Preparation and Characterization of Tripterygium wilfordii Multi-Glycoside Nanoparticle Using Supercritical Anti-Solvent Process

Fengli Chen,Tong Li,Kexin Hou,Guoqiang Cui,Lili Li,Yuangang Zu,Lei Yang,Shuangyang Li,Zaizhi Liu

doi:10.3390/ijms15022695

Abstract

The aim of this study was to prepare nanosized Tripterygium wilfordii multi-glycoside (GTW) powders by the supercritical antisolvent precipitation process (SAS), and to evaluate the anti-inflammatory effects. Ethanol was used as solvent and carbon dioxide was used as an antisolvent. The effects of process parameters such as precipitation pressure (15–35 MPa), precipitation temperature (45–65 °C), drug solution flow rates (3–7 mL/min) and drug concentrations (10–30 mg/mL) were investigated. The nanospheres obtained with mean diameters ranged from 77.5 to 131.8 nm. The processed and unprocessed GTW were characterized by scanning electron microscopy, X-ray diffraction, Fourier-transform infrared spectroscopy and thermal gravimetric analysis. The present study was designed to investigate the beneficial effect of the GTW nanoparticles on adjuvant-induced arthritis in albino rats. The processed and unprocessed GTW were tested against Freund’s complete adjuvant-induced arthritis in rats. Blood samples were collected for the estimation of interleukins (IL-1α, IL-1β) and tumor necrosis factor-α (TNF-α). It was concluded that physicochemical properties and anti-inflammatory activity of GTW nanoparticles could be improved by physical modification, such as particle size reduction using supercritical antisolvent (SAS) process. Further, SAS process was a powerful methodology for improving the physicochemical properties and anti-inflammatory activity of GTW.

Highlights

Tripterygium wilfordii is a woody twining vine belonging to the family Celastraceae
There were a total of 29 runs for optimizing the four individual parameters in the current Box–Behnken design (BBD), which was applied to the production of glycoside of T. wilfordii (GTW) nanoparticles
GTW nanoparticles with a minimum MPS of 77.5 nm were successfully prepared from ethanol by a supercritical antisolvent (SAS) process when the temperature was 63.5 °C, pressure was 29.4 MPa, the drug concentration was 10.2 mg/mL, the solution flow rate was 5.4 mL/min and the CO2 flow rate was

Summary

Introduction

It is native to Southern and Eastern China, Korea, and Japan [1] It has been used in traditional Chinese medicine for over 2000 years [2], including treating fever, chills, sores, edema, carbuncle, joint pain, and inflammation [3,4]. The main bioactive components of GTW, such as triptolide, tripdiolide, triptonide, and triptohairic acid, were subjected to standardization. In recent years, it has attracted much interest from scholars from various countries due to its anti-inflammatory [2,6,7], immunosuppressive [7,8], antitumor [9], antiviral effects [10], and its therapeutic impact on rheumatoid arthritis [11] and nephritis [12]. Its long-term and large-dosing administration was restricted by the low solubility of its useful components

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Results

Conclusion