Department of Pharmacy, Federal University of Rio Grande do Norte, Avenue General Cordeiro de Faria, s/n, Petrópolis, Natal, Rio Grande do Norte, ZIP Code 59012-570, Brazil.
Department of Physiology, Federal University of Sergipe, Avenue Marechal Rondon, s/n, Jardim Rosa Elze, São Cristóvão, Sergipe, ZIP Code 49100-000, Brazil.
Biomed Pharmacother. 2018 Jan;97:870-879. doi: 10.1016/j.biopha.2017.10.161. Epub 2017 Nov 7.
Hecogenin acetate (HA) is an acetylated sapogenin that has shown potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors. However, HA exhibits poor aqueous solubility, which may limit its application. This study aims to develop amorphous solid dispersions (ASD) using five hydrophilic polymers, to characterize them and to evaluate their antihyperalgesic activity. Physicochemical characterization was performed by X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM) and Fourier Transformed Infrared (FTIR) spectroscopy. In order to evaluate the hyperalgesia of the ASD, sciatic nerve crush injury (NCI) was induced in mice followed by administration of the ASD, where three parameters were evaluated: mechanical and thermal hyperalgesia as well as grip strength. XRD and SEM showed that ASD of HA with HPMC obtained by kneading (KND) presented an amorphous profile, unlike the others polymers, indicating interaction between HA and HPMC. FTIR analysis evidenced the strong interaction between HA and HPMC. Although the results of mechanical hyperalgesia were slightly improved on the groups treated with ASD of HA with HPMC, the thermal hyperalgesia showed that the incorporation of HA into HPMC matrix significantly improved its antinociceptive activity.
醋酸表雄酮（HA）是一种乙酰化的甾体皂苷元，具有潜在的抗痛觉过敏活性，抑制下行性疼痛并作用于阿片受体。然而，HA 的水溶性较差，这可能限制了它的应用。本研究旨在使用五种亲水性聚合物开发无定形固体分散体（ASD），对其进行表征，并评估其抗痛觉过敏活性。通过 X 射线衍射（XRD）、扫描电子显微镜（SEM）和傅里叶变换红外（FTIR）光谱对其进行理化性质表征。为了评估 ASD 的痛觉过敏，在小鼠坐骨神经挤压损伤（NCI）后给予 ASD，并评估了三个参数：机械性和热痛觉过敏以及握力。XRD 和 SEM 结果表明，与其他聚合物不同，通过 kneading（KND）法制备的 HA 与 HPMC 的 ASD 呈现无定形形态，表明 HA 与 HPMC 之间存在相互作用。FTIR 分析表明 HA 与 HPMC 之间存在强相互作用。尽管用 HPMC 载体制备的 HA 的 ASD 治疗组的机械性痛觉过敏结果略有改善，但热痛觉过敏表明 HA 掺入 HPMC 基质显著提高了其镇痛活性。
