α, β-Arteether (ART) antimalarial drug is used to treat chloroquine-resistant malaria and cerebral malaria. The drug's solubility in water is relatively low (17 μg/mL), and 40% of the drug degrades in the stomach, resulting in poor bioavailability. This article discusses the quality by design technique used for formulation development and optimization of nanostructured lipid carriers (NLCs). The ART-NLCs were made by solvent diffusion method. To develop solid NLCs, the NLCs were freeze-dried and encapsulated in enteric-coated capsule shells. The prepared NLCs showed particle size ranging between 156.8 ± 12 nm while zeta potential ranging between - 26.1 ± 0.22 mV. They also showed high encapsulation efficiency (> 85%) and an amorphous drug's lipid matrix state. Pharmacokinetic parameters of optimized formulation enhance oral bioavailability to 18.45%. These investigations demonstrated the superiority of NLCs for improvement of solubility as well as oral bioavailability of poorly water-soluble drugs.
Keywords: In vivo performance; bioavailability; drug loading; nanostructured lipid carriers; permeability; quality by design.
© 2022. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.