Abstract
Celastrol (also called tripterine) is a quinone methide triterpene isolated from the root extract of Tripterygium wilfordii (thunder god vine in traditional Chinese medicine). Over the past two decades, celastrol has gained wide attention as a potent anti-inflammatory, anti-autoimmune, anti-cancer, anti-oxidant, and neuroprotective agent. However, its clinical translation is very challenging due to its lower aqueous solubility, poor oral bioavailability, and high organ toxicity. To deal with these issues, various formulation strategies have been investigated to augment the overall celastrol efficacy in vivo by attempting to increase the bioavailability and/or reduce the toxicity. Among these, nanotechnology-based celastrol formulations are most widely explored by pharmaceutical scientists worldwide. Based on the survey of literature over the past 15 years, this mini-review is aimed at summarizing a multitude of celastrol nanoformulations that have been developed and tested for various therapeutic applications. In addition, the review highlights the unmet need in the clinical translation of celastrol nanoformulations and the path forward.
Highlights
Clinical translation of bioactive compounds extracted from medicinal plants has gained substantial interest over the past several years due to their superior pharmacological activities especially as antiinflammatory, anti-tumor, and neuroprotective agents
Celastrol nanoformulations have shown significant benefits in several therapeutic applications against prostate cancer, breast and pancreatic cancers, nonsmall-cell lung cancer, ovarian cancer, and human colon cancer and other applications in treating rheumatoid arthritis, polycystic kidney disease, inflammation, and Parkinson’s disease (Abbas et al, 2007; Salminen et al, 2010; Yadav et al, 2010; Mou et al, 2011; Kim et al, 2013; Chang et al, 2018; Qi et al, 2018; Zha et al, 2018; Lin et al, 2019; Song et al, 2019; Wang et al, 2019; Yan et al, 2020). This review summarizes such state-of-the-art therapeutic applications of celastrol nanoformulations in the subsequent sections
Medicinal plants containing bioactive constituents are a great resource for modern drug development, and Tripterygium wilfordii is one of them
Summary
Clinical translation of bioactive compounds extracted from medicinal plants has gained substantial interest over the past several years due to their superior pharmacological activities especially as antiinflammatory, anti-tumor, and neuroprotective agents. One such widely investigated medicinal plant is Tripterygium wilfordii, a perennial vine of the Celastraceae family, commonly known as “thunder god vine” or “lei gong teng.”. Albeit potent, its clinical translation is impeded due to two main disadvantages that are poor water solubility of 0.044 mg/ml at 25°C (BCS class IV drug) (Yang et al, 2019), which limits its bioavailability, and high systemic toxicity resulting from its narrow therapeutic index (Zhang et al, 2014; Shi et al, 2020)
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