School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden, Penang, Malaysia.
Int J Nanomedicine. 2011;6:387-96. doi: 10.2147/IJN.S14667. Epub 2011 Feb 17.
As a topical delivery system, a nanoscaled emulsion is considered a good carrier of several active ingredients that convey several side effects upon oral administration, such as nonsteroidal anti-inflammatory drugs (NSAIDs).
We investigated the in vitro permeation properties and the in vivo pharmacodynamic activities of different nanoscaled emulsions containing ibuprofen, an NSAID, as an active ingredient and newly synthesized palm olein esters (POEs) as the oil phase.
A ratio of 25:37:38 of oil phase:aqueous phase:surfactant was used, and different additives were used for the production of a range of nanoscaled emulsions. Carbopol® 940 dispersion neutralized by triethanolamine was employed as a rheology modifier. In some circumstances, menthol and limonene were employed at different concentrations as permeation promoters. All formulae were assessed in vitro using Franz diffusion cell fitted with full-thickness rat skin. This was followed by in vivo evaluation of the anti-inflammatory and analgesic activities of the promising formulae and comparison of the effects with that of the commercially available gel.
Among all other formulae, formula G40 (Carbopol® 940-free formula) had a superior ability in transferring ibuprofen topically compared with the reference. Carbopol® 940 significantly decreased the amount of drug transferred from formula G41 through the skin as a result of swelling, gel formation, and reduction in drug thermodynamic activity. Nonetheless, the addition of 10% w/w of menthol and limonene successfully overcame this drawback since, relative to the reference, higher amount of ibuprofen was transferred through the skin. By contrast, these results were relatively comparable to that of formula G40. Pharmacodynamically, the G40, G45, and G47 formulae exhibited the highest anti-inflammatory and analgesic effects compared with other formulae.
The ingredients and the physical properties of the nanoscaled emulsions produced by using the newly synthesized POEs succeeded to deliver ibuprofen competently.
作为一种局部递送系统，纳米乳剂被认为是几种活性成分的良好载体，这些成分在口服给药时会带来几种副作用，如非甾体抗炎药（NSAIDs）。
我们研究了含有布洛芬（一种 NSAID）作为活性成分和新合成的棕榈油酯（POEs）作为油相的不同纳米乳剂的体外渗透特性和体内药效学活性。
使用油相：水相：表面活性剂的比例为 25:37:38，并使用不同的添加剂来生产一系列纳米乳剂。使用三乙醇胺中和的 Carbopol® 940 分散体作为流变改性剂。在某些情况下，使用不同浓度的薄荷醇和柠檬烯作为渗透促进剂。所有配方均在配备全厚大鼠皮肤的 Franz 扩散细胞中进行体外评估。随后对有前途的配方进行体内抗炎和镇痛活性评估，并与市售凝胶的效果进行比较。
在所有其他配方中，与参比配方相比，无 Carbopol® 940 的配方 G40 具有更好的将布洛芬经皮传递的能力。Carbopol® 940 的加入会由于肿胀、凝胶形成和药物热力学活性的降低而减少配方 G41 中药物透过皮肤的量。然而，添加 10%w/w 的薄荷醇和柠檬烯成功克服了这一缺点，因为与参比配方相比，更多的布洛芬透过皮肤传递。相比之下，这些结果与配方 G40 相对可比。药效学上，与其他配方相比，配方 G40、G45 和 G47 表现出最高的抗炎和镇痛效果。
使用新合成的 POEs 制备的纳米乳剂的成分和物理性质成功地将布洛芬递送到体内。
