Development of mucoadhesive vaginal films with metronidazole using Poly(2-ethyl-2-oxazoline) – Polycarbophil blends via hot melt extrusion
Akhmetova, M. K., Abilova, G. K., Duisengali, A. B., Nurlybaeva, T. A., Uzakbaeva, S. S., Irmukhametova, G. S., Bekeshev, A. Z. and Khutoryanskiy, V.
It is advisable to refer to the publisher's version if you intend to cite from this work. See Guidance on citing. To link to this item DOI: 10.1016/j.eurpolymj.2025.114175 Abstract/SummaryMucoadhesive vaginal films are increasingly regarded as a versatile platform for local drug delivery, offering prolonged mucosal retention, ease of administration, and enhanced bioavailability. In this study, vaginal films based on blends of poly(2-ethyl-2-oxazoline) (POZ) and polycarbophil (PC) were developed and characterized, incorporating metronidazole as a poorly soluble antimicrobial drug. The films were prepared using hot-melt extrusion. Their physicochemical and mechanical properties, mucoadhesive performance, and ex vivo retention on the mucosal surface were studied Particular attention was given to the effects of polymer ratio and plasticizer content on these characteristics. Key findings revealed that incorporating polycarbophil into POZ-based films significantly enhanced mucoadhesive strength, particularly in formulations containing glycerol as a plasticizer, which provided improved flexibility and adhesion. In ex vivo studies using sheep vaginal mucosa, POZ/PC films exhibited strong retention, with the POZ/PC (80:20) formulation showing significantly longer adhesion under simulated physiological fluid flow. Differential scanning calorimetry analysis confirmed partial amorphization of metronidazole in the films, reducing its crystallinity from 100 % to ∼ 65–70 %. Additionally, the films provided sustained drug release and demonstrated notable antimicrobial activity against S. aureus and E. coli.
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