Di Filippo Leonardo Delello, Duarte Jonatas Lobato, Roque-Borda Cesar Augusto, Pavan Fernando Rogério, Meneguin Andreia Bagliotti, Chorilli Marlus, Melero Ana, Guillot Antonio José, Spagnol Caroline Magnani, Correa Marcos Antônio
School of Pharmaceutical Sciences, Sao Paulo State University "Julio de Mesquita Filho", Araraquara 14800903, SP, Brazil.
Pharmaceutical Technology and Parasitology, Department of Pharmacy, University of Valencia, 46010 Valencia, Spain.
Life (Basel). 2022 Jul 14;12(7):1049. doi: 10.3390/life12071049.
Vitamins are widely found in nature, for example, in plants and fruits. Ascorbic acid and nicotinamide are examples of these compounds that have potent antioxidant properties, besides stimulating collagen production and depigmenting properties that protect the skin from premature aging. To overcome the skin barrier and reduce the instability of antioxidant compounds, alternative systems have been developed to facilitate the delivery of antioxidants, making them efficiently available to the tissue for an extended time without causing damage or toxicity. The objective of this study was to obtain chitosan biodegradable microparticles containing ascorbic acid and nicotinamide for topical delivery. The microparticles were obtained by spray drying and characterized chemically by means of scanning electron microscopy, infrared spectroscopy, X-ray diffraction, and differential exploratory calorimetry. The drugs were successfully encapsulated and the microparticles showed positive zeta potential. In vitro release assays showed a sustained release profile. The evaluation of ex vivo skin permeation and retention demonstrated low permeation and adequate retention of the compounds in the epidermis/dermis, suggesting the efficient delivery from the obtained microparticles. Antibacterial assays have shown that microparticles can inhibit the growth of microorganisms in a time- and dose-dependent manner, corroborating their use in cosmetic products for application on the skin.
维生素在自然界中广泛存在，例如在植物和水果中。抗坏血酸和烟酰胺就是这些具有强大抗氧化特性的化合物的例子，此外还具有刺激胶原蛋白生成和美白的特性，可保护皮肤防止过早衰老。为了克服皮肤屏障并降低抗氧化化合物的不稳定性，人们开发了替代系统来促进抗氧化剂的递送，使它们能够在较长时间内有效地为组织所用，而不会造成损伤或毒性。本研究的目的是制备含有抗坏血酸和烟酰胺的壳聚糖可生物降解微粒用于局部给药。通过喷雾干燥获得微粒，并通过扫描电子显微镜、红外光谱、X射线衍射和差示扫描量热法进行化学表征。药物成功包封，微粒显示出正的ζ电位。体外释放试验显示出缓释曲线。离体皮肤渗透和滞留评估表明，化合物在表皮/真皮中的渗透较低且滞留充分，这表明从所得微粒中能有效递送。抗菌试验表明，微粒能以时间和剂量依赖的方式抑制微生物生长，证实了它们在用于皮肤的化妆品中的应用。
