da Rocha Priscila Bianca Rodrigues, Souza Bruno Dos Santos, Andrade Lígia Marquez, Marreto Ricardo Neves, Lima Eliana Martins, Taveira Stephânia Fleury
Laboratory of Nanosystems and Drug Delivery Devices (NanoSYS), School of Pharmacy, Universidade Federal de Goiás, Brazil.
Pharmaceutical Technology Laboratory, School of Pharmacy, Universidade Federal de Goiás, Brazil.
Planta Med. 2017 Dec;83(18):1431-1437. doi: 10.1055/s-0043-113325. Epub 2017 Jun 26.
The topical application of extract has been commonly used for many different purposes but especially for cosmetic use in the treatment of gynoid lipodystrophy. Asiaticoside, the most active component in this extract, is responsible for its therapeutic activities. However, little is known to date about asiaticoside skin penetration. Thus, an analytical method for asiaticoside quantification in different skin layers after the topical application of extract was developed and skin permeation studies were performed with the plant extract to apply the analytical method developed. An extraction procedure to recover asiaticoside from the biological matrix was also developed. Asiaticoside was assayed by HPLC/UV (high-performance liquid chromatography-ultraviolet detection) using a gradient of ACN (acetonitrile) and 0.2% phosphoric acid (flow rate of 1.0 mL/min). The analytical procedure was validated according to U. S. Food and Drug Administration guidelines. Selectivity was shown, as endogenous skin components did not interfere with the asiaticoside peak. Analytical curve was linear (3 to 60 µg/mL) and the lower limit of quantification was determined (3 µg/mL). Asiaticoside recoveries from skin samples were 95.1% and 66.7% for the stratum corneum and remaining skin, respectively. After 48 h of permeation studies, a substantial amount of asiaticoside was quantified in the skin layers. The presence of asiaticoside was also detected in the receptor solution of Franz diffusion cells after 48 h (5.81 ± 1.00 µg/mL). The method was reliable and reproducible for asiaticoside quantification in skin samples, thereby making it possible to determine the cutaneous penetration profile of this drug in permeation studies.
该提取物的局部应用已被广泛用于多种不同目的，尤其是用于治疗女性型脂肪营养不良的美容用途。积雪草苷是该提取物中最具活性的成分，负责其治疗活性。然而，迄今为止，关于积雪草苷的皮肤渗透情况知之甚少。因此，开发了一种用于在局部应用该提取物后对不同皮肤层中的积雪草苷进行定量的分析方法，并使用该植物提取物进行了皮肤渗透研究，以应用所开发的分析方法。还开发了一种从生物基质中回收积雪草苷的提取程序。使用乙腈（ACN）和0.2%磷酸的梯度（流速为1.0 mL/min），通过高效液相色谱-紫外检测（HPLC/UV）对积雪草苷进行测定。根据美国食品药品监督管理局的指南对分析程序进行了验证。结果显示具有选择性，因为内源性皮肤成分不会干扰积雪草苷峰。分析曲线呈线性（3至60 μg/mL），并确定了定量下限（3 μg/mL）。角质层和其余皮肤的皮肤样品中积雪草苷的回收率分别为95.1%和66.7%。在进行48小时的渗透研究后，在皮肤层中定量了大量的积雪草苷。48小时后，在Franz扩散池的受体溶液中也检测到了积雪草苷的存在（5.81±1.00 μg/mL）。该方法对于皮肤样品中积雪草苷的定量是可靠且可重复的，从而使得在渗透研究中确定该药物的皮肤渗透概况成为可能。
