Resorbable Beads Provide Extended Release of Antifungal Medication: In Vitro and In Vivo Analyses

• Main Authors: Yung-Heng Hsu (Author), Huang-Yu Chen (Author), Jin-Chung Chen (Author), Yi-Hsun Yu (Author), Ying-Chao Chou (Author), Steve Wen-Neng Ueng (Author), Shih-Jung Liu (Author)
• Format: Book
• Published: MDPI AG, 2019-10-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 1999-4923; 10.3390/pharmaceutics11110550
• Keywords: fluconazole; orthopedic infection; poly(<span style="font-variant: small-caps">d</span>,<span style="font-variant: small-caps">l</span>-lactide-<i>co</i>-glycolide) beads; sustained release; Pharmacy and materia medica; RS1-441
• Source: Pharmaceutics, Vol 11, Iss 11, p 550 (2019)

Fungal osteomyelitis has been difficult to treat, with first-line treatments consisting of implant excision, radical debridement, and local release of high-dose antifungal agents. Locally impregnated antifungal beads are another popular treatment option. This study aimed to develop biodegradable antifungal-agent-loaded Poly(<span style="font-variant: small-caps;">d</span>,<span style="font-variant: small-caps;">l</span>-lactide-<i>co</i>-glycolide) (PLGA) beads and evaluate the in vitro/in vivo release patterns of amphotericin B and fluconazole from the beads. Beads of different sizes were formed using a compression-molding method, and their morphology was evaluated via scanning electron microscopy. Intrabead incorporation of antifungal agents was evaluated via Fourier-transform infrared spectroscopy, and in vitro fluconazole liberation curves of PLGA beads were inspected via high-performance liquid chromatography. When we implanted the drug-incorporated beads into the bone cavity of rabbits, we found that a high level of fluconazole (beyond the minimum therapeutic concentration [MTC]) was released for more than 49 d in vivo. Our results indicate that compression-molded PLGA/fluconazole beads have potential applications in treating bone infections.