Cartagena Andres Felipe, Lyra Amanda Martinez, Kapuchczinski Aline Cristina, Urban Amanda Migliorini, Esmerino Luis Antonio, Klein Traudi, Nadal Jessica Mendes, Farago Paulo Vitor, Campanha Nara Hellen
Graduate Program in Dentistry, Department of Dentistry, State University of Ponta Grossa, Ponta Grossa. Brazil.
Graduate Programs in Pharmaceutical Science, Department of Pharmacy, State University of Ponta Grossa, Ponta Grossa. Brazil.
Curr Drug Deliv. 2017;14(8):1144-1153. doi: 10.2174/1567201813666161006115041.
Miconazole nitrate has been widely employed in treatment of oral mycoses, however your immediate bio-availability and location in the affected area is critical.
The aim of this study was to prepare and evaluate Eudragit® L100 and Gantrez MS-955 microparticles containing miconazole nitrate for oral delivery.
Microparticles were prepared by spray-drying method to achieve high encapsulation efficiency and increase the drug solubility. The microparticles were formed containing 10% and 20% of drug on polymer Eudragit® L100 (E10 and E20), Gantrez MS-955 (G10 and G20) or their combination (EG10 and EG20). The influence of formulation factors (polymer:drug ratio, type of polymer) on yield percent, encapsulation efficiency, particle size, Fourier-transformed infrared spectroscopy (FTIR), X-ray diffraction, differential scanning calorimetry, in vitro drug release and antifungal activity were investigated.
Acceptable yield, micrometer-sized and drug-loading efficiencies higher than 89% were obtained. No change in FTIR assignments was recorded after the microencapsulation procedure. X-ray and differential scanning calorimetry studies revealed amorphous/non-crystalline formulations. Miconazole nitrate-microparticles provided a remarkable increase of dissolution rate of the drug. Miconazole nitrate and G10, G20 and EG20 microparticles fitted to biexponential kinetic model, and E10, E20 and EG10 microparticles, monoexponential kinetic model. The antifungal activity test demonstrated that miconazole nitrate-microparticles possessed the same anti-Candida albicans activity as the pure drug.
These results indicate that miconazole nitrate-microparticles are feasible carriers for increased release of miconazole at oral environment.
硝酸咪康唑已广泛用于治疗口腔真菌病，但其即时生物利用度以及在感染部位的分布情况至关重要。
本研究旨在制备并评估含硝酸咪康唑的尤特奇® L100和甘泰雷斯MS - 955微粒用于口服给药。
采用喷雾干燥法制备微粒以实现高包封率并提高药物溶解度。制备的微粒中药物在尤特奇® L100（E10和E20）、甘泰雷斯MS - 955（G10和G20）聚合物上的含量为10%和20%，或二者的组合（EG10和EG20）。研究了配方因素（聚合物与药物比例、聚合物类型）对产率、包封率、粒径、傅里叶变换红外光谱（FTIR）、X射线衍射、差示扫描量热法、体外药物释放和抗真菌活性的影响。
获得了可接受的产率、微米级粒径以及高于89%的载药效率。微囊化过程后FTIR谱峰归属未发生变化。X射线和差示扫描量热法研究表明制剂为无定形/非晶态。硝酸咪康唑微粒显著提高了药物的溶解速率。硝酸咪康唑与G10、G20和EG20微粒符合双指数动力学模型，而E10、E20和EG10微粒符合单指数动力学模型。抗真菌活性试验表明硝酸咪康唑微粒具有与纯药物相同的抗白色念珠菌活性。
这些结果表明硝酸咪康唑微粒是在口腔环境中增加咪康唑释放的可行载体。
