#TITLE_ALTERNATIVE#

• Main Author: BIN JAMALUDIN NIM: 20714313, WAHYUDIN
• Format: Theses
• Language: Indonesia
• Online Access: https://digilib.itb.ac.id/gdl/view/31529
• Institution: Institut Teknologi Bandung

Sulfasalazine is a antireumatoid artritis and include to BCS class IV, which has a <br /> <br /> low solubility and low permeability properties. Oral bioavailability for <br /> <br /> sulfasalazine is less than 15%. An oral nanostructured lipid carrier (NLC) <br /> <br /> formulation can be developed as once of alternative to improve the bioavailability <br /> <br /> of sulfasalazine. NLC was prepared by hot homogenazation and sonication method. <br /> <br /> Evaluation was carried out by characterization, in vivo testing and <br /> <br /> pharmacokinetic parameters determination. After the optimization has been <br /> <br /> accomplished, three formulation were selected with composition of PEG 8 Beeswax <br /> <br /> as a solid lipid and caprylic / capric triglyceride as a liquid lipid at a total <br /> <br /> concentration of 12% (ratio 9 : 1). The F1 formulation used a Cremophor RH 60 <br /> <br /> with a concentration of 2% as a single stabilizer. For F2 and F3 were stabilized by <br /> <br /> a combination of stabilizer and 1% Poloxamer 188, stabilizer and 0.75% TPGS <br /> <br /> respectively. The characterizations showed that F1, F2 and F3 have particle size <br /> <br /> of 234 ± 7.9 nm, 216 ± 8.6 nm and 241 ± 4.1 nm with polydispersity index of 0.406, <br /> <br /> 0.466 and 0.329 respectively. While the obtained potential zeta values were -8.8 <br /> <br /> mV, -6.1 mV, and -6.6 mV respectively. Almost 100 % of sulfasalazine was <br /> <br /> entrapped in lipid with entrapping efficiency of 99,9 %. Analysis with differential <br /> <br /> scanning calorimetry (DSC) showed a single endothermic peak of NLC. The <br /> <br /> Morphology of F1, F2 and F3 evaluated by transmission electron microscopy <br /> <br /> (TEM) and revealed a spherical shape. The in vivo study showed not only <br /> <br /> pronounced improvement in Cmaxbut also increasing on AUC0-&#8734;value compared to <br /> <br /> sulfasalazine suspension by 3,387 times. Therefore, NLC a suitable formulation for <br /> <br /> improving oral bioavailability of sulfasalazine. <br /> <br />