Abstract

Bu çalışmada, flukonazol (FLZ) yüklü poli(laktik-ko-glikolik asit) (PLGA) nanopartikülleri (NP'ler), Candida albicans ATCC 90028'e karşı antibiyofilm aktiviteyi artırmak için polivinil alkol (PVA) ve PVA-rhamnolipid (R)'den oluşan iki farklı formülasyon ile hazırlandı. Bu formülasyonların enkapsülasyon etkinliği, ilaç yükleme kapasitesi, in vitro salınım, karakterizasyonu ve antibiyofilm aktivitesi karşılaştırıldı. NP'lerin karakterizasyonu, taramalı elektron mikroskobu (SEM) ve Zetasizer ile analiz edildi. İlaç yükleme kapasitesi ve enkapsülasyon etkinliği yüzdeleri, spektrofotometrik yöntemle ölçüldü. PLGA-NP'ler, ortalama büyüklükleri ~300 nm, küresel şekilli ve FLZ yüklü PVA ve PVA-R-PLGA-NP'lerin yüzey yükü sırasıyla -25,9±1.99, -48,1±2.46'dır. PVA-R-PLGA-NP'lerde sürekli FLZ salınımı (6 saat sonra >%60) elde edildi. PVA-FLZ-PLGA ve PVA-R-FLZ-PLGA'nın enkapsülasyon etkinliği yüzdeleri sırasıyla %50 ve %85'tir. Antibiyofilm inhibisyon yüzdeleri sırasıyla %55 ve %63'tür. Bu sonuçlar, PVA-R-FLZ-PLGA ilaç taşıma sisteminin C.albicans'ın neden olduğu enfeksiyonlarda kullanılabilecek yeni bir tedavi yaklaşımı olduğunu göstermektedir. 

EVALUATION OF THE ANTIBIOFILM EFFECT OF FLUCONAZOLE LOADED PLGA NANOPARTICLES PREPARED USING RHAMNOLIPID ON Candida albicans

Abstract

In this study, fluconazole (FLZ) loaded poly (lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) were prepared with two different formulations consisting of polyvinyl alcohol (PVA) and PVA-rhamnolipid (R) in order to improve antibiofilm activity against Candida albicans ATCC 90028. The encapsulation efficiency, drug loading capacity, in-vitro release, characterization and antibiofilm activity of these formulations were compared. Characterization of NPs were analyzed by scanning electron microscopy (SEM) and Zetasizer. Drug loading capacity and encapsulation efficiency percentages were measured by spectrophotometric method. PLGA-NPs were spherical in shape with mean sizes of ~300 nm and surface charge of FLZ loaded PVA and PVA-R-PLGA NPs -25,9±1.99, -48,1±2.46, respectively. Sustained release of FLZ (≥60% after 6 h) were obtained in PVA-R PLGA-NPs. The encapsulation efficiency percentages of PVA-FLZ-PLGA and PVA-R-FLZ-PLGA were 50% and 85%, respectively. Antibiofilm inhibition percentages are 55% and 63%, respectively. These results show that the PVA-R-FLZ-PLGA drug delivery system is a new therapeutic approach that can be used in infections caused by C. albicans. 

Keywords

• Drug delivery
• PLGA nanoparticles
• Sustained release
• Candida albicans
• Biofilm

Thanks

We thank the High Technology Research and Application Center (YUTAM) for providing research facilities to carry out this research work.

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