A one-platform comparison study of brinzolamide-loaded liposomes, niosomes, transfersomes, and transniosomes for better management of glaucoma

IF 5.3 2区 医学 Q1 PHARMACOLOGY & PHARMACY International Journal of Pharmaceutics Pub Date : 2024-09-25 DOI:10.1016/j.ijpharm.2024.124741
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Abstract

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/cm2/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.

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为更好地治疗青光眼而对布林佐胺脂质体、niosomes、transferomes 和 transniosomes 进行的单平台比较研究。
由于各种解剖和生理障碍,眼部给药面临着巨大挑战。超可变形囊泡已成为更好的囊泡系统,可实现更深的角膜渗透并提高眼部生物利用度。本研究旨在开发一种具有更好变形能力的混合囊泡系统,并将其与传统囊泡载体进行比较。这种被称为 "transniosomes "的超变形囊泡是niosomes、脂质体和转移体的结合体,以布林佐胺为模型药物。通过体外、体内和体外特性分析,配制出了布林佐胺负载型转囊体(BRZ-TN),并将其与不同的囊泡系统进行了比较。优化后的 BRZ-TN 囊泡大小为 112.06 ± 4.13 nm,包埋效率为 93.63 ± 0.30 %。BRZ-TN 的变形指数为 6.405,10 小时内的渗透率为 86.68 ± 2.51%,是其他传统囊泡系统的约 1.3 倍。此外,BRZ-TN 的药物通量为 0.247 ± 0.01 mg/cm2/h,表观渗透率为 0.09 ± 1.21 cm/s。临床前实验证实了优化后的 BRZ-TN 的优越性,给药 6 小时后,眼内压(IOP)降低了 37%,这表明它具有延长疗效和改善眼部生物利用度的作用。这项研究结果表明,反式纳米体优于其他载体,有望成为眼部给药的纳米载体。
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来源期刊
CiteScore
10.70
自引率
8.60%
发文量
951
审稿时长
72 days
期刊介绍: The International Journal of Pharmaceutics is the third most cited journal in the "Pharmacy & Pharmacology" category out of 366 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.
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