DEVELOPMENT OF VAGINAL IBUPROFEN MICROPARTICLES: A DoE-BASED OPTIMIZATION STUDY

Öz

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.

Anahtar Kelimeler

• Factorial design
• microparticle
• ibuprofen
• vaginal drug delivery

VAJİNAL İBUPROFEN MİKROPARTİKÜLLERİNİN GELİŞTİRİLMESİ: DoE TABANLI BİR OPTİMİZASYON ÇALIŞMASI

Öz

Amaç: Bu çalışma, sürekli ilaç salınımı, geliştirilmiş lokal etki ve azaltılmış sistemik maruziyet hedefleyen tam faktöriyel tasarım yaklaşımı kullanarak ibuprofenin vajinal taşıma için hidroksipropil metilselüloz (HPMC) bazlı mikropartikülleri formüle etmeyi ve optimize etmeyi amaçlamaktadır.

Gereç ve Yöntem: İbuprofen yüklü HPMC mikropartikülleri, çözücü olarak diklorometan (DCM) ve sürekli faz olarak sıvı parafin kullanılarak basit desolvasyon yöntemi ile hazırlanmıştır. HPMC:DCM oranı ve parafin hacmi bağımsız değişkenler olarak seçilirken, partikül boyutu ve ilaç yükleme verimliliği bağımlı değişkenler olarak değerlendirilmiştir. Partikül karakterizasyonu Zetasizer, SEM ve DSC kullanılarak gerçekleştirilmiştir. İn vitro ilaç salınımı simüle edilmiş vajinal koşullar altında (pH 4,5) değerlendirilmiştir.

Sonuç ve Tartışma: Partikül boyutları 1.09 ila 10.23 µm arasında değişmiş ve polidispersite indeksleri 0.5'in altında olup kabul edilebilir bir tekdüzelik olduğunu göstermektedir. İlaç yükleme verimliliği %66.47 ile %89.23 arasında ve daha yüksek HPMC konsantrasyonlarıyla yükleme verimliliği artmaktadır. İn vitro ilaç salım çalışmaları, 180 dakika boyunca yaklaşık %88'e ulaşan sürekli ibuprofen salımını göstermiş ve ANOVA, HPMC:DCM oranının hem parçacık boyutunu hem de ilaç tutulmasını önemli ölçüde etkilediğini doğrulamıştır (p < 0,0001). Optimize edilmiş HPMC tabanlı mikropartiküller, kontrollü salım, yüksek ilaç yüklemesi ve azaltılmış sistemik yan etkilerle iyileştirilmiş terapötik etkinlik potansiyeli sunan ibuprofen için umut verici bir vajinal ilaç verme sistemi sağlamaktadır.

Anahtar Kelimeler

• Faktöriyel tasarım
• mikropartikül
• ibuprofen
• vajinal ilaç taşıma

Kaynakça

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