应用Box-Behnken设计优化曲伏前列素眼内递送系统。

IF 4.3 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Journal of Liposome Research Pub Date : 2022-12-01 Epub Date: 2022-01-17 DOI:10.1080/08982104.2022.2025828
Marwa H Shukr, Soha Ismail, Ghada G El-Hossary, Amany H El-Shazly
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引用次数: 5

摘要

目前,曲伏前列素是一种用于治疗青光眼的合成前列腺素F2α类似物,通过滴眼液给药。由于其生物利用度极低,且患者依从性不佳,本研究的目的是提高其生物利用度,延长其释放时间,采用Box-Behnken设计对其进行设计和优化。采用溶剂浇铸法制备了具有最小粒径(PS)、最大聚分散指数(PDI)和最大ζ电位(ZP)、包封效率(EE)和粘接强度的纳米微泡凝胶。体内研究表明,与市面上销售的滴眼液(travoswix®)相比,曲伏前列素塑料纳米囊泡凝胶和眼植入物的生物利用度更高,这一点得到了证明,除了对眼表面无刺激性外,它们还具有更高的Cmax和AUC0-∞。然而,与纳米微泡凝胶相比,纳米微泡眼内植入物的效果更持久。本研究提示曲伏前列素塑料纳米囊泡眼植入物是一种治疗青光眼的新型眼部给药系统。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Spanlastics nanovesicular ocular insert as a novel ocular delivery of travoprost: optimization using Box-Behnken design and in vivo evaluation.

Currently, travoprost is a synthetic prostaglandin F2α analogue used in the treatment of glaucoma, it is delivered by eye drop solution. Due to its very low bioavailability and patient non-compliance, the objective of the current study was to enhance its bioavailability, and prolong its release Spanlastic nano-vesicles gels were designed and optimized using Box-Behnken design. The optimized spanlastic nano-vesicles gel exhibited the lowest particle size (PS), polydispersity index (PDI) and the highest zeta potential (ZP), encapsulation efficiency (EE) and mucoadhesive strength was fabricated into spanlastic nano-vesicles ocular insert by solvent casting. In vivo studies showed enhanced bioavailability of travoprost spanlastic nano-vesicles gel and ocular insert compared to the marketed eye drops (travoswix®), as proven by their higher Cmax and AUC0-∞, in addition to being nonirritant to ocular surfaces. However, spanlastic nano-vesicles ocular insert showed more prolonged effect than spanlastic nano-vesicles gel. According to our study, it can be suggested that travoprost spanlastic nano-vesicles ocular insert is a novel ocular delivery system for glaucoma treatment.

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来源期刊
Journal of Liposome Research
Journal of Liposome Research 生物-生化与分子生物学
CiteScore
10.50
自引率
2.30%
发文量
24
审稿时长
3 months
期刊介绍: The Journal of Liposome Research aims to publish original, high-quality, peer-reviewed research on the topic of liposomes and related systems, lipid-based delivery systems, lipid biology, and both synthetic and physical lipid chemistry. Reviews and commentaries or editorials are generally solicited and are editorially reviewed. The Journal also publishes abstracts and conference proceedings including those from the International Liposome Society. The scope of the Journal includes: Formulation and characterisation of systems Formulation engineering of systems Synthetic and physical lipid chemistry Lipid Biology Biomembranes Vaccines Emerging technologies and systems related to liposomes and vesicle type systems Developmental methodologies and new analytical techniques pertaining to the general area Pharmacokinetics, pharmacodynamics and biodistribution of systems Clinical applications. The Journal also publishes Special Issues focusing on particular topics and themes within the general scope of the Journal.
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