Chang Chenqi, Lu Chang, Zheng Yu, Lin Lili, Chen XiuZhen, Chen Linwei, Chen Zhipeng, Chen Rui
College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
Department of Pharmacy, The Affiliated Taizhou People's Hospital of Nanjing Medical University, Nanjing Medical University, Taizhou, Jiangsu, 225300, China.
J Pharm Anal. 2025 Jul;15(7):101201. doi: 10.1016/j.jpha.2025.101201. Epub 2025 Jan 21.
Respiratory syncytial virus (RSV) is a ubiquitous respiratory virus that affects individuals of all ages; however, there is a notable lack of targeted treatments. RSV infection is associated with a range of respiratory symptoms, including bronchiolitis and pneumonia. Baicalin (BA) exhibits significant therapeutic effects against RSV infection through mechanisms of viral inhibition and anti-inflammatory action. Nonetheless, the clinical application of BA is constrained by its low solubility and bioavailability. In this study, we prepared BA nanodrugs (BA NDs) with enhanced water solubility utilizing the supramolecular self-assembled strategy, and we further conducted a comparative analysis of this pharmacological activity between free drugs and NDs of BA. Both and results demonstrated that BA NDs significantly enhanced the dual effects of viral inhibition and inflammation relief compared to free BA, attributed to prolonged lung retention, improved cellular uptake, and increased targeting affinity. Our study confirms that the nanosizing strategy, a straightforward approach to enhance drug solubility, can also increase biological activity compared to free drugs with the same content, thereby providing a potential ND for RSV treatment. This correlation analysis between the existing forms of drugs and their biological activity offers a novel perspective for research on the active ingredients of traditional Chinese medicine.
呼吸道合胞病毒（RSV）是一种普遍存在的呼吸道病毒，可感染各年龄段的人群；然而，目前明显缺乏针对性的治疗方法。RSV感染与一系列呼吸道症状相关，包括细支气管炎和肺炎。黄芩苷（BA）通过病毒抑制和抗炎作用机制，对RSV感染具有显著的治疗效果。尽管如此，BA的临床应用因其低溶解度和生物利用度而受到限制。在本研究中，我们利用超分子自组装策略制备了具有增强水溶性的BA纳米药物（BA NDs），并进一步对BA的游离药物和纳米药物之间的这种药理活性进行了比较分析。体外和体内结果均表明，与游离BA相比，BA NDs显著增强了病毒抑制和炎症缓解的双重作用，这归因于其在肺部的滞留时间延长、细胞摄取改善以及靶向亲和力增加。我们的研究证实，纳米尺寸策略作为一种提高药物溶解度的简单方法，与相同含量的游离药物相比，还可以提高生物活性，从而为RSV治疗提供了一种潜在的纳米药物。这种药物现有形式与其生物活性之间的相关性分析为中药活性成分的研究提供了新的视角。
