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Bigels based on polyelectrolyte complexes as vaginal drug delivery systems.

Raúl Cazorla-Luna¹, Fernando Notario-Pérez², Araceli Martín-Illana¹

¹Departamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n 28040, Madrid, Spain.

International Journal of Pharmaceutics

|December 10, 2024

Summary

New chitosan-based bigels form polyelectrolyte complexes for pH-independent drug release in vaginal environments. These versatile bigels offer tunable properties, improving upon current vaginal drug delivery systems.

Keywords:

Controlled drug release Electrochemical impedance Freeze-drying HIV/AIDS Mucoadhesion Tenofovir pH-dependent release

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Area of Science:

Materials Science
Polymer Chemistry
Pharmaceutical Sciences

Background:

Bigels incorporating cationic chitosan and anionic polymers (karaya gum, pectin, xanthan gum) were prepared.
Formation of polyelectrolyte complexes between these polymers modifies bigel characteristics.
Freeze-dried bigels were tested for vaginal environment conditions.

Purpose of the Study:

To evaluate the swelling and drug release profiles of bigels in simulated vaginal conditions.
To investigate the impact of polyelectrolyte complex formation on drug release.
To assess the influence of polymer composition on bigel properties and mucoadhesivity.

Main Methods:

Preparation of bigels using chitosan and anionic polymers.
Freeze-drying of bigels.
Evaluation of swelling and drug release in simulated vaginal media (normal and post-ejaculation).

Main Results:

Polyelectrolyte complex formation resulted in pH-independent sustained drug release.
Predominance of one polymer led to pH-dependent drug release, potentially useful therapeutically.
Increased chitosan content improved mechanical properties; increased anionic polymer enhanced mucoadhesivity.

Conclusions:

The developed bigels offer tunable physicochemical properties for vaginal drug delivery.
Polyelectrolyte complex formation is key to achieving pH-independent sustained release.
These versatile bigel systems present advantages over existing vaginal drug delivery formulations.