Imam Syed Sarim, Alshehri Sultan, Altamimi Mohammad A, Almalki Raed Khalid Hassan, Hussain Afzal, Bukhari Sarah I, Mahdi Wael A, Qamar Wajhul
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Polymers (Basel). 2022 Feb 25;14(5):921. doi: 10.3390/polym14050921.
We prepared apigenin (APG)-loaded bilosomes (BLs) and evaluated them for vesicle size, zeta-potential and encapsulation efficiency. The formulations were prepared with cholesterol (CHL), sodium deoxy cholate (SDC), Tween 80 (T80) and phosphatidylcholine (PC) using solvent evaporation method. The prepared formulations showed the optimum result was coated with much mucoadhesive polymer chitosan (CH, 0.25 and 0.5% w/v). The chitosan-coated bilosomes (CH-BLs) were further evaluated for surface morphology, drug−polymer interaction, mucoadhesion, permeation, antimicrobial activity and cell viability. The prepared APG-BLs showed nano-metric size (211 ± 2.87 nm to 433 ± 1.98 nm), polydispersibility index <0.5, negative zeta potential (−15 to −29 mV) and enhanced encapsulation efficiency (69.5 ± 0.93 to 81.9 ± 1.3%). Based on these findings, selected formulation (F2) was further coated with chitosan and showed a marked increase in vesicle size (298 ± 3.56 nm), a positive zeta potential (+17 mV), superior encapsulation efficiency (88.1 ± 1.48%) and improved drug release (69.37 ± 1.34%). Formulation F2C1 showed significantly enhanced permeation and mucoadhesion (p < 0.05) compared to formulation F2 due to the presence of CH as a mucoadhesive polymer. The presence of CH on the surfaces of BLs helps to open the tight membrane junctions and leads to enhanced permeation. A TEM study revealed non-aggregated smooth surface vesicles. The antimicrobial and cell viability assessment revealed better effects in terms of zone of inhibition and cell line assessment against two different cancer cell line. From the study, it can be concluded that APG-CHBLs could be a superior alternative to conventional delivery systems.
我们制备了载有芹菜素（APG）的双分子层脂质体（BLs），并对其囊泡大小、zeta电位和包封率进行了评估。使用溶剂蒸发法，用胆固醇（CHL）、脱氧胆酸钠（SDC）、吐温80（T80）和磷脂酰胆碱（PC）制备了这些制剂。制备的制剂显示最佳结果是用大量的粘膜粘附聚合物壳聚糖（CH，0.25%和0.5% w/v）进行包衣。对壳聚糖包衣的双分子层脂质体（CH-BLs）的表面形态、药物-聚合物相互作用、粘膜粘附性、渗透性、抗菌活性和细胞活力进行了进一步评估。制备的APG-BLs呈现纳米尺寸（211±2.87 nm至433±1.98 nm），多分散指数<0.5，负zeta电位（-15至-29 mV）以及提高的包封率（69.5±0.93%至81.9±1.3%）。基于这些发现，选择的制剂（F2）进一步用壳聚糖包衣，显示囊泡大小显著增加（298±3.56 nm），正zeta电位（+17 mV），优异的包封率（88.1±1.48%）和改善的药物释放（69.37±1.34%）。与制剂F2相比，制剂F2C1由于存在作为粘膜粘附聚合物的CH而显示出显著增强的渗透性和粘膜粘附性（p<0.05）。BLs表面CH的存在有助于打开紧密的膜连接并导致渗透性增强。透射电子显微镜研究揭示了无聚集的光滑表面囊泡。抗菌和细胞活力评估在针对两种不同癌细胞系的抑制圈和细胞系评估方面显示出更好的效果。从该研究可以得出结论，APG-CHBLs可能是传统给药系统的一种优越替代物。
