ENHANCING SOLUBILITY AND PERMEABILITY OF ANDROGRAPHOLIDE, ISOLATED FROM ANDROGRAPHIS PANICULATA, THROUGH ITS SELF-EMULSIFYING DRUG DELIVERY SYSTEM (SEDD)

Le Thi Kim Van ^1,*, Keiko Minami², Higashino Haruki²,  Le Viet Dung¹, Hoang Thi Thanh Nga¹, Trinh Hien Trung³,  Makoto Kataoka², Yamashita Shinji ²

¹National Institute of Medicinal Materials, Hanoi, Vietnam;

²Faculty of Pharmaceutical Sciences, Setsunan University, Osaka, Japan;

³School of Pharmacy, Haiphong University of Medicine and Pharmacy

*Corresponding author: lethikimvan@gmail.com

(Received September, 04^th, 2016)

Summary

Enhancing Solubility and Permeability of Andrographolide, Isolated from Andrographis paniculata,

Through its Self-Emulsifying Drug Delivery System (SEDD)

Andrographolide has a low aqueous solubility and oral bioavailability, which limits its clinical application. The dosage forms of andrographolide were reformed to improve its aqueous solubility and oral bioavailability. The formulation, bioavailbility of andrographolide, was studied. A formulation of dried O/W microemulsion (F4) consisting of an oil phase of capmul PG-8, and surfactant of cremophor RH40 and co-surfactant of alcohol, and water, together with manitol as solid carrier was found to be ideal, with mean droplet size of 148.8 nm and 159.9 nm in emulsion before freeze drying and after redispersion. The fomulation 4 (F4) also showed the high increase of solubility 98 % in dissolution and 3% in permeation, in comparison to andrographolide (50% in dissolution and 0.07 % in permeation). It led to improve on prediction of human absorption from 12% (andrographolide) to 80% (F4). Therefore, the study would promise an application after further study in formula stimulation

Keywords: Andrographolide, Poor water-soluble drug, D/P systems, Dried-microemulsion, SEDDs.