Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Al-Jouf, Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Drug Deliv. 2021 Dec;28(1):2562-2573. doi: 10.1080/10717544.2021.2008055.
The present research was aimed to develop luteolin (LL) loaded pegylated bilosomes (PG-BLs) for oral delivery. The luteolin bilosomes (BLs) were prepared by the thin-film hydration method and further optimized by the Box-Behnken design (four-factors at three-levels). The prepared LL-BLs were evaluated for vesicle size (VS), PDI, zeta potential (ZP), and entrapment efficiency to select the optimized formulation. The optimized formulation was further assessed for surface morphology, drug release, gut permeation, antioxidant, and antimicrobial study. The cytotoxicity study was conducted on breast cancer cell lines (MDA-MB-231 and MCF7). The optimized formulation LL-PG-BLs-opt exhibited a VS of 252.24 ± 3.54 nm, PDI of 0.24, ZP of -32 mV with an encapsulation efficiency of 75.05 ± 0.65%. TEM study revealed spherical shape vesicles without aggregation. The DSC and XRD results revealed that LL was encapsulated into a PG-BLs matrix. LL-PG-BLs-opt exhibited a biphasic release pattern as well as significantly high permeation (<.05) was achieved vis-a-vis LL-BL-opt and LL dispersion. The antioxidant activity result revealed 70.31 ± 3.22%, 83.76 ± 2.56%, and 96.87 ± 2.11% from LL-dispersion, LL-BLs-opt, and LL-PG-BLs-opt, respectively. Furthermore, LL-PG-BLs-opt exhibited high cell viability on both cell lines than LL-BL-opt and pure LL. The IC value was found to be 390 µM and 510 µM against MCF7 and MDA-MB-231 cancer cells, respectively. The antimicrobial activity result exhibited LL-PG-BLs-opt had better antibacterial activity than pure LL against and . Hence, PG-BLs might provide an efficient nano oral delivery for the management of the different diseases.
本研究旨在开发用于口服递送的木犀草素（LL）负载的聚乙二醇化双分子层囊泡（PG-BLs）。木犀草素双分子层囊泡（BLs）通过薄膜水化法制备，并通过 Box-Behnken 设计（四因素三水平）进一步优化。制备的 LL-BLs 进行囊泡大小（VS）、PDI、Zeta 电位（ZP）和包封效率评估，以选择最佳配方。进一步评估最佳配方的表面形态、药物释放、肠道渗透、抗氧化和抗菌研究。细胞毒性研究在乳腺癌细胞系（MDA-MB-231 和 MCF7）上进行。最佳配方 LL-PG-BLs-opt 的 VS 为 252.24 ± 3.54nm、PDI 为 0.24、ZP 为-32mV，包封效率为 75.05 ± 0.65%。TEM 研究表明，囊泡呈球形，无聚集。DSC 和 XRD 结果表明 LL 被包封到 PG-BLs 基质中。LL-PG-BLs-opt 表现出双相释放模式，与 LL-BL-opt 和 LL 分散体相比，渗透显著提高（<.05）。抗氧化活性结果表明，LL 分散体、LL-BLs-opt 和 LL-PG-BLs-opt 的抗氧化活性分别为 70.31 ± 3.22%、83.76 ± 2.56%和 96.87 ± 2.11%。此外，LL-PG-BLs-opt 在两种细胞系上的细胞活力均高于 LL-BL-opt 和纯 LL。IC 值分别为 390µM 和 510µM，对 MCF7 和 MDA-MB-231 癌细胞有效。抗菌活性结果表明，与纯 LL 相比，LL-PG-BLs-opt 对 和 具有更好的抗菌活性。因此，PG-BLs 可能为不同疾病的管理提供有效的纳米口服递送。
