Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand.
Int J Pharm. 2012 Feb 28;423(2):303-11. doi: 10.1016/j.ijpharm.2011.11.032. Epub 2011 Dec 2.
Ellagic acid (EA) is a potent antioxidant phytochemical substance which has limitation to use due to its poor biopharmaceutical properties, low solubility and low permeability. The aim of the present study was to develop niosomal formulations obtained from the mixture of Span 60 and Tween 60 that could encapsulate EA for dermal delivery. The EA-loaded niosomes were prepared with 1:0, 2:1, 1:1, 0:1 Span 60 and Tween 60, using polyethylene glycol 400 (PEG 400), propylene glycol (PG) or methanol (MeOH) as a solubilizer. The influence of formulations on vesicle size, entrapment efficiency and stability of EA-loaded niosomes was investigated. It was found that all ratios of surfactants could produce EA-loaded niosomes when using 15% (v/v) PG, 15% (v/v) PEG 400 or 20% (v/v) MeOH. The niosomes were spherical multilamellar vesicles showing the localization of EA in the vesicles. The vesicle sizes of the niosomes after extrusion were 124-752 nm with PI less than 0.4. The percentages of entrapment efficiency (% E.E.) of all EA-loaded niosomes varied between 1.35% and 26.75% while PEG 400 niosomes gave the highest % E.E. The most stable and highest entrapped formulation was 2:1 Span 60 and Tween 60 niosomes. Additionally, the in vitro skin permeation revealed that penetration of EA from the niosomes depended on vesicle size, the amount of EA entrapped and the added solubilizers which could act as a permeation enhancer. From skin distribution study, the EA-loaded niosomes showed more efficiency in the delivery of EA through human epidermis and dermis than EA solution. The results indicated that the Span 60 and Tween 60 niosomes may be a potential carrier for dermal delivery of EA.
鞣花酸(EA)是一种有效的抗氧化植物化学物质,但由于其生物制药性质差、溶解度低和渗透性低,其使用受到限制。本研究的目的是开发由 Span 60 和 Tween 60 混合物制成的尼奥斯omal 制剂,以将 EA 包封用于皮肤递送。用聚乙二醇 400 (PEG 400)、丙二醇(PG)或甲醇(MeOH)作为助溶剂,用 1:0、2:1、1:1、0:1 的 Span 60 和 Tween 60 制备 EA 负载的尼奥斯omal。研究了制剂对 EA 负载的尼奥斯omal 囊泡大小、包封效率和稳定性的影响。结果发现,当使用 15%(v/v)PG、15%(v/v)PEG 400 或 20%(v/v)MeOH 时,所有比例的表面活性剂都可以产生 EA 负载的尼奥斯omal。尼奥斯omal 呈球形多层囊泡状,表明 EA 定位于囊泡中。挤出后尼奥斯omal 的囊泡大小为 124-752nm,PI 小于 0.4。所有 EA 负载的尼奥斯omal 的包封效率(%E.E.)百分比在 1.35%至 26.75%之间,而 PEG 400 尼奥斯omal 的包封效率最高。最稳定和包封效率最高的制剂是 2:1 Span 60 和 Tween 60 尼奥斯omal。此外,体外皮肤渗透研究表明,EA 从尼奥斯omal 中的渗透取决于囊泡大小、包封的 EA 量和添加的助溶剂,助溶剂可以作为渗透增强剂。从皮肤分布研究中可以看出,与 EA 溶液相比,EA 负载的尼奥斯omal 更有效地将 EA 递送至人表皮和真皮。结果表明,Span 60 和 Tween 60 尼奥斯omal 可能是 EA 经皮递送的潜在载体。