Akhgari Abbas, Iraji Pariya, Rahiman Niloufar, Hasanzade Farouji Akram, Abbaspour Mohammadreza
Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Targeted Drug Delivery Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.
Iran J Basic Med Sci. 2022 Mar;25(3):405-413. doi: 10.22038/IJBMS.2022.61563.13625.
Folic acid is an essential vitamin, labile to hydrolysis in the acidic environment of the stomach with low water solubility and bioavailability. In order to solve these problems, enteric oral folic acid-loaded microfibers with a pH-sensitive polymer by electrospinning method were prepared.
Electrospinning was performed at different folic acid ratios and voltages. Fibers were evaluated in terms of mechanical strength, acidic resistance, and drug release. Additionally, DSC (Differential Scanning Calorimetry), FTIR (Fourier-transform infrared spectroscopy), and XRD (X-ray diffraction) analyses were performed on the optimal formulation.
Drug ratio and voltage had a considerable effect on fibers' entrapment efficiency, acid resistance, and mechanical strength. Based on the obtained results, the optimum formulation containing 1.25% of the drug/polymer was prepared at 18 kV. The entrapment efficiency of the optimal sample was above 90% with an acid resistance of higher than 70%. The tensile test confirmed the high mechanical properties of the optimum microfiber. DSC and XRD tests indicated that folic acid was converted to an amorphous form in the fiber structure and the FTIR test confirmed the formation of a chemical bond between the drug and the polymer. The release of the drug from the optimal fiber was about 90% in 60 min.
In conclusion, the optimal formulation of folic acid with proper mechanical properties can be used as a candidate dosage form for further bioavailability investigations.
叶酸是一种必需维生素，在胃的酸性环境中易水解，水溶性和生物利用度低。为了解决这些问题，采用静电纺丝法制备了载有叶酸的肠溶微纤维，其采用了一种pH敏感聚合物。
在不同叶酸比例和电压下进行静电纺丝。对纤维的机械强度、耐酸性和药物释放进行了评估。此外，对最佳配方进行了差示扫描量热法（DSC）、傅里叶变换红外光谱法（FTIR）和X射线衍射法（XRD）分析。
药物比例和电压对纤维的包封率、耐酸性和机械强度有显著影响。根据所得结果，在18 kV电压下制备了含1.25%药物/聚合物的最佳配方。最佳样品的包封率高于90%，耐酸性高于70%。拉伸试验证实了最佳微纤维具有高机械性能。DSC和XRD测试表明叶酸在纤维结构中转变为无定形形式，FTIR测试证实了药物与聚合物之间形成了化学键。药物从最佳纤维中的释放率在60分钟内约为90%。
总之，具有适当机械性能的叶酸最佳配方可作为进一步生物利用度研究的候选剂型。
