Gels and liposomes in optimized ocular drug delivery: Studies on ciprofloxacin formulations

Budai, Lívia; Hajdú, Melinda; Budai, Marianna; Gróf, Pál; Béni, Szabolcs; Noszál, Béla; Klebovich, Imre; Antal, István

doi:10.1016/j.ijpharm.2007.04.013

Cited by 116 publications

(58 citation statements)

References 36 publications

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“…Poor bioavailability of drugs from conventional ocular dosage forms is mainly due to the precorneal loss factors, which include tear dynamics, insufficient residence time in the conjunctival sac and non-productive absorption (1)(2)(3).…”

Section: Introductionmentioning

confidence: 99%

Ciprofloxacin as Ocular Liposomal Hydrogel

Hosny

2010

AAPS PharmSciTech

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Abstract. The purpose of this study was to prepare and characterize an ocular effective prolonged-release liposomal hydrogel formulation containing ciprofloxacin. Reverse-phase evaporation was used for preparation of liposomes consisting of soybean phosphatidylcholine (PC) and cholesterol (CH). The effect of PC/CH molar ratio on the percentage drug encapsulation was investigated. The effect of additives such as stearylamine (SA) or dicetyl phosphate (DP) as positive and negative charge inducers, respectively, were studied. Morphology, mean size, encapsulation efficiency, and in vitro release of ciprofloxacin from liposomes were evaluated. For hydrogel preparation, Carbopol 940 was applied. In vitro transcorneal permeation through excised albino rabbit cornea was also determined. Optimal encapsulation efficiency of 73.04±3.06% was obtained from liposomes formulated with PC/CH at molar ratio of 5:3 and by increasing CH content above this limit, the encapsulation decreased. Positively charged liposomes showed superior entrapment efficiency (82.01±0.52) over the negatively charged and the neutral liposomes. Hydrogel containing liposomes with lipid content PC, CH, and SA in molar ratio 5:3:1, respectively, showed the best release and transcorneal permeation with the percentage permeation of 30.6%. These results suggest that the degree of encapsulation of ciprofloxacin into liposomes and prolonged in vitro release depend on composition of the vesicles. In addition, the polymer hydrogel used in preparation ensure steady and prolonged transcorneal permeation. In conclusion, ciprofloxacin liposomal hydrogel is a suitable delivery system for improving the ocular bioavailability of ciprofloxacin.

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Section: Introductionmentioning

confidence: 99%

Ciprofloxacin as Ocular Liposomal Hydrogel

Hosny

2010

AAPS PharmSciTech

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“…The gel was evaluated for viscosity, rheological property, in vitro release and ex vivo studies. The Ciprofloxacin loaded liposomes showed better entrapment efficiency due to electrostatic charge properties and showed five time enhancement in transcorneal permeation in rabbit model 28,29 .…”

Section: Work Done In Liposomal Dosagementioning

confidence: 96%

Untitled

2012

IJPSR

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The eye is the most easily reachable organ available for topical drug delivery of local as well as interiorly acting drugs. Ideal drug delivery system aims to provide loading and maintenance dose of drug while being within therapeutic limits at the desired site of action for the desired period of time. In the treatment of ocular disease, the site of action is very narrow and undesired side effects may cause serious injuries to eye tissues. Thus, ideal ocular drug delivery should be site specific, controlled release and nonirritating. Many drugs (more than 85%) belong to BCS class IV exhibiting poor solubility and permeability. Moreover; the precorneal losses like tear secretion, naso-lachrymal drainage and less permeability of corneal tissue causes only 1% absorption of instilled dose. These limitations lead to increased loading dose and dosing frequency to maintain minimum therapeutic level for action which ultimately causes over exposure of drug to eye and leads to serious side effects. Due to these hurdles of conventional drug delivery system, the vesicular drug delivery system is gaining more popularity day by day as they offer improved permeability and altered bioavailability of drug. These formulations mainly include liposome and niosome made up of phospholipids and non-ionic surfactants respectively. They are non-antigenic, biodegradable and non-irritating. The present article reveals the key-work done on vesicular drug delivery system as potential ocular drug delivery system and justifies the need for further research on vesicular drug delivery system as ocular vehicles.

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“…The bioadhesive polymer such as poly (vinyl alcohol) and polymethacrylic acid derivatives were used for gel preparation and lecithin and α-L-dipalmithoylphosphatidylcholine provided the encapsulating agent for drug into liposome. Encapsulation of the CPFX into liposomes prolonged the in vitro release of the antibacterial agent from liposomal vesicles and by use of liposomal formulation, higher drug concentration can be achieved at the site of action along with prolonged contact time, thus ocular bioavailability can be improved [54].…”

Section: Liposome Incorporated In Situ Gelmentioning

confidence: 99%

Newer Trends in In Situ Gelling Systems for Controlled Ocular Drug Delivery

Jain¹,

Kumar²,

Singh³

et al. 2016

JAPLR

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In situ -gelling systems has the great potential in the wide areas of drug delivery. The application areas of such systems are broad and these systems can be formulated not only as gels but also as in situ gelling nanospheres, microspheres and liposomes. To overcome the drawbacks associated with conventional drug delivery systems and take advantages of both solutions and gels, such as accurate dosing, ease of administration of the former and longer precorneal residence of the latter, a newer concept of in situ gelling drug delivery systems was came in light for the first time in the early 1980s. In situ gelling systems are the polymeric solutions which can be administered in solution form and immediately undergoes sol-gel phase transition in to a viscoelastic gel upon exposure to physiological conditions (e.g. pH, temperature and ionic concentration) or application of external triggers. In situ gelling systems seems to have wide applications in ocular therapy. A lot of research is going on in this area proves the fact that in situ gelling systems can be advantageous in the ocular drug delivery. In the present review we will discuss recent researches involving application of in situ gelling polymers, their applications in the various domains of drug delivery and marketed formulations based on in situ gelling systems.

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Gels and liposomes in optimized ocular drug delivery: Studies on ciprofloxacin formulations

Cited by 116 publications

References 36 publications

Ciprofloxacin as Ocular Liposomal Hydrogel

Ciprofloxacin as Ocular Liposomal Hydrogel

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Newer Trends in In Situ Gelling Systems for Controlled Ocular Drug Delivery

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