Wong Chee Ning, Lee Siew-Keah, Lim Yang Mooi, Yang Shi-Bing, Chew Yik-Ling, Chua Ang-Lim, Liew Kai Bin
M. Kandiah Faculty of Medicine and Health Sciences, Universiti Tunku Abdul Rahman, Kajang 43000, Malaysia.
Institute of Biomedical Sciences, Academia Sinica, Taipei 115201, Taiwan.
Pharmaceutics. 2025 Apr 7;17(4):485. doi: 10.3390/pharmaceutics17040485.
D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), an amphiphilic derivative of natural vitamin E, functions as both a drug efflux inhibitor and a protector against enzymatic degradation and has been widely incorporated into nano-formulations for drug design and delivery. This systematic review evaluates TPGS-based organic nanocarriers, emphasizing their potential to enhance bioavailability of active compounds which include drugs and phytochemicals, improve pharmacokinetic profiles, and optimize therapeutic outcomes, eventually overcoming the limitations of conventional oral active compounds delivery. Data collection was carried out by entering key terms (TPGS) AND (Micelle OR Liposome OR Nanoparticle OR Nanotube OR Dendrimer OR Niosome OR Nanosuspension OR Nanomicelle OR Nanocrystal OR Nanosphere OR Nanocapsule) AND (Oral Bioavailability) into the Scopus database. Full-text articles published in English and relevant to TPGS, which featured organic materials, utilized an oral administration route, and included pharmacokinetic study, were included to the final review. Data selection was conducted by two review authors and subsequently approved by all other authors through a consensus process. The outcomes of the included studies were reviewed and categorized based on the types of nanocarriers. An initial search of the database yielded 173 records. After screening by title and abstract, 52 full-text articles were analyzed. A total of 21 papers were excluded while 31 papers were used in this review. This review concludes that TPGS-based organic nanocarriers are able to enhance the bioavailability of various active compounds, including several phytochemicals, leveraging TPGS's amphiphilic nature, inhibition of efflux transporters, protection against degradation, and stabilization properties. Despite using the same excipient, variability in particle size, zeta potential, and encapsulation efficiency among nanocarriers indicates the need for tailored formulations. A comprehensive approach involving the development and standardized comparison of diverse TPGS-incorporated active compound formulations is essential to identify the optimal TPGS-based nanocarrier for improving a particular active compound's bioavailability.
聚乙二醇1000维生素E琥珀酸酯(TPGS)是天然维生素E的两亲性衍生物,兼具药物外排抑制剂和抗酶解保护剂的功能,已广泛应用于药物设计和递送的纳米制剂中。本系统评价评估了基于TPGS的有机纳米载体,强调其提高包括药物和植物化学物质在内的活性化合物生物利用度、改善药代动力学特征以及优化治疗效果的潜力,最终克服传统口服活性化合物递送的局限性。通过在Scopus数据库中输入关键词(TPGS)AND(胶束或脂质体或纳米颗粒或纳米管或树枝状大分子或非离子表面活性剂泡囊或纳米混悬液或纳米胶束或纳米晶体或纳米球或纳米胶囊)AND(口服生物利用度)来进行数据收集。最终纳入综述的是发表于英文且与TPGS相关的全文文章,这些文章以有机材料为特色,采用口服给药途径,并包括药代动力学研究。数据筛选由两位综述作者进行,随后经所有其他作者通过共识过程批准。纳入研究的结果根据纳米载体类型进行审查和分类。对数据库的初步检索产生了173条记录。经标题和摘要筛选后,分析了52篇全文文章。总共排除了21篇论文,本综述使用了31篇论文。本综述得出结论,基于TPGS的有机纳米载体能够利用TPGS的两亲性、对外排转运体的抑制作用、抗降解保护作用和稳定性能,提高包括多种植物化学物质在内的各种活性化合物的生物利用度。尽管使用了相同的辅料,但纳米载体之间在粒径、zeta电位和包封效率方面的差异表明需要定制制剂。一种涉及开发和标准化比较多种含TPGS活性化合物制剂的综合方法对于确定用于提高特定活性化合物生物利用度的最佳基于TPGS的纳米载体至关重要。