Scalia Santo, Trotta Valentina, Iannuccelli Valentina, Bianchi Anna
Department of Chemical and Pharmaceutical Sciences, University of Ferrara, 44121 Ferrara, Italy.
Department of Chemical and Pharmaceutical Sciences, University of Ferrara, 44121 Ferrara, Italy.
Colloids Surf B Biointerfaces. 2015 Nov 1;135:42-49. doi: 10.1016/j.colsurfb.2015.07.043. Epub 2015 Jul 22.
In this study, lipid microparticles (LMs) uncoated or coated with chitosan, and containing the antioxidant polyphenol, resveratrol were developed in order to enhance its in vivo skin permeation. The LMs loaded with resveratrol were prepared by melt emulsification and sonication, using tristearin as lipidic material and hydrogenated phosphatidylcholine as the surfactant. Two different methods were examined for the coating of the LMs: chitosan addition during LM preparation or treatment of already formed LMs with a chitosan solution. The latter method achieved a better modulation of the in vitro release of resveratrol and hence was used for subsequent studies. The resveratrol loading and mean diameter of the LMs were 4.1 ± 0.3% (w/w) and 5.7 μm and 3.8 ± 0.2 % (w/w) and 6.1 μm for the uncoated and the chitosan-coated LMs, respectively. Chitosan coating changed the LM surface charge, from a negative zeta potential value (-17.8 ± 4.8 mV) for the uncoated particles, to a higher positive values (+64.2 ± 4.4 mV) for the chitosan-coated ones. Creams containing resveratrol free, encapsulated in the uncoated or chitosan-coated LMs were applied to the forearm of human volunteers and the penetration of the polyphenol in the stratum corneum was investigated in vivo by the tape stripping technique. Uncoated LMs did not produce any significant increase in the fraction of the applied resveratrol dose diffused in the stratum corneum (32.8 ± 8.9 %) compared to the control cream containing the non-encapsulated polyphenol (26.2 ± 5.6 % of the applied dose). On the other hand, application of the cream containing the chitosan-coated LMs produced a significant enhancement in the in vivo permeation of resveratrol to 49.3 ± 5.9% of the applied dose, the effect being more marked in the upper region of the horny layer. The observed improvement in the human stratum corneum penetration of resveratrol achieved by the LMs coated with chitosan should favour the efficiency of its topical application.
在本研究中，为提高抗氧化多酚白藜芦醇的体内皮肤渗透性，制备了未包衣或用壳聚糖包衣且含有白藜芦醇的脂质微粒（LM）。以三硬脂酸甘油酯为脂质材料、氢化磷脂酰胆碱为表面活性剂，通过熔融乳化和超声处理制备负载白藜芦醇的LM。研究了两种不同的LM包衣方法：LM制备过程中添加壳聚糖或用壳聚糖溶液处理已形成的LM。后一种方法能更好地调节白藜芦醇的体外释放，因此用于后续研究。未包衣和壳聚糖包衣LM的白藜芦醇负载量和平均直径分别为4.1±0.3%（w/w）和5.7μm以及3.8±0.2%（w/w）和6.1μm。壳聚糖包衣改变了LM的表面电荷，未包衣颗粒的ζ电位为负值（-17.8±4.8 mV），而壳聚糖包衣颗粒的ζ电位为较高的正值（+64.2±4.4 mV）。将不含白藜芦醇、包裹于未包衣或壳聚糖包衣LM中的乳膏涂抹于人类志愿者的前臂，采用胶带剥离技术在体内研究多酚在角质层中的渗透情况。与含有未包裹多酚的对照乳膏（占涂抹剂量的26.2±5.6%）相比，未包衣LM并未使涂抹的白藜芦醇剂量在角质层中的扩散分数有任何显著增加（32.8±8.9%）。另一方面，涂抹含有壳聚糖包衣LM的乳膏使白藜芦醇的体内渗透率显著提高至涂抹剂量的49.3±5.9%，在角质层上部区域效果更明显。观察到壳聚糖包衣的LM使白藜芦醇在人体角质层中的渗透率提高，这应有利于其局部应用的效果。
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