超声对优化盐酸匹洛卡品负载niosomes眼部给药稳定性的评价。

IF 4.4 3区 医学 Q2 ENGINEERING, BIOMEDICAL
Progress in Biomaterials Pub Date : 2021-09-01 Epub Date: 2021-09-22 DOI:10.1007/s40204-021-00164-5
Kruga Owodeha-Ashaka, Margaret O Ilomuanya, Affiong Iyire
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引用次数: 29

摘要

Niosomes被越来越多地用于增强药物在眼组织中的渗透和滞留,用于眼后和眼前给药。它们已被用于包封亲水和疏水药物,但它们的使用仍然受到稳定性和包封效率差的挑战,特别是在亲水药物中。因此,重点是了解影响其稳定性的参数,并对其进行优化以改善结果。盐酸匹洛卡平(HCl)是一种亲水药物,用于青光眼眼压的治疗。我们的目的是优化匹罗卡品盐酸粒质体,并评估超声对其稳定性指标的影响,如粒径、多分散性指数(PDI)、zeta电位和包封效率。采用乙醚注射法制备匹罗卡品乳质体。不同的成分浓度和这些变化对niosomal特性的影响进行了评估。通过对优化的载药配方进行30 min和60 min的超声处理,确定了Tween 60比Span 60更适合包封亲水性药物,包封效率(EE)最高,多分散性和粒径指标更好。最佳超声时间为30 min,可使EE从24.5%增加到42%,zeta电位从(-)14.39±8.55 mV增加到(-)18.92±7.53 mV。除了选择合适的表面活性剂和不同的产品组成浓度外,优化超声参数可用于微调niosomal属性,以达到延长眼睛保持和维持长期稳定性的最理想状态。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Evaluation of sonication on stability-indicating properties of optimized pilocarpine hydrochloride-loaded niosomes in ocular drug delivery.

Evaluation of sonication on stability-indicating properties of optimized pilocarpine hydrochloride-loaded niosomes in ocular drug delivery.

Evaluation of sonication on stability-indicating properties of optimized pilocarpine hydrochloride-loaded niosomes in ocular drug delivery.

Niosomes are increasingly explored for enhancing drug penetration and retention in ocular tissues for both posterior and anterior eye delivery. They have been employed in encapsulating both hydrophilic and hydrophobic drugs, but their use is still plagued with challenges of stability and poor entrapment efficiency particularly with hydrophilic drugs. As a result, focus is on understanding the parameters that affect their stability and their optimization for improved results. Pilocarpine hydrochloride (HCl), a hydrophilic drug is used in the management of intraocular pressure in glaucoma. We aimed at optimizing pilocarpine HCl niosomes and evaluating the effect of sonication on its stability-indicating properties such as particle size, polydispersity index (PDI), zeta potential and entrapment efficiency. Pilocarpine niosomes were prepared by ether injection method. Composition concentrations were varied and the effects of these variations on niosomal properties were evaluated. The effects of sonication on niosomes were determined by sonicating optimized drug-loaded formulations for 30 min and 60 min. Tween 60 was confirmed to be more suitable over Span 60 for encapsulating hydrophilic drugs, resulting in the highest entrapment efficiency (EE) and better polydispersity and particle size indices. Optimum sonication duration as a process variable was determined to be 30 min which increased EE from 24.5% to 42% and zeta potential from (-)14.39 ± 8.55 mV to (-)18.92 ± 7.53 mV. In addition to selecting the appropriate surfactants and varying product composition concentrations, optimizing sonication parameters can be used to fine-tune niosomal properties to those most desirable for extended eye retainment and maintenance of long term stability.

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来源期刊
Progress in Biomaterials
Progress in Biomaterials MATERIALS SCIENCE, BIOMATERIALS-
CiteScore
9.60
自引率
4.10%
发文量
35
期刊介绍: Progress in Biomaterials is a multidisciplinary, English-language publication of original contributions and reviews concerning studies of the preparation, performance and evaluation of biomaterials; the chemical, physical, biological and mechanical behavior of materials both in vitro and in vivo in areas such as tissue engineering and regenerative medicine, drug delivery and implants where biomaterials play a significant role. Including all areas of: design; preparation; performance and evaluation of nano- and biomaterials in tissue engineering; drug delivery systems; regenerative medicine; implantable medical devices; interaction of cells/stem cells on biomaterials and related applications.
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