Thammasat University Research Unit in Smart Materials and Innovative Technology for Pharmaceutical Applications (SMIT-Pharm), Faculty of Pharmacy, Thammasat University, Pathumthani 12120, Thailand.
Pharmaceutical Intellectual Center "Prachote Plengwittaya", Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Int J Mol Sci. 2024 May 16;25(10):5413. doi: 10.3390/ijms25105413.
Fluconazole (FZ) is a potential antifungal compound for treating superficial and systemic candidiasis. However, the use of conventional oral drug products has some limitations. The development of buccal film may be a potential alternative to oral formulations for FZ delivery. The present study involved the development of novel FZ-loaded solid lipid nanoparticles (FZ-SLNs) in pectin solutions and the investigation of their particle characteristics. The particle sizes of the obtained FZ-SLNs were in the nanoscale range. To produce pectin films with FZ-SLNs, four formulations were selected based on the small particle size of FZ-SLNs and their suitable polydispersity index. The mean particle sizes of all chosen FZ-SLNs formulations did not exceed 131.7 nm, and the mean polydispersity index of each formulation was less than 0.5. The properties of films containing FZ-SLNs were then assessed. The preparation of all FZ-SLN-loaded pectin films provided the mucoadhesive matrices. The evaluation of mechanical properties unveiled the influence of particle size variation in FZ-SLNs on the integrity of the film. The Fourier-transform infrared spectra indicated that hydrogen bonds could potentially form between the pectin-based matrix and the constituents of FZ-SLNs. The differential scanning calorimetry thermogram of each pectin film with FZ-SLNs revealed that the formulation was thermally stable and behaved in a solid state at 37 °C. According to a drug release study, a sustained drug release pattern with a burst in the initial stage for all films may be advantageous for reducing the lag period of drug release. All prepared films with FZ-SLNs provided a sustained release of FZ over 6 h. The films containing FZ-SLNs with a small particle size provided good permeability across the porcine mucosa. All film samples demonstrated antifungal properties. These results suggest the potential utility of pectin films incorporating FZ-SLNs for buccal administration.
氟康唑（FZ）是一种治疗浅表和全身念珠菌病的潜在抗真菌化合物。然而，传统的口服药物产品有一些局限性。颊膜的开发可能是口服制剂用于 FZ 给药的潜在替代方法。本研究涉及在果胶溶液中开发新型 FZ 负载的固体脂质纳米粒（FZ-SLNs），并研究其颗粒特性。所得到的 FZ-SLNs 的粒径在纳米范围内。为了生产含有 FZ-SLNs 的果胶膜，根据 FZ-SLNs 的小粒径和合适的多分散指数选择了四种配方。所有选定的 FZ-SLNs 配方的平均粒径均不超过 131.7nm，且每个配方的平均多分散指数均小于 0.5。然后评估了含有 FZ-SLNs 的膜的性能。所有 FZ-SLN 负载的果胶膜的制备均提供了粘膜粘附基质。机械性能评估揭示了 FZ-SLNs 中粒径变化对膜完整性的影响。傅里叶变换红外光谱表明，果胶基基质与 FZ-SLNs 的成分之间可能形成氢键。每个含有 FZ-SLNs 的果胶膜的差示扫描量热法图谱表明，制剂在 37°C 下热稳定且呈固态。根据药物释放研究，所有膜在初始阶段均有药物突释的持续药物释放模式可能有利于减少药物释放的滞后期。所有含有 FZ-SLNs 的制备膜均能在 6 小时内持续释放 FZ。含有粒径较小的 FZ-SLNs 的膜提供了良好的跨猪粘膜渗透性。所有膜样品均表现出抗真菌性能。这些结果表明，含有 FZ-SLNs 的果胶膜用于颊部给药具有潜在的应用价值。
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