An update on Nanoparticle Formulation Design of Piperine to Improve its Oral bioavailability: A Review

Piperine, a crystalline alkaloid compound isolated from Piper nigrum, Piper longum, and other types of pipers, has many excellent pharmacological advantages for preventing and treating some specific diseases, such as analgesic, anti-inflammatory, hepatoprotective, antimetastatic, antithyroid, immunomodulatory, antitumor, rheumatoid arthritis, osteoarthritis, Alzheimer's, and anticancer. However, its potential for clinical use through oral administration is hindered by water solubility and poor bioavailability. The low level of oral bioavailability is caused by low solubility in water and is photosensitive, susceptible to isomerization by UV light, which causes piperine concentration to decrease. A lot of nanoparticle formulation approaches have been applied to improve the poor oral bioavailability of piperine. Oral nanoparticle formulation strategies have been successfully implemented in increasing the solubility and bioavailability of piperine within the body, such as the formulation of nanoparticles, nanosuspensions, liposomes, complexation using polymers, and micro/nano-emulsions. This nanoparticle formulation approach has been successful in increasing the solubility, permeability, and bioavailability of piperine effectively. In addition, this nanoparticle formulated piperine can deliver piperine in a targeted manner and increase the efficacy of piperine treatments, such as for Alzheimer’s disease, epilepsy, rheumatoid arthritis, diabetes, breast cancer, colon cancer, and human brain cancer.