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Bioadhesive films containing fluconazole for mucocutaneous candidiasis.

Patel SK, Shah DR, Tiwari S - Indian J Pharm Sci (2015 Jan-Feb)

Bottom Line: Bioadhesive strength was found to be more than 18 g.Microenvironment pH was near to 7.0 for most of the formulations.As revealed in FT-IR and DSC studies, drug was found to be compatible with the excipients used in this study.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Maliba Pharmacy College, Uka Tarasadia University, Bardoli-394 350, India.

ABSTRACT
Fluconazole is a broad spectrum antifungal agent that has been extensively applied for the management of oral, pharyngeal and cutaneous candidiasis. Fluconazole has a high volume of distribution (0.55-0.65 l/kg) and has systemic toxicity due to high drug-drug interaction. The present study focuses on the formulation of bioadhesive film as a controlled release carrier for fluconazole. The formulation was intended to provide localized delivery of fluconazole exclusively at the site of infection, thereby reducing its total dose and hence, dose-related toxicities. Bioadhesive films were prepared by solvent casting method using sodium alginate and polyvinyl alcohol alone as well as in various combinations. Prepared films were evaluated for physical characteristics like, weight and content uniformity, film thickness, swelling index, microenvironment pH and folding endurance. In vitro drug release, in vitro and ex vivo residence time, bioadhesive strength and skin irritation were also studied. Accelerated stability study was conducted on the optimized formulation as per ICH guidelines. Weight of all the films were not more than 20 mg. Thickness of the films ranged between 0.09 to 0.15 mm whereas swelling indices showed a high extent of variation. Films composed of polyvinyl alcohol alone provided a swelling index of 6%. Bioadhesive strength was found to be more than 18 g. Microenvironment pH was near to 7.0 for most of the formulations. Ex vivo residence time of optimized batch was more than 5 h and it provided controlled drug release up to 8 h. As revealed in FT-IR and DSC studies, drug was found to be compatible with the excipients used in this study.

No MeSH data available.


Related in: MedlinePlus

DSC thermograms of FLZ and physical mixture of FLZ and polymers.Differential scanning calorimetry (DSC) thermograms of (a) pure fluconazole (FLZ) and (b) physical mixture of fluconazole and polymers.
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Figure 1: DSC thermograms of FLZ and physical mixture of FLZ and polymers.Differential scanning calorimetry (DSC) thermograms of (a) pure fluconazole (FLZ) and (b) physical mixture of fluconazole and polymers.

Mentions: DSC thermograms revealed a sharp characteristic, endothermic melting peak of FLZ at 136.35° (fig. 1a), which was indicative of the pure state of the drug. Recrystallized forms of FLZ showed an additional endothermic peak at 102.30° which could be due to effect of bound solvent used during recrystallization. Certain amount of solvent remains as bound solvent within the crystal lattice which cannot be removed through normal drying procedure. In case of physical mixtures of drug and polymer (SA and PVA) a sharp endothermic peak of the drug was observed at the melting temperature 140.60° (fig. 1b). These results demonstrated that FLZ did not interact with the chosen additives[22].


Bioadhesive films containing fluconazole for mucocutaneous candidiasis.

Patel SK, Shah DR, Tiwari S - Indian J Pharm Sci (2015 Jan-Feb)

DSC thermograms of FLZ and physical mixture of FLZ and polymers.Differential scanning calorimetry (DSC) thermograms of (a) pure fluconazole (FLZ) and (b) physical mixture of fluconazole and polymers.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4355883&req=5

Figure 1: DSC thermograms of FLZ and physical mixture of FLZ and polymers.Differential scanning calorimetry (DSC) thermograms of (a) pure fluconazole (FLZ) and (b) physical mixture of fluconazole and polymers.
Mentions: DSC thermograms revealed a sharp characteristic, endothermic melting peak of FLZ at 136.35° (fig. 1a), which was indicative of the pure state of the drug. Recrystallized forms of FLZ showed an additional endothermic peak at 102.30° which could be due to effect of bound solvent used during recrystallization. Certain amount of solvent remains as bound solvent within the crystal lattice which cannot be removed through normal drying procedure. In case of physical mixtures of drug and polymer (SA and PVA) a sharp endothermic peak of the drug was observed at the melting temperature 140.60° (fig. 1b). These results demonstrated that FLZ did not interact with the chosen additives[22].

Bottom Line: Bioadhesive strength was found to be more than 18 g.Microenvironment pH was near to 7.0 for most of the formulations.As revealed in FT-IR and DSC studies, drug was found to be compatible with the excipients used in this study.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Maliba Pharmacy College, Uka Tarasadia University, Bardoli-394 350, India.

ABSTRACT
Fluconazole is a broad spectrum antifungal agent that has been extensively applied for the management of oral, pharyngeal and cutaneous candidiasis. Fluconazole has a high volume of distribution (0.55-0.65 l/kg) and has systemic toxicity due to high drug-drug interaction. The present study focuses on the formulation of bioadhesive film as a controlled release carrier for fluconazole. The formulation was intended to provide localized delivery of fluconazole exclusively at the site of infection, thereby reducing its total dose and hence, dose-related toxicities. Bioadhesive films were prepared by solvent casting method using sodium alginate and polyvinyl alcohol alone as well as in various combinations. Prepared films were evaluated for physical characteristics like, weight and content uniformity, film thickness, swelling index, microenvironment pH and folding endurance. In vitro drug release, in vitro and ex vivo residence time, bioadhesive strength and skin irritation were also studied. Accelerated stability study was conducted on the optimized formulation as per ICH guidelines. Weight of all the films were not more than 20 mg. Thickness of the films ranged between 0.09 to 0.15 mm whereas swelling indices showed a high extent of variation. Films composed of polyvinyl alcohol alone provided a swelling index of 6%. Bioadhesive strength was found to be more than 18 g. Microenvironment pH was near to 7.0 for most of the formulations. Ex vivo residence time of optimized batch was more than 5 h and it provided controlled drug release up to 8 h. As revealed in FT-IR and DSC studies, drug was found to be compatible with the excipients used in this study.

No MeSH data available.


Related in: MedlinePlus