Role of Pluronic F127 micelles in enhancing ocular delivery of ciprofloxacin

Taha, Ehab I.; Badran, Mohamed M.; El-Anazi, Magda H.; Bayomi, Mohsen A.; El-Bagory, Ibrahim M.

doi:10.1016/j.molliq.2014.09.021

Cited by 42 publications

(10 citation statements)

References 24 publications

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“…The AH level was increased by ~0.3-fold when compared to marketed ophthalmic solution (53). In another study, 50 μL of CIP loaded pluronic micelles (0.3 % w/v) enhanced AH concentration of CIP by 10%, 2 h post topical application, when compared to commercial CIP eye drops (54). In the present study ocular bioavailability of CIP was enhanced in the anterior and posterior segment ocular tissues, ranging from ~3–5-fold increase with PEG-CIP-NLC formulation, in comparison to control marketed formulation.…”

Section: Discussionmentioning

confidence: 96%

Ocular disposition of ciprofloxacin from topical, PEGylated nanostructured lipid carriers: Effect of molecular weight and density of poly (ethylene) glycol

Balguri

Adelli

Janga

et al. 2017

International Journal of Pharmaceutics

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Ciprofloxacin (CIP) is an antibacterial agent prescribed for the treatment of ocular infections. The objective of the present project is to investigate the effect of surface PEG functionalization of the Nano structured lipid carriers (NLCs) on formulation stability, ocular penetration and distribution. CIP NLCs were tested with different molecular weight (poly ethylene glycol) PEGs ranging from (2K to 20K) grafted onto the phospholipid and with different chain lengths (14–18 carbons) of phospholipids derivatized with PEG-2K. Drug load in the formulations was maintained at 0.3% w/v. Formulations prepared were evaluated with respect to in vitro release, transcorneal permeation, autoclavability, morphological characteristics and in vivo ocular tissue distribution. Scanning Transmission electron microscopy (STEM) studies revealed that the PEG-CIP-NLCs were spherical in shape. Transcorneal penetration of CIP was optimum with PEG molecular weight in between 2K to 10K. Carbon chain length of the phospholipid, however, did not affect transcorneal penetration of CIP. In vivo ocular tissue CIP concentrations attained from the various formulations was consistent with the in vitro data obtained. The results suggest that surface functionalization of PEGs, within a specified range of molecular weight and surface packing density, significantly enhance trans-ocular penetration and impart sterilization-stabilization characteristics into the formulations.

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Section: Discussionmentioning

confidence: 96%

Ocular disposition of ciprofloxacin from topical, PEGylated nanostructured lipid carriers: Effect of molecular weight and density of poly (ethylene) glycol

Balguri

Adelli

Janga

et al. 2017

International Journal of Pharmaceutics

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“…It seems that polymeric micelles have higher capacity for drug loading when a higher drug concentration is used. It was reported that polymeric micelles increased ciprofloxacin solubility in aqueous environment with different pH values [ 38 ], therefore, it seems that polymeric micelles increase ciprofloxacin aqueous solubility by providing a sufficient amount of EE%. Contour plots of the relation between the independent variables and P.Z, EE% are shown in Figure 1 .…”

Section: Resultsmentioning

confidence: 99%

Permeability of Ciprofloxacin-Loaded Polymeric Micelles Including Ginsenoside as P-glycoprotein Inhibitor through a Caco-2 Cells Monolayer as an Intestinal Absorption Model

2018

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The low oral bioavailability of ciprofloxacin is associated with two distinct challenges: its low aqueous solubility and efflux by p-glycoproteins (P-gp) in the intestinal membrane. Several studies were conducted in order to improve its solubility and permeability through the gastrointestinal membrane. In this study, in a full factorial design study, eight polymeric micelles were prepared and their characteristics, including particle size, loading and release rate were evaluated. Polymeric micelles demonstrated particle sizes below 190 nm and 27–88% loading efficiency. Drug release was affected by drug solubility, polymeric micelle erosion and swelling in simulated gastrointestinal fluids. An optimized polymeric micelle was prepared based on appropriate characteristics such as high drug loading and low particle size; and was used for a permeation study on Caco-2 cells. Optimized polymeric micelles with and without ginsenoside and ginsenoside alone enhanced drug permeability through Caco-2 cells significantly in the absorptive direction. The effect of ginsenoside was dose dependent and the maximum effect was seen in 0.23 mg/mL concentration. Results showed that P-gp may not be responsible for ciprofloxacin secretion into the gut. The main mechanism of ciprofloxacin transport through Caco-2 cells in both directions is active diffusion and P-gp has inhibitory effects on ciprofloxacin permeability in the absorptive direction that was blocked by ginsenoside and micelles without ginsenoside.

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“…Taha et al reported enhanced bioavailability of ciprofloxacin using polymeric micelles of Pluronic R F127. They observed a statistically significant increase in the area under the aqueous humor concentration versus time curve in comparison to the marketed formulation [100].…”

Section: Ethylene Oxide and Propylene Oxide-based Polymeric Micellesmentioning

confidence: 97%

Recent Advances in Topical Nano drug-delivery Systems for the Anterior Ocular Segment

2018

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Over the past decade, there has been a rise in the number of clinical cases of moderate to severe anterior segment ocular diseases. Conventional topical ophthalmic formulations have several limitations - to address which, novel drug-delivery systems are needed. Additionally, formidable physiological barriers limit ocular bioavailability through the topical route of application. During the last decade, various nano-scaled ocular drug-delivery strategies have been reported. Some of these exploratory, topical, noninvasive approaches have shown promise in improving penetration into the anterior segment tissues of the eye. In this article, we review the available literature with respect to the safety, efficiency and effectiveness of these nano systems.

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Role of Pluronic F127 micelles in enhancing ocular delivery of ciprofloxacin

Cited by 42 publications

References 24 publications

Ocular disposition of ciprofloxacin from topical, PEGylated nanostructured lipid carriers: Effect of molecular weight and density of poly (ethylene) glycol

Ocular disposition of ciprofloxacin from topical, PEGylated nanostructured lipid carriers: Effect of molecular weight and density of poly (ethylene) glycol

Permeability of Ciprofloxacin-Loaded Polymeric Micelles Including Ginsenoside as P-glycoprotein Inhibitor through a Caco-2 Cells Monolayer as an Intestinal Absorption Model

Recent Advances in Topical Nano drug-delivery Systems for the Anterior Ocular Segment

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