Niosomes for enhanced oral delivery of pioglitazone: in vitro characterization and in vivo evaluation.

IF 2.8 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Aya R Elbasuony, Abdelaziz E Abdelaziz, Eman A Mazyed, Gamal M El Maghraby
{"title":"Niosomes for enhanced oral delivery of pioglitazone: in vitro characterization and in vivo evaluation.","authors":"Aya R Elbasuony, Abdelaziz E Abdelaziz, Eman A Mazyed, Gamal M El Maghraby","doi":"10.1093/jpp/rgaf015","DOIUrl":null,"url":null,"abstract":"<p><strong>Objectives: </strong>The aim was to investigate oleic acid and nigella oil modified niosomes as novel carriers for enhanced pioglitazone (PGZ) oral delivery.</p><p><strong>Methods: </strong>PGZ was encapsulated into niosomes of cholesterol, tween 80, and span 60 before (F1) and after incorporation of nigella oil (F2) or oleic acid (F3) as membrane fluidizers. Niosomes were characterized for morphology, size, zeta potential, PGZ entrapment, and release. Hypoglycemic effect was also assessed.</p><p><strong>Key findings: </strong>Vesicles were spherical recording size values of 286.4, 111.3, and 137.5 nm for F1, F2, and F3 niosomes, respectively. The zeta potential predicted good stability of niosomes. The lipophilic nature of PGZ resulted in more than 99% entrapment into niosomes. PGZ niosomes significantly boosted rate and extent of hypoglycemic activity compared with the unprocessed PGZ. This is clear from the Tmax, which was 3.6, 1.5, 0.87, and 0.62 h for control, F1, F2, and F3, respectively. This was associated with increase in the area above hypoglycemia curve, which was 655.8, 1613.6, 1617.2, and 1764.9 mg h/dl for the same formulations, respectively.</p><p><strong>Conclusion: </strong>Vesicular structure is responsible for enhanced oral bioavailability and drug release is not the limiting factor. Fluidizing material showed potential contribution in enhanced efficacy but requires future verification.</p>","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":" ","pages":""},"PeriodicalIF":2.8000,"publicationDate":"2025-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Pharmacy and Pharmacology","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1093/jpp/rgaf015","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0

Abstract

Objectives: The aim was to investigate oleic acid and nigella oil modified niosomes as novel carriers for enhanced pioglitazone (PGZ) oral delivery.

Methods: PGZ was encapsulated into niosomes of cholesterol, tween 80, and span 60 before (F1) and after incorporation of nigella oil (F2) or oleic acid (F3) as membrane fluidizers. Niosomes were characterized for morphology, size, zeta potential, PGZ entrapment, and release. Hypoglycemic effect was also assessed.

Key findings: Vesicles were spherical recording size values of 286.4, 111.3, and 137.5 nm for F1, F2, and F3 niosomes, respectively. The zeta potential predicted good stability of niosomes. The lipophilic nature of PGZ resulted in more than 99% entrapment into niosomes. PGZ niosomes significantly boosted rate and extent of hypoglycemic activity compared with the unprocessed PGZ. This is clear from the Tmax, which was 3.6, 1.5, 0.87, and 0.62 h for control, F1, F2, and F3, respectively. This was associated with increase in the area above hypoglycemia curve, which was 655.8, 1613.6, 1617.2, and 1764.9 mg h/dl for the same formulations, respectively.

Conclusion: Vesicular structure is responsible for enhanced oral bioavailability and drug release is not the limiting factor. Fluidizing material showed potential contribution in enhanced efficacy but requires future verification.

增强吡格列酮口服给药的Niosomes:体外表征和体内评价。
目的:探讨油酸和黑油修饰的纳米体作为增强吡格列酮口服给药的新载体。方法:以黑油(F2)或油酸(F3)作为膜流化剂,分别将PGZ包埋于胆固醇、tween 80和span 60的膜小体中(F1)。研究了Niosomes的形态、大小、zeta电位、PGZ包裹和释放。还评估了降糖效果。主要发现:F1、F2和F3小体的囊泡为球形,记录大小分别为286.4、111.3和137.5 nm。zeta电位预示着纳米体具有良好的稳定性。PGZ的亲脂性导致其在小体中的包裹率超过99%。与未加工的PGZ相比,PGZ小体显著提高了降糖活性的速度和程度。从Tmax中可以清楚地看出这一点,对照组、F1、F2和F3的Tmax分别为3.6、1.5、0.87和0.62小时。这与低血糖曲线上方面积的增加有关,相同配方的低血糖曲线上方面积分别为655.8、1613.6、1617.2和1764.9 mg h/dl。结论:囊泡结构是提高口服生物利用度的主要原因,药物释放不是限制因素。流化材料对提高效能有潜在贡献,但需要进一步验证。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
CiteScore
6.60
自引率
0.00%
发文量
91
审稿时长
3 months
期刊介绍: JPP keeps pace with new research on how drug action may be optimized by new technologies, and attention is given to understanding and improving drug interactions in the body. At the same time, the journal maintains its established and well-respected core strengths in areas such as pharmaceutics and drug delivery, experimental and clinical pharmacology, biopharmaceutics and drug disposition, and drugs from natural sources. JPP publishes at least one special issue on a topical theme each year.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信