Kirilov P, Rum S, Gilbert E, Roussel L, Salmon D, Abdayem R, Serre C, Villa C, Haftek M, Falson F, Pirot F
Université Claude Bernard Lyon 1, EA4169 "Aspects fondamentaux, cliniques et thérapeutiques de la fonction barrière cutanée", SFR Lyon-Est Santé - INSERM US 7 - CNRS UMS 3453, ISPB, Laboratoire de Pharmacie Galénique Industrielle, plateforme FRIPHARM, 8 Avenue Rockefeller, F-69373 Lyon cedex 08, France.
Int J Cosmet Sci. 2014 Aug;36(4):336-46. doi: 10.1111/ics.12131. Epub 2014 May 16.
The preparation and physicochemical characterization of organogel nanoparticles dispersed in water have been developed. These systems could be employed as nanocarrier for cosmetic applications or as hydrophobic reservoirs for drug delivery.
Gelled particles of organic liquid and 12-hydroxystearic acid (organogelator) were obtained by hot emulsification (T>Tgel), with a surfactant (acetylated glycol stearate) and polymers (sodium hyaluronate and polyvinyl alcohol) as stabilizing agents, and cooling at room temperature (T<Tgel). An organic UVB sunscreen molecule, obtained by microwave activation, was used as a hydrophobic model molecule. The physicochemical properties of the starting organogel (gelation tests; rheological study) and the dispersed gelled particles (rheological study; particle mean size, size distribution, zeta-potential measurements; physical stability evaluation; UVB absorption and water resistance ability) were studied. The synthesis of sunscreen compound using microwave activation was also described.
According to the gelation test results, organogels were obtained with various organic liquids. Vaseline and almond oils were selected as organic medium for the gelled nanoparticle preparation. A preliminary formulation study was carried out in order to determine the optimal experimental conditions to obtain stable nanoparticle dispersions. Gelled nanoparticles contained the sunscreen model molecule, with mean size of 450 nm, polydispersity index of 0.18 and zeta-potential value above -30 mV, were obtained by ultrasound probe homogenization method. A comparative study of their dispersion ageing showed a greatly enhanced stability after gelation. According to the UVB absorption evaluation, gelled particles improved the photoprotective ability and the photostability of immobilized UVB blocker. They showed a high water resistance (~83%) even after 40 min of immersion.
The obtained results demonstrate the interest of these gelled nanoparticles and their aqueous dispersion for the preparation of new formulations for cosmetic and dermo-cosmetic applications.
已开发出分散于水中的有机凝胶纳米颗粒的制备方法及其物理化学特性表征。这些体系可用作化妆品应用的纳米载体或药物递送的疏水储库。
通过热乳化(T>Tgel)获得有机液体与12-羟基硬脂酸(有机凝胶剂)的凝胶化颗粒,使用表面活性剂(乙酰化乙二醇硬脂酸酯)和聚合物(透明质酸钠和聚乙烯醇)作为稳定剂,并在室温下冷却(T<Tgel)。通过微波活化获得的有机中波紫外线防晒分子用作疏水模型分子。研究了起始有机凝胶的物理化学性质(凝胶化测试;流变学研究)以及分散的凝胶化颗粒的物理化学性质(流变学研究;颗粒平均尺寸、尺寸分布、ζ电位测量;物理稳定性评估;中波紫外线吸收和耐水性)。还描述了使用微波活化合成防晒化合物的方法。
根据凝胶化测试结果,用各种有机液体获得了有机凝胶。选择凡士林和杏仁油作为凝胶化纳米颗粒制备的有机介质。进行了初步配方研究,以确定获得稳定纳米颗粒分散体的最佳实验条件。通过超声探头均质化方法获得了含有防晒模型分子的凝胶化纳米颗粒,其平均尺寸为450nm,多分散指数为0.18,ζ电位值高于-30mV。对其分散体老化的比较研究表明,凝胶化后稳定性大大提高。根据中波紫外线吸收评估,凝胶化颗粒提高了固定化中波紫外线阻滞剂的光保护能力和光稳定性。即使浸泡40分钟后,它们仍显示出高耐水性(约83%)。
所得结果证明了这些凝胶化纳米颗粒及其水分散体对于制备化妆品和皮肤化妆品应用新配方的价值。