Human skin penetration and distribution of nimesulide from hydrophilic gels containing nanocarriers
Human skin penetration and distribution of nimesulide from hydrophilic gels containing nanocarriers
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DOI：
10.1016/j.ijpharm.2007.03.031
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发表时间：
2007-08-16
影响因子：
5.8
通讯作者：
Guterres, Silvia S.
中科院分区：
文献类型：
--
作者：
Alves, Marta P.;Scarrone, Ana L.;Guterres, Silvia S.
这项工作的目的是研究在体外皮肤渗透的药物模型（尼美舒利）从半固体局部制剂含有纳米球，纳米胶囊或纳米乳液。采用纳米沉淀法、界面沉积法和自发乳化法制备了纳米结构悬浮液。纳米乳的流体动力学直径为252 nm，纳米胶囊为277 nm，含有尼美舒利的纳米球为202 nm。将不同的纳米载体系统引入亲水性凝胶中，并使用剥离技术和Franz型扩散池研究其将药物递送到人体皮肤中的能力。从含有纳米胶囊的凝胶（GNM-NC）和含有纳米球的凝胶（GNM-NS）释放到角质层（SC）中的尼美舒利的量是相似的。另一方面，对于含凝胶的纳米乳剂（GNM-NE），尼美舒利在SC中未定量，但其已直接渗透至真皮。使用含纳米胶囊的凝胶（GNM-NC）的尼美舒利在皮肤深层的渗透大于使用含纳米球的凝胶（GNM-NS）或含纳米乳剂的凝胶（GNM-NE）。含有纳米载体的凝胶（GNM-NC、GNM-NS和GNM-NE）能够在皮肤的活性层中释放药物，与相同浓度的非颗粒化尼美舒利负载制剂相比。(c)2007 Elsevier B. V.保留所有权利。
The objective of this work was to study the in vitro skin penetration of a drug model (nimesulide) from semi-solid topical formulations containing nanospheres, nanocapsules or nanoemulsion. Nanoprecipitation, interfacial deposition and spontaneous emulsification methods were used to prepare the nanostructured suspension. The hydrodynamic diameters were 252 nm for the nanoemulsion, 277 nm for the nanocapsules and 202 nm for the nanospheres containing nimesulide. The different nanocarrier systems were incorporated in the hydrophilic gets and their ability of delivering the drug into the human skin were investigated using stripping technique and Franz-type diffusion cells. The amount of nimesulide released into the stratum corneum (SC) from the gel containing nanocapsules (GNM-NC) and the gel containing nanospheres (GNM-NS) was similar. On the other hand, for the gel containing nanoemulsion (GNM-NE), the nimesulide was not quantified in SC, but it has been directly permeated for the dermis. The penetration of the nimesulide using the gel containing nanocapsules (GNM-NC) was larger in the deeper skin than using the gel containing nanospheres (GNM-NS) or the one containing nanoemulsion (GNM-NE). The gels containing nanocarriers (GNM-NC, GNM-NS and GNM-NE) were able to release the drug in the viable layer of the skin, comparing to a non-particulated nimesulide-loaded formulation at the same concentration. (c) 2007 Elsevier B.V. All rights reserved.