Alves Marta P, Scarrone Ana L, Santos Marcos, Pohlmann Adriana R, Guterres Sílvia S
Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Av. Ipiranga 2752, CEP 90610-000, Porto Alegre, RS, Brazil.
Int J Pharm. 2007 Aug 16;341(1-2):215-20. doi: 10.1016/j.ijpharm.2007.03.031. Epub 2007 Mar 30.
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 252nm for the nanoemulsion, 277nm for the nanocapsules and 202nm for the nanospheres containing nimesulide. The different nanocarrier systems were incorporated in the hydrophilic gels 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.
这项工作的目的是研究药物模型（尼美舒利）从含有纳米球、纳米胶囊或纳米乳剂的半固体局部用制剂中的体外皮肤渗透情况。采用纳米沉淀法、界面沉积法和自发乳化法制备纳米结构悬浮液。含尼美舒利的纳米乳剂的流体动力学直径为252nm，纳米胶囊为277nm，纳米球为202nm。将不同的纳米载体系统掺入亲水性凝胶中，并使用剥离技术和Franz型扩散池研究它们将药物递送至人皮肤的能力。从含纳米胶囊的凝胶（GNM-NC）和含纳米球的凝胶（GNM-NS）中释放到角质层（SC）中的尼美舒利量相似。另一方面，对于含纳米乳剂的凝胶（GNM-NE），在SC中未检测到尼美舒利，但它已直接渗透到真皮中。与相同浓度的非微粒载尼美舒利制剂相比，含纳米胶囊的凝胶（GNM-NC）对尼美舒利的渗透在更深层皮肤中比含纳米球的凝胶（GNM-NS）或含纳米乳剂的凝胶（GNM-NE）更大。与相同浓度的非微粒载尼美舒利制剂相比，含纳米载体的凝胶（GNM-NC、GNM-NS和GNM-NE）能够在皮肤的活性层中释放药物。
