#TITLE_ALTERNATIVE#
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 /> <...
Saved in:
| Main Author: | |
|---|---|
| Format: | Theses |
| Language: | Indonesia |
| Online Access: | https://digilib.itb.ac.id/gdl/view/31529 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| Institution: | Institut Teknologi Bandung |
| Language: | Indonesia |
| Summary: | 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-∞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 />
|
|---|