ABSTRACT

Andrographolide (AG) is the main bioactive component present in Andrographispaniculata plant leaf extracts, which is responsible for a wide spectrum of pharmacological activities, such as strong anti-inflammatory activity, as well as anticancer, immunomodulatory, and antihyperlipidemic activities and hepatoprotection. The remarkable free radical scavenger capacity of this compound plays an important role against oxidative stress in general via the inhibition of pathways related to inflammation and apoptosis. However, AG bioavailability is compromised by its physicochemical properties, such as low aqueous stability, short biological half-life, and poor cellular permeability, resulting in poor bioactivity which limits its potential clinical use. Taking full advantage of the therapeutic potential of AG presents a challenge facing its inadequate pharmacokinetics. With the advent of novel drug delivery systems, AG can be formulated as the payload of nanosystems as a strategy to retain stability, improve the pharmacokinetics, and, depending on the carrier formulation, allow AG vectorization. In this chapter, a critical analysis of AG is carried out with emphasis on its therapeutic activity, followed by a discussion on new delivery systems, their current producing methods, and their therapeutic role in improving the management of chronic illnesses by circumventing the limiting physicochemical characteristics and pharmacokinetics of the Biopharmaceutics Classification System (BCS) Class II AG.