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. 2011:2011:237501.
doi: 10.5402/2011/237501. Epub 2011 Aug 25.

Preparation of Fluconazole β-Cyclodextrin Complex Ocuserts: In Vitro and In Vivo Evaluation

Hindustan Abdul Ahad  1 , J Sreeramulu, B Suma Padmaja, M Narasimha Reddy, P Guru Prakash
Affiliations

Preparation of Fluconazole β-Cyclodextrin Complex Ocuserts: In Vitro and In Vivo Evaluation

Hindustan Abdul Ahad et al. ISRN Pharm. 2011.

Abstract

The main purpose of the present study was to develop ocuserts of Fluconazole β-CD (beta-cyclodextrin) complex and to evaluate both in vitro and in vivo. Fluconazole was made complex with β-CD, and the release rate was controlled by HPMC K(4)M and ethyl cellulose polymers using dibutyl Phthalate as permeability enhancer. Drug-polymer interactions were studied by Fourier transform infrared spectroscopic studies. The formulated ocuserts were tested for physicochemical parameters of in vitro release and in vivo permeation in rabbits. The optimized formulations (F-5 and F-8) were subjected to stability studies. The formulated ocuserts were found to have good physical characters, thickness, diameter, uniformity in weight, folding endurance, less moisture absorption, and controlled release of drug both in vitro and in vivo. The optimized formulations retained their characteristics even after stability studies. The study clearly showed that this technique was an effective way of formulating ocuserts for retaining the drug concentration at the intended site of action for a sufficient period of time and to elicit the desired pharmacological response.

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Figures

Figure 1
Figure 1
Various formulations of ocuserts.
Figure 2
Figure 2
Fluconazole pure drug.
Figure 3
Figure 3
Fluconazole and β-CD.
Figure 4
Figure 4
Fluconazole with HPMC.
Figure 5
Figure 5
Fluconazole with EC.
Figure 6
Figure 6
Fluconazole ocusert.
Figure 7
Figure 7
Zero-order plots.
Figure 8
Figure 8
First-order plots.
Figure 9
Figure 9
Higuchi's plots.
Figure 10
Figure 10
Korsmeyer Peppa's plots.
Figure 11
Figure 11
Hixson Crowell's plots.
Figure 12
Figure 12
Plots of in vivo cumulative drug release versus time for F-5 and F-8.
Figure 13
Figure 13
Rabbit with ocusert.
See this image and copyright information in PMC

References

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