RIFABUTIN FORMULATION IN THE FORM OF LIPID NANOPARTICLES WHICH ARE POTENTIAL FOR ORAL ADMINISTRATION

• Main Author: Hidayat, Taufik
• Format: Theses
• Language: Indonesia
• Online Access: https://digilib.itb.ac.id/gdl/view/44115
• Institution: Institut Teknologi Bandung

Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis. The annual death number caused by tuberculosis is very large. The most common case is tuberculosis co-infection with HIV. Rifabutin is one of the drug taken for patients with this condition. Rifabutin has a few limitations including low solubility in water and consecuently low bioavailability. In order to improve the oral bioavailability, rifabutin loaded solid lipid nanoparticles (SLN) have been developed. The purpose of this study is to produce, characterize rifabutin SLN and determine bioavailability relative of SLN to rifabutin suspension. SLN is produced using a combination of high shear homogenation and ultrasonication methods, showing that the production method has good reproducibility. Three optimization F1, F2 and F3 formulations have been developed which have particle size less than 250 nm, entrapement efficiency of more than 97%. SLN produced is physically and chemically stable in 28 day. In vitro release test results showed a release at pH 1.2 of less than 50% for 4 hours and slower at pH 6.8 ie around 30% were released for 12 hours. The three formulations were tested in vivo using Wistar strain rats at a dose of 30 mg / kg body weight given orally. Pharmacokinetic profiles in male wistar rats showed increased AUCo-?and Cmax on F2 formulations. In addition SLN rifabutin using tween 80 as stabilizer can increase the relative bioavailability of rifabutin compared to suspension.