Asasutjarit Rathapon, Sookdee Papawee, Veeranondha Sukitaya, Fuongfuchat Asira, Itharat Arunporn
Thammasat University Research Unit in Drug, Health Product Development and Application (DHP-DA), Department of Pharmaceutical Sciences, Faculty of Pharmacy, Thammasat University, Pathum Thani, 12120, Thailand.
Department of Applied Thai Traditional Medicine, Center of Excellence on Applied Thai Traditional Medicine Research (CEATMR), Faculty of Medicine, Thammasat University, Pathum Thani, 12120, Thailand.
Heliyon. 2020 Jun 9;6(6):e04139. doi: 10.1016/j.heliyon.2020.e04139. eCollection 2020 Jun.
Piperine-rich herbal mixture (PHM) used in this study is a traditional Thai medicine that contains 21 oriental herbs. It is called "Sahastara remedy" and is officially included in the Thai National List of Essential Medicine since A.D. 2011. PHM has been used orally to relieve muscle and bone pains. It contains fruits as a major constituent and also fruits, PHM thus has anti-inflammatory activities that mostly come from the bioactivities of piperine consisting of these pepper fruits. Unfortunately, PHM usually causes gastrointestinal side effects. Consequently, a topical product containing an alcoholic extract of PHM (PHM-E), i.e., film-forming solution (FFS) was developed to overcome this drawback. The aims of this study were to investigate the anti-inflammatory activity of PHM-E, to evaluate physicochemical properties and the anti-inflammatory activity of FFS containing PHM-E (PHM-E FFS). Anti-inflammatory activities of PHM-E were investigated in the RAW 264.7 cells. Physicochemical properties, toxicities and anti-inflammatory activities of PHM-E FFS including its dry film (PHM-E film) were determined. PHM-E showed anti-inflammatory activities with dose dependent manners via inhibition of nitric oxide and prostaglandin E production by the RAW 264.7 cells and promotion of the cell phenotype polarization from M1 to M2. PHM-E FFS had low viscosity and exhibited the Newtonian behavior. It provided elastic PHM-E film with low tensile strength. The release profile of piperine from PHM-E film followed a zero-kinetic model. PHM-E FFS demonstrated compatibility with the skin cells, minimal ocular irritant when accidentally splashing into the eye and moderate-to-high potency for inhibition of inflammatory symptoms in the rats. PHM-E FFS thus had potential for use in the further clinical study to investigate its efficacy and safety in patients.
本研究中使用的富含胡椒碱的草药混合物（PHM）是一种传统泰国药物，包含21种东方草药。它被称为“萨哈斯塔拉疗法”，自公元2011年起正式列入泰国国家基本药物清单。PHM一直用于口服缓解肌肉和骨骼疼痛。它以果实为主要成分，也含有果实，因此PHM具有抗炎活性，主要来自这些胡椒果实中胡椒碱的生物活性。不幸的是，PHM通常会引起胃肠道副作用。因此，开发了一种含有PHM酒精提取物（PHM-E）的外用产品，即成膜溶液（FFS），以克服这一缺点。本研究的目的是研究PHM-E的抗炎活性，评估含PHM-E的FFS（PHM-E FFS）的理化性质和抗炎活性。在RAW 264.7细胞中研究了PHM-E的抗炎活性。测定了PHM-E FFS及其干膜（PHM-E膜）的理化性质、毒性和抗炎活性。PHM-E通过抑制RAW 264.7细胞产生一氧化氮和前列腺素E，并促进细胞表型从M1向M2极化，呈现出剂量依赖性的抗炎活性。PHM-E FFS粘度低，表现出牛顿流体行为。它提供了具有低拉伸强度的弹性PHM-E膜。胡椒碱从PHM-E膜中的释放曲线遵循零动力学模型。PHM-E FFS与皮肤细胞具有相容性，意外溅入眼睛时眼部刺激性最小，对大鼠炎症症状的抑制作用具有中到高效力。因此，PHM-E FFS有潜力用于进一步的临床研究，以调查其在患者中的疗效和安全性。
