Encapsulation of Andrographolide in poly(lactide-co-glycolide) Nanoparticles: Formulation Optimization and in vitro Efficacy Studies

Abstract

Andrographolide is a potential chemopreventive and chemotherapeutic agent that suffers from poor aqueous solubility. Encapsulation in poly(lactide-co-glycolide) (PLGA) nanoparticles can overcome solubility issues and enable sustained release of the drug, resulting in improved therapeutic efficacy. In this study, andrographolide was encapsulated in PLGA nanoparticles via emulsion solvent evaporation technique. Effect of various formulation parameters including polymer composition, polymer molecular weight, polymer to drug ratio, surfactant concentration and the organic solvent used on nanoparticle properties were investigated. A selected formulation was used to determine the effect of encapsulation in nanoparticles on andrographolide’s in vitro anticancer efficacy. Nanoparticles formulated using a polymer with 85:15 lactide to glycolide ratio and ethyl acetate as the organic solvent were found to be optimal based on average hydrodynamic particle size (135 ± 4 nm) and drug loading (2.6 ± 0.6%w/w). This formulation demonstrated sustained release of andrographolide over 48 h and demonstrated significantly greater in vitro anticancer efficacy compared to free drug in a metastatic breast cancer cell line. These results suggest that additional, more in-depth efficacy studies are warranted for the nanoparticle formulation of andrographolide.

Andrographolide Derivatives Target the KEAP1/NRF2 Axis and Possess Potent Anti‐SARS‐CoV‐2 Activity

“…Recent pharmaceutical studies were aimed at improving the poor bioavailability and solubility of andrographolide via appropriate delivery systems. [ 26 , 27 ] However, appropriate chemical modifications of andrographolide could be an even better option to overcome such issues. Therefore, three different amide derivatives ( 16 a – 16 c ) were synthesized from linear aliphatic or aromatic amines.…”

Andrographolide Induces anti-SARS-CoV-2 Response Through host-directed Mechanism: anin silicoStudy

“…Furthermore, Yen, with his colleagues, experimented and found that silver-loaded andrographolide nanoparticles enhance bioavailability by 594.3% and are efficient against pro-inflammatory cytokines (eg, IL-1β, IL-6 and TNF-α) and the chemokine IL-8 [ 106 ]. Similarly, in an in vitro breast cancer model, encapsulating andrographolide in PLGA nanoparticles helps to overcome solubility difficulties and allowed for continuous drug release [ 107 ]. The use of hydroxypropyl-β-cyclodextrin (HP-β-CD) formulated andrographolide molecule increased its bioavailability by 1.19 percent [ 109 ].…”

An insight into the pharmacological and analytical potential of Andrographolide

“…However, extensive research is to be done on its administration to higher animals and humans, and cytotoxicity limits should be checked. Moreover, studies have been conducted on the drug delivery system of andrographolide conjugated with microparticles and nanoparticles [132,133]. In the form of vesicles, nanoemulsions, micelles, and gold nanoparticles, andrographolide is used to treat various disorders.…”