Rathor Sandeep, Bhatt Dinesh Chandra
Department of Pharmaceutical Sciences, Guru Jambheswar University of Sciences & Technology, Hisar, Haryana 125001, India.
Department of Pharmaceutics, School of Medical and Applied Sciences, Sohna Road, Gurugram, Haryana 122103 India.
Pharm Nanotechnol. 2022;10(2):125-136. doi: 10.2174/2211738510666220328151512.
The proposed study was aimed to formulate and evaluate the glipizidephospholipid nano-complex. Since glipizide is a poorly soluble drug, its complexation with phospholipids is an ideal approach to improving solubility.
To improve the oral potency of glipizide, its phospholipid complex was prepared by employing the solvent evaporation method. The formulations were characterized using DSC, FTIR, PXRD, SEM, TEM, and hot stage microscopy (HSM). Solubility tests of the glipizidephospholipid nano-complex revealed a significant increase in aqueous solubility compared to glipizide's physical combination. The oral bioavailability of the glipizide-phospholipid nanocomplex was measured by using HPLC in Wistar rats' plasma. FTIR and PXRD results revealed no significant interaction between the drug and the phospholipid in the formulation. SEM and TEM studies confirmed the morphology of the formulation assuring the conversion of crystalline form into an amorphous structure.
The glipizide-phospholipid nano-complex had a greater peak plasma concentration (5.2 vs. 3.8 g/mL), a larger AUC (26.31 vs. 19.55 μgh/L), and a longer T1/2 (2.1 vs. 4.1 h) than free glipizide, indicating that it improved drug dissolution rate.
The outcomes suggested that a phospholipid complexation is a potential approach to increasing water-insoluble drugs' oral bioavailability.
本拟进行的研究旨在制备并评估格列吡嗪磷脂纳米复合物。由于格列吡嗪是一种难溶性药物，将其与磷脂复合是提高溶解度的理想方法。
为提高格列吡嗪的口服效能，采用溶剂蒸发法制备其磷脂复合物。通过差示扫描量热法（DSC）、傅里叶变换红外光谱法（FTIR）、粉末X射线衍射法（PXRD）、扫描电子显微镜（SEM）、透射电子显微镜（TEM）和热台显微镜（HSM）对制剂进行表征。格列吡嗪磷脂纳米复合物的溶解度测试显示，与格列吡嗪的物理混合物相比，其水溶性显著增加。采用高效液相色谱法（HPLC）测定Wistar大鼠血浆中格列吡嗪磷脂纳米复合物的口服生物利用度。FTIR和PXRD结果显示制剂中药物与磷脂之间无显著相互作用。SEM和TEM研究证实了制剂的形态，确保了晶型向无定形结构的转变。
与游离格列吡嗪相比，格列吡嗪磷脂纳米复合物具有更高的血浆峰浓度（5.2对3.8μg/mL）、更大的曲线下面积（AUC，26.31对19.55μg·h/L）和更长的半衰期（T1/2，2.1对4.1小时），表明其提高了药物溶解速率。
结果表明，磷脂复合是提高水不溶性药物口服生物利用度的一种潜在方法。
