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Formulation and In Vitro Characterization of Thiolated Buccoadhesive Film of Fluconazole

Abstract

The present work is focused on the development of thiolated film for fluconazole buccal delivery. To this end, unmodified polymers chitosan and sodium carboxymethylcellulose (NaCMC) backbone was covalently modified by thioglycolic acid (TGA) and cysteine, respectively. The thiolated buccoadhesive film was evaluated in terms of thickness, weight uniformity, water-uptake capacity, drug content, and release patterns. Moreover, mucoadhesion profile was investigated on buccal mucosa. The resulting chitosan–TGA and NaCMC–cysteine conjugates displayed 171 ± 13 and 380 ± 19 μmol thiol groups per gram of polymer (mean ± SD; n = 3), respectively. The water binding capacity of the thiolated film was significantly ∼2-fold higher (p < 0.05) as compared to unmodified film. The obtained thiolated film displayed 5.8-fold higher mucoadhesive properties compared with corresponding film. Controlled release of drugs from film was observed over 8 h. The transport of fluconazole across excised buccal mucosa was enhanced up to 17-fold in comparison with fluconazole applied in buffer. Based on these findings, thiolated film seems to be promising for fluconazole buccal delivery.

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Acknowledgments

The authors acknowledge the financial support provided by the Quaid-i-Azam University Research Fund for this work, and we are immensely grateful to Dr. Nasir Mehmood Ahmad (School of Chemical and Materials Engineering, NUST, Islamabad, Pakistan) in helping us to get the FTIR of our samples done at School of Chemical and Materials Engineering, NUST, Islamabad, Pakistan.

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Correspondence to Gul Shahnaz.

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Guest Editors: Claudio Salomon, Francisco Goycoolea, and Bruno Moerschbacher

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Naz, K., Shahnaz, G., Ahmed, N. et al. Formulation and In Vitro Characterization of Thiolated Buccoadhesive Film of Fluconazole. AAPS PharmSciTech 18, 1043–1055 (2017). https://doi.org/10.1208/s12249-016-0607-y

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KEY WORDS

  • buccal delivery
  • controlled release
  • mucoadhesion
  • polymeric buccoadhesive film
  • thiolated polymers