Liangxing Tu

Andrographis paniculata is a plant of the Acanthaceae family and its primary bioactive constituent, andrographolide, exhibits a broad spectrum of pharmacological activities and notable clinical efficacy. However, its poor solubility and limited bioavailability pose significant challenges for therapeutic applications. To overcome these limitations, researchers have synthesized andrographolide sulfonates by reacting andrographolide with ethanol and sulfuric acid. This sulfonated derivative significantly enhances water solubility and bioavailability while retaining key pharmacological properties such as anti-inflammatory and antiviral activities. As a representative formulation, Xiyanping injection has been widely employed in the treatment of respiratory infections, pneumonia, and related conditions, playing a critical role during the COVID-19 pandemic. Despite its widespread application, there has yet to be a comprehensive review of its chemical composition and pharmacological mechanisms. Additionally, the safety of Xiyanping injection remains a topic of some debate. This review systematically examines the chemical composition, pharmacological activities, clinical applications, and adverse reactions of andrographolide sulfonates and their formulation in Xiyanping injection to provide a scientific basis for further research and applications, while also offering valuable insights for the development of similar sulfonated drugs.

Resveratrol (Res), an active ingredient derived from a multitude of plants, exhibits multiple pharmacological activities. However, its poor water solubility and low bioavailability present significant challenges to its clinical application. Our study aimed to improve the transdermal absorption of Res using dissolving microneedle (MN) technology, which could effectively overcome the stratum corneum barrier. Res-loaded dissolving microneedles (Res-MNs) were fabricated using polyvinyl pyrrolidone K90 (PVP K90) as the matrix material, and a two-step casting procedure was employed. The process was optimized using the Box–Behnken experimental design approach. The characteristics of Res-MNs in vitro, including morphology, solubility, safety evaluation, and skin permeation, were studied. The results showed that the optimum preparation conditions of Res-MNs were a centrifugation time of 10 minutes, a solvent concentration of 25%, and a prescription ratio (Res: matrix) of 0.375. The skin permeability of the Res-MNs was enhanced compared with Res suspension and Res gel. The cumulative release of Res-MNs in vitro was 75%, which was approximately 5 and 3 times that of the Res suspension group and Res gel group. These results suggest that dissolving MNs may represent a potential approach for enhancing the transdermal delivery of poorly absorbed drugs such as Res.

Intestinal lymphatic transport offers an alternative and effective way to deliver drugs, such as avoiding first-pass metabolism, enhancing oral bioavailabi