DEVELOPMENT OF VAGINAL IBUPROFEN MICROPARTICLES: A DoE-BASED OPTIMIZATION STUDY VAJİNAL İBUPROFEN MİKROPARTİKÜLLERİNİN GELİŞTİRİLMESİ: DoE TABANLI BİR OPTİMİZASYON ÇALIŞMASI


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Özyılmaz E. D., ÇOMOĞLU T.

Ankara Universitesi Eczacilik Fakultesi Dergisi, cilt.50, sa.2, ss.277-288, 2026 (Scopus, TRDizin)

Özet

Objective: This study aims to formulate and optimize hydroxypropyl methylcellulose (HPMC)-based microparticles for the vaginal delivery of ibuprofen using a full factorial design approach, aiming for sustained drug release, enhanced local effect, and reduced systemic exposure. Material and Method: Ibuprofen-loaded HPMC microparticles were prepared via the simple desolvation method using dichloromethane (DCM) as solvent and liquid paraffin as the continuous phase. The HPMC:DCM ratio and volume of paraffin were selected as independent variables, while particle size and drug loading efficiency were evaluated as responses. Particle characterization was performed using Zetasizer, SEM, and DSC. In vitro drug release was assessed under simulated vaginal conditions (pH 4.5) Result and Discussion: Particle sizes ranged from 1.09 to 10.23 µm with polydispersity indices below 0.5, indicating acceptable uniformity. Drug loading efficiency was between 66.47% and 89.23%, increasing with higher HPMC concentrations. In vitro release studies demonstrated sustained ibuprofen release, reaching approximately 88% over 180 minutes. ANOVA confirmed that the HPMC:DCM ratio significantly affected both particle size and drug entrapment (p < 0.0001). The optimized HPMC-based microparticles provide a promising vaginal drug delivery system for ibuprofen, offering controlled release, high drug loading, and potential for improved therapeutic efficacy with reduced systemic side effects.