Andrographolide-loaded nanoparticles for brain delivery: Formulation, characterisation and in vitro permeability...

Area of Science:

• Pharmacology
• Nanotechnology
• Neuroscience

Background:

• Andrographolide (AG) from Andrographis paniculata has anti-inflammatory and neuroprotective potential.
• Low bioavailability limits AG's therapeutic application, especially for neurodegenerative disorders.

Purpose of the Study:

• To enhance AG's bioavailability and blood-brain barrier (BBB) permeability using nanoparticles.
• To compare the efficacy of human serum albumin (HSA) nanoparticles (NPs) and poly ethylcyanoacrylate (PECA) NPs in delivering AG across the BBB.

Main Methods:

• AG was loaded into HSA NPs (thermo-crosslinked - HSAT, chemically crosslinked - HSAC) and PECA NPs.
• Nanoparticle characterization included size, zeta potential, and drug release studies.
• An in vitro BBB model (hCMEC/D3 cells) and UPLC-MS/MS were used to assess AG permeability.

Main Results:

• Free AG did not cross the in vitro BBB model.
• HSAT NPs improved AG's BBB permeation twofold while preserving BBB integrity.
• PECA NPs temporarily disrupted BBB integrity.

Conclusions:

• Nanoparticle formulation, specifically HSAT NPs, can overcome AG's low bioavailability and enhance its delivery across the BBB.
• HSAT NPs represent a promising strategy for developing AG-based therapies for neurodegenerative diseases.