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Improved corneal bioavailability of ofloxacin: biodegradable microsphere-loaded ion-activated in situ gel delivery system.

Sayed EG, Hussein AK, Khaled KA, Ahmed OA - Drug Des Devel Ther (2015)

Bottom Line: The prepared OFX formulations were then investigated in vivo compared with commercially available OFX eyedrops.Incorporation of OFX-loaded microspheres in Gelrite solution (0.4% w/v) significantly altered the release profiles of OFX-loaded microspheres in situ gel formula compared with the corresponding OFX gels and OFX microspheres.In vivo results in rabbits showed that OFX-loaded microspheres in situ gel formula improved the relative bioavailability by 11.7-fold compared with the commercially available OFX eyedrops.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Minia University, Minia, Egypt.

ABSTRACT
The aim of the study was to improve corneal penetration and bioavailability of ofloxacin (OFX) eye preparations. OFX was incorporated in poly (lactide-co-glycolide) as biodegradable microspheres using oil in oil emulsion solvent evaporation technique. The prepared OFX microspheres were then incorporated in Gelrite(®) in situ gel preparation. In addition, OFX Gelrite-based in situ gel formulations were prepared. OFX formulations were characterized for gelling capacity, viscosity, and rheological properties. Release studies for OFX microspheres, OFX in situ gel, and OFX-loaded microspheres in situ gel formulations were carried out to investigate release characteristics of the drug. The prepared OFX formulations were then investigated in vivo compared with commercially available OFX eyedrops. Results showed that the optimum Gelrite concentration was at 0.4%-0.7% w/v; the prepared formulations were viscous liquid transformed into a pourable gel immediately after the addition of simulated tear fluid with a gelling factor of 27-35. Incorporation of OFX-loaded microspheres in Gelrite solution (0.4% w/v) significantly altered the release profiles of OFX-loaded microspheres in situ gel formula compared with the corresponding OFX gels and OFX microspheres. In vivo results in rabbits showed that OFX-loaded microspheres in situ gel formula improved the relative bioavailability by 11.7-fold compared with the commercially available OFX eyedrops. In addition, the longer duration of action of OFX-loaded microspheres in situ gel formula preparations is thought to avoid frequent instillations, which improves patient tolerability and compliance.

No MeSH data available.


Related in: MedlinePlus

Concentration time profiles in aqueous humor of rabbits, following topical administration of different OFX formulations.Notes: (Inset) In vivo pharmacokinetic parameters of OFX from the studied groups. *P<0.05 compared with commercial product.Abbreviations: AUC, area under the curve maximum; AUCrel, the relative area under the curve compared with commercial product; Cmax, maximum OFX concentration in aqueous humor; OFX, ofloxacin; SD, standard deviation; Tmax, the time to reach this concentration.
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f6-dddt-9-1427: Concentration time profiles in aqueous humor of rabbits, following topical administration of different OFX formulations.Notes: (Inset) In vivo pharmacokinetic parameters of OFX from the studied groups. *P<0.05 compared with commercial product.Abbreviations: AUC, area under the curve maximum; AUCrel, the relative area under the curve compared with commercial product; Cmax, maximum OFX concentration in aqueous humor; OFX, ofloxacin; SD, standard deviation; Tmax, the time to reach this concentration.

Mentions: Aqueous humor drug concentrations following various times of instillation of 0.3 mg of OFX as microspheres, Gelrite-loaded microspheres in situ gel, and the commercially available eye drops are shown in Figure 6. Compared with the other investigated formulations, OFX microspheres showed the highest Cmax and shortest Tmax values (Figure 6, inset table). This indicates the highest rate of absorption. Commercial OFX eye drops showed the lowest Cmax, which could possibly be attributed to the rapid drainage, and hence reduced residence time, of the applied OFX dose from the commercial eye drops. OFX microspheres in Gelrite in situ gel formula showed improved Cmax data compared with the commercial product and delayed action compared to all investigated formulations. This result indicates a prolonged pattern of release and absorption from OFX microspheres in Gelrite in situ gel formula.


Improved corneal bioavailability of ofloxacin: biodegradable microsphere-loaded ion-activated in situ gel delivery system.

Sayed EG, Hussein AK, Khaled KA, Ahmed OA - Drug Des Devel Ther (2015)

Concentration time profiles in aqueous humor of rabbits, following topical administration of different OFX formulations.Notes: (Inset) In vivo pharmacokinetic parameters of OFX from the studied groups. *P<0.05 compared with commercial product.Abbreviations: AUC, area under the curve maximum; AUCrel, the relative area under the curve compared with commercial product; Cmax, maximum OFX concentration in aqueous humor; OFX, ofloxacin; SD, standard deviation; Tmax, the time to reach this concentration.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4362657&req=5

f6-dddt-9-1427: Concentration time profiles in aqueous humor of rabbits, following topical administration of different OFX formulations.Notes: (Inset) In vivo pharmacokinetic parameters of OFX from the studied groups. *P<0.05 compared with commercial product.Abbreviations: AUC, area under the curve maximum; AUCrel, the relative area under the curve compared with commercial product; Cmax, maximum OFX concentration in aqueous humor; OFX, ofloxacin; SD, standard deviation; Tmax, the time to reach this concentration.
Mentions: Aqueous humor drug concentrations following various times of instillation of 0.3 mg of OFX as microspheres, Gelrite-loaded microspheres in situ gel, and the commercially available eye drops are shown in Figure 6. Compared with the other investigated formulations, OFX microspheres showed the highest Cmax and shortest Tmax values (Figure 6, inset table). This indicates the highest rate of absorption. Commercial OFX eye drops showed the lowest Cmax, which could possibly be attributed to the rapid drainage, and hence reduced residence time, of the applied OFX dose from the commercial eye drops. OFX microspheres in Gelrite in situ gel formula showed improved Cmax data compared with the commercial product and delayed action compared to all investigated formulations. This result indicates a prolonged pattern of release and absorption from OFX microspheres in Gelrite in situ gel formula.

Bottom Line: The prepared OFX formulations were then investigated in vivo compared with commercially available OFX eyedrops.Incorporation of OFX-loaded microspheres in Gelrite solution (0.4% w/v) significantly altered the release profiles of OFX-loaded microspheres in situ gel formula compared with the corresponding OFX gels and OFX microspheres.In vivo results in rabbits showed that OFX-loaded microspheres in situ gel formula improved the relative bioavailability by 11.7-fold compared with the commercially available OFX eyedrops.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Minia University, Minia, Egypt.

ABSTRACT
The aim of the study was to improve corneal penetration and bioavailability of ofloxacin (OFX) eye preparations. OFX was incorporated in poly (lactide-co-glycolide) as biodegradable microspheres using oil in oil emulsion solvent evaporation technique. The prepared OFX microspheres were then incorporated in Gelrite(®) in situ gel preparation. In addition, OFX Gelrite-based in situ gel formulations were prepared. OFX formulations were characterized for gelling capacity, viscosity, and rheological properties. Release studies for OFX microspheres, OFX in situ gel, and OFX-loaded microspheres in situ gel formulations were carried out to investigate release characteristics of the drug. The prepared OFX formulations were then investigated in vivo compared with commercially available OFX eyedrops. Results showed that the optimum Gelrite concentration was at 0.4%-0.7% w/v; the prepared formulations were viscous liquid transformed into a pourable gel immediately after the addition of simulated tear fluid with a gelling factor of 27-35. Incorporation of OFX-loaded microspheres in Gelrite solution (0.4% w/v) significantly altered the release profiles of OFX-loaded microspheres in situ gel formula compared with the corresponding OFX gels and OFX microspheres. In vivo results in rabbits showed that OFX-loaded microspheres in situ gel formula improved the relative bioavailability by 11.7-fold compared with the commercially available OFX eyedrops. In addition, the longer duration of action of OFX-loaded microspheres in situ gel formula preparations is thought to avoid frequent instillations, which improves patient tolerability and compliance.

No MeSH data available.


Related in: MedlinePlus