Aya R Elbasuony, Abdelaziz E Abdelaziz, Eman A Mazyed, Gamal M El Maghraby
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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.
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.