) and incubated for 15 min. Following topical instillation of G5 to rabbits corneas, higher amount of Mox was retained in the aqueous humor up to 24 h with significant 6-fold increase in the C(max) and AUC((0-∞)) compared to vigamox commercial eye drops. After post corneal infection with S. aureus, both approaches were effectively treating the infection without causing ocular irritation or collateral damage to corneal tissue where G5 showed remarkable improvement after four days compared to seven days of PDT treatment.

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“…19 For instance, owing to the nature of sol-togel transition upon changes in pH, alginates polymers and carbopol were used to deliver ciprofloxacin, and then the antimicrobial efficiency test proved that the formulation prolonged the antimicrobial effect of ciprofloxacin. 20 However, all these environment-sensitive hydrogels have a significant weakness; that is, their response time is too slow. Hence, it is necessary to develop fast-acting hydrogels with enough mechanical strength.…”

Section: Significant and Sustained Improvement In Lung Function And Rmentioning

confidence: 99%

Recent advances in materials for extended-release antibiotic delivery system

et al. 2011

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To maintain antimicrobial activity, frequent administration of conventional formulations of many antibiotics with short half-life is necessary. Otherwise, concentration under MIC occurs frequently in the course of anti-infective treatment, which induces antibiotic resistance. By maintaining a constant plasma drug concentration over MIC for a prolonged period, extended-release dosage forms maximize the therapeutic effect of antibiotics while minimizing antibiotic resistance. Another undoubted advantage of extended-release formulation is improved patient compliance. For better release properties, many materials have been introduced into the matrix and coating extended-release system in the past few years. Materials that have been widely used in industry are hydrophilic matrix materials such as hydroxypropylmethylcellulose. The excellent biocompatibility and extensive laboratory studies provide biodegradable polymers great potential for industrial applications. In addition, it seems like the researches on tailored materials that are obtained by chemical modification of the existing materials or combination of different carriers in physical mixtures have a long way to go. Meanwhile, with the development of polymers and inorganic porous nanocarriers, nanotechnology is applied increasingly for the extended delivery of antibiotics. This review highlights the development of materials used in extended-release formulation and nanoparticles for antibiotic delivery. We also provide an overview of the antibiotic extended-release products that have provided clinical benefit or are undergoing the clinical trial.

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Ophthalmic controlled release in situ gelling systems for ciprofloxacin based on polymeric carriers

Cited by 40 publications

References 23 publications

Assessment of ocular surface toxicity after topical instillation of nitric oxide donors

Assessment of ocular surface toxicity after topical instillation of nitric oxide donors

Moxifloxacin-gelrite In Situ ophthalmic gelling system against photodynamic therapy for treatment of bacterial corneal inflammation

Recent advances in materials for extended-release antibiotic delivery system

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