Aldawsari Mohammed F, Alam Aftab, Imran Mohd
Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-kharj 11942, Saudi Arabia.
Department of Pharmacognosy, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
ACS Omega. 2024 Jun 10;9(25):27300-27311. doi: 10.1021/acsomega.4c01718. eCollection 2024 Jun 25.
This study conducts a systematic investigation of the creation and optimization of a rutin-loaded transethosome intended for topical use. The formulation's characteristics were thoroughly assessed for vesicle size (160.45 ± 1.98 nm), polydispersity index (0.235 ± 0.067), and zeta potential (-22.89 mV), with an entrapment efficiency and drug loading of 89.99 ± 1.55% and 8.9 ± 2.11%, respectively, and found to have a spherical shape by the use of transmission electron microscopy. The conversion to a gel suitable for application on the skin was carried out. The drug release form Opt-RUT-TE formulation (73.61 ± 2.55%) was significantly higher than that of release form RUT-suspension (34.52 ± 1.19%). The drug that permeated the skin from Opt-RUT-TEG (935.25 ± 10.49 μg/cm) was significantly higher than the permeability from RUT-Suspension gel (522.57 ± 6.79 μg/cm). Notably, tape stripping analysis revealed that the Opt-RUT-TE gel effectively penetrated the skin layers, with a higher concentration observed in the epidermis-dermis than in the RUT-suspension gel. The transethosomal gel exhibited favorable characteristics, highlighting its capacity to efficiently permeate the skin and suppress the growth of microorganisms, and Opt-RUT-TEG showed a higher microorganism inhibition zone (Gram-positive bacteria) than that of RUT-suspension gel. The investigation highlights the significant therapeutic possibilities of rutin in a transethosomal gel formulation for treating dermatological diseases by improving skin permeability and exhibiting antibacterial effects.
本研究对用于局部给药的芦丁传递体的制备及优化进行了系统研究。对该制剂的特性进行了全面评估,包括囊泡大小(160.45±1.98nm)、多分散指数(0.235±0.067)和zeta电位(-22.89mV),包封率和载药量分别为89.99±1.55%和8.9±2.11%,通过透射电子显微镜观察发现其呈球形。进行了向适合皮肤应用的凝胶的转化。Opt-RUT-TE制剂的药物释放率(73.61±2.55%)显著高于芦丁悬浮液的释放率(34.52±1.19%)。从Opt-RUT-TEG渗透到皮肤中的药物(935.25±10.49μg/cm)显著高于从芦丁悬浮凝胶的渗透率(522.57±6.79μg/cm)。值得注意的是,胶带剥离分析表明,Opt-RUT-TE凝胶有效地穿透了皮肤层,在表皮-真皮中的浓度高于芦丁悬浮凝胶。传递体凝胶表现出良好的特性,突出了其有效渗透皮肤和抑制微生物生长的能力,并且Opt-RUT-TEG显示出比芦丁悬浮凝胶更高的微生物抑制区(革兰氏阳性菌)。该研究突出了芦丁在传递体凝胶制剂中通过提高皮肤渗透性和发挥抗菌作用来治疗皮肤病的显著治疗潜力。