Formulation studies of benzydamine mucoadhesive formulations for vaginal administration

Abstract

Background: Vaginal cavity represents a good site for drug administration and delivery. Aim: The aim of this work was the design of new mucoadhesive semisolid dosage forms for vaginal delivery of benzydamine. Method: Simple gels, obtained by using sodium carboxymethylcellulose (NaCMC) and hydroxyethylcellulose (HEC), were employed as water phase of an oil-in-water emulsion (O/W cream) to obtain emulgels, more stable and manageable than gels. Successively, in order to modify the emulgel consistency, the ingredient cetostearylic alcohol was replaced by the same amount of gel or vaseline. All the preparations were submitted to mucoadhesion and rheological, extrusion, and release studies and compared to market vaginal cream Tantum Rosa®. Results: HEC formulations showed good drug release profiles and good rheological behavior but low mucoadhesion strength, whereas NaCMC (4% gel) formulations had better drug release and very high mucoadhesive strength. However, the presence of NaCMC 4% conferred too much viscosity to the preparation. Taking into consideration all performances, the most suitable formulations for vaginal applications resulted in those containing NaCMC (3% gel) and with gel replacing cetostearylic alcohol as they showed good ex vivo performances in terms of manageability and high bioadhesion to vaginal mucosa.

Key words:

• Benzydamine
• emulgels
• mucoadhesion
• rheology
• vaginal inflammation

Acknowledgments

Authors are very much grateful to Dr. Giampiero Guerri from USL N 1 Città di Castello (Perugia, Italy) for providing porcine mucosa to perform ex vivo experiments and Mr. Marco Marani from Dipartimento di Chimica e Tecnologia del Farmaco (Perugia, Italy) for the precious collaboration and technical assistance.