Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.
Pharm Dev Technol. 2021 Mar;26(3):316-327. doi: 10.1080/10837450.2020.1870237. Epub 2021 Jan 6.
In this study, chitosan (CS) caged classic liposomes (CLs) and flexible liposomes (FLs) were developed to enhance the oral bioavailability of rivaroxaban (RVX) in the fasted condition. The prepared formulations were subjected to physicochemical characterization included: FTIR, DSC, zeta potential, particle size, polydispersity index, entrapment efficiency, dissolution, and transmission electron microscope imaging. The selected formulation (RVX-TFL2) composed of PL S100/Tween 80 (85/15% w/w) and coated with CS solution in the strength of (0.2% w/v) had a particle size of 105.67 nm, a zeta potential of +5.67 mV and EE of 96.07%. Compared to RXV suspension, the pharmacokinetic parameters ( , AUC, and AUC) of RVX-TFL2 showed no statistically significant difference ( > 0.05) in the fasted and fed test animals. Besides, RVX bioavailability with RVX-TFL2 was improved by 59.66% and 26.97% in the fed and fasted states, respectively, compared to RVX suspension in the fed state. The result highlighted the efficacy of the prepared liquid formulation comprising CS coated liposomes in improving the oral bioavailability of RVX regardless of the fed state. Moreover, the studied liquid formulation could be utilized in developing a liquid dosage form that might be useful as a pediatric formulation of RVX.
在这项研究中，壳聚糖（CS）笼状经典脂质体（CL）和柔性脂质体（FL）被开发出来，以提高利伐沙班（RVX）在空腹条件下的口服生物利用度。所制备的制剂进行了物理化学特性分析，包括：傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）、Zeta 电位、粒径、多分散指数、包封效率、溶解度和透射电子显微镜成像。选定的制剂（RVX-TFL2）由 PL S100/Tween 80（85/15%w/w）组成，并涂覆有 CS 溶液（强度为 0.2%w/v），粒径为 105.67nm，Zeta 电位为+5.67mV，EE 为 96.07%。与 RVX 混悬剂相比，RVX-TFL2 在空腹和进食的动物中的药代动力学参数（ 、AUC 和 AUC ）没有统计学上的显著差异（ > 0.05）。此外，与 RVX 混悬剂在进食状态相比，RVX-TFL2 使 RVX 的生物利用度在进食和空腹状态下分别提高了 59.66%和 26.97%。结果表明，包含 CS 包被脂质体的制备液体制剂在改善 RVX 的口服生物利用度方面是有效的，而不管进食状态如何。此外，所研究的液体制剂可用于开发液体制剂，可能对 RVX 的儿科制剂有用。
