Nanotechnology-Based Celastrol Formulations and Their Therapeutic Applications.

Area of Science:

• Pharmacology and Traditional Chinese Medicine
• Nanotechnology in Drug Delivery
• Natural Product Chemistry

Background:

• Celastrol, a triterpene from Tripterygium wilfordii, exhibits significant anti-inflammatory, anti-autoimmune, anti-cancer, antioxidant, and neuroprotective properties.
• Clinical application of celastrol is hindered by poor aqueous solubility, low oral bioavailability, and substantial organ toxicity.
• Various formulation strategies are being explored to enhance celastrol's in vivo efficacy by improving bioavailability and reducing toxicity.

Purpose of the Study:

• To review and summarize nanotechnology-based celastrol formulations developed over the past 15 years.
• To highlight the therapeutic applications tested for these nanoformulations.
• To identify challenges and future directions for the clinical translation of celastrol nanoformulations.

Main Methods:

• Comprehensive literature survey of celastrol nanoformulations published in the last 15 years.
• Analysis of formulation strategies and their impact on celastrol efficacy and toxicity.
• Evaluation of therapeutic applications investigated for developed nanoformulations.

Main Results:

• A multitude of celastrol nanoformulations have been developed and evaluated for diverse therapeutic uses.
• Nanotechnology approaches have shown potential in overcoming celastrol's pharmacokinetic and toxicity limitations.
• Significant research efforts are focused on optimizing celastrol delivery systems.

Conclusions:

• Nanotechnology-based formulations represent a promising strategy to overcome the clinical translation barriers of celastrol.
• Further research is needed to address the unmet needs in the clinical translation of celastrol nanoformulations.
• Identifying a clear path forward is crucial for realizing the therapeutic potential of celastrol.