Pharmacy Department, Health Sciences Center, Universidade Federal do Rio Grande do Norte (UFRN), Natal 59012-570, Rio Grande do Norte (RN), Brazil.
Department of Pharmacy, Laboratory of Biological Activity, Federal University of Amazonas, Manaus 69077-000, AM, Brazil.
Molecules. 2017 Sep 9;22(9):1512. doi: 10.3390/molecules22091512.
α,β Amyrin (ABAM) is a natural mixture of pentacyclic triterpenes that has shown a variety of pharmacological properties, including anti-inflammatory effect. ABAM is isolated from Burseraceae oilresins, especially from the species, which is commonly found in the Brazilian Amazon. This work aimed to develop solid dispersions (SD) of ABAM with the following hydrophilic polymers: polyvinylpyrrolidone (PVP-K30), polyethylene glycol (PEG-6000) and hydroxypropylmethylcellulose (HPMC). The SDs were prepared by physical mixture (PM), kneading (KND) and rotary evaporation (RE) methods. In order to verify any interaction between ABAM and the hydrophilic polymers, physicochemical characterization was performed by Fourier transform infrared (FTIR), scanning electron microscopy (SEM), powder X-ray diffraction (XRD), thermogravimetry (TG) and differential scanning calorimetry (DSC) analysis. Furthermore, an in vitro anti-inflammatory assay was performed with ABAM alone and as SDs with the hydrophilic polymers. The results from the characterization analysis show that the SDs were able to induce changes in the physicochemical properties of ABAM, which suggests interaction with the polymer matrix. In vitro anti-inflammatory assay showed that the SDs improved the anti-inflammatory activity of ABAM and showed no cytotoxicity. In conclusion, this study showed the potential use of SDs as an efficient tool for improving the stability and anti-inflammatory activity of ABAM without cytotoxicity.
α、β 桉脂素(ABAM)是一种具有多种药理作用的天然五环三萜混合物,具有抗炎作用。ABAM 从安息香科树脂中分离出来,特别是从巴西亚马逊常见的 物种中分离出来。本工作旨在制备 ABAM 与以下亲水性聚合物的固体分散体(SD):聚乙烯吡咯烷酮(PVP-K30)、聚乙二醇(PEG-6000)和羟丙基甲基纤维素(HPMC)。SD 通过物理混合物(PM)、捏合(KND)和旋转蒸发(RE)方法制备。为了验证 ABAM 与亲水性聚合物之间是否存在任何相互作用,通过傅里叶变换红外(FTIR)、扫描电子显微镜(SEM)、粉末 X 射线衍射(XRD)、热重分析(TG)和差示扫描量热法(DSC)分析进行了物理化学特性表征。此外,还进行了 ABAM 单独以及与亲水性聚合物形成 SD 的体外抗炎测定。表征分析的结果表明,SD 能够诱导 ABAM 物理化学性质的变化,这表明与聚合物基质存在相互作用。体外抗炎测定表明,SD 提高了 ABAM 的抗炎活性,且无细胞毒性。总之,本研究表明 SD 作为一种有效工具,具有提高 ABAM 的稳定性和抗炎活性而无细胞毒性的潜力。