Pharmaceutical Nanotechnology Research Laboratory, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
Pharmaceutical Nanotechnology Research Laboratory, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
Int J Pharm. 2024 Dec 5;666:124741. doi: 10.1016/j.ijpharm.2024.124741. Epub 2024 Sep 25.
Ocular drug delivery presents significant challenges due to various anatomical and physiological barriers. Ultradeformable vesicles have emerged as better vesicular systems for achieving deeper corneal penetration and enhanced ocular bioavailability. This research aims to develop a hybrid vesicular system with improved deformability and compare it to conventional vesicular carriers. The ultradeformable vesicle, termed "transniosomes," is a combination of niosomes, liposomes, and transfersomes, loaded with brinzolamide as model drug. The brinzolamide-loaded transniosomes (BRZ-TN) was formulated and compared with different vesicular systems through in vitro, ex vivo, and in vivo characterizations. The optimized BRZ-TN demonstrated a vesicle size of 112.06 ± 4.13 nm and an entrapment efficiency of 93.63 ± 0.30 %. With a deformability index of 6.405, the BRZ-TN exhibited a permeability of 86.68 ± 2.51 % over 10 h, which is approximately 1.3 times higher than other conventional vesicular systems. Additionally, the BRZ-TN showed a drug flux of 0.247 ± 0.01 mg/cm/h and an apparent permeability of 0.09 ± 1.21 cm/s. Pre-clinical experiments confirmed the superiority of the optimized BRZ-TN, achieving a 37 % reduction in intraocular pressure (IOP), post 6hr of administration, indicating its prolonged therapeutic effect and improved ocular bioavailability. The findings of this study suggest that transniosomes are superior to other carriers and hold great promise as a nanocarrier for ocular drug delivery.
由于各种解剖学和生理学屏障的存在,眼部药物传递存在重大挑战。超变形囊泡作为更好的囊泡系统,已被用于实现更深的角膜穿透和增强眼部生物利用度。本研究旨在开发一种具有改善变形性的混合囊泡系统,并将其与传统囊泡载体进行比较。这种超变形囊泡被称为“转胞囊”,是由 niosomes、liposomes 和 transfersomes 组成的混合物,负载布立佐胺作为模型药物。制备了载布立佐胺的转胞囊(BRZ-TN),并通过体外、离体和体内特性比较了不同的囊泡系统。优化的 BRZ-TN 显示出 112.06±4.13nm 的囊泡大小和 93.63±0.30%的包封效率。BRZ-TN 的变形指数为 6.405,在 10h 内表现出 86.68±2.51%的通透性,约是其他传统囊泡系统的 1.3 倍。此外,BRZ-TN 显示出 0.247±0.01mg/cm/h 的药物通量和 0.09±1.21cm/s 的表观渗透率。临床前实验证实了优化的 BRZ-TN 的优越性,给药 6 小时后眼压(IOP)降低了 37%,表明其具有延长的治疗效果和改善的眼部生物利用度。本研究结果表明,转胞囊优于其他载体,有望成为眼部药物传递的纳米载体。