Perpustakaan Digital ITB

Salbutamol Sulphate (SS) is a 13-2-adrenegic agonist used to treat asthma. SS has a unique site-specific absorption at the stomach and upper layer of the small intestines. This is due to the anionic nature of the mucus layer which interacted with the cationic SS. The bioavailability of the drug is relatively low at —40 % due to extensive sulfonation at the gut and degradation in the colon. Increasing the surface area and contact time can counter this drawback. Developing it into nano-sized can prevent fast excretion of the drug from the stomach. In this research, SS in muco-adhesive gastroretentive nanoparticles were formulated. The purpose of this research was to formulate mucoadhesive nanoparticles based on Chitosan (CS) which is cationic with addition of non-ionic and anionic polymers which form nanoparticle core to enable adsorption of cationic SS to interact with the anionic mucus layer. Developments of the SS gastro-retentive nanoparticles were done by two methods. First was the ionotropic gelation of Chitosan with Sodium Tripolyphosphate (STPP) with addition of Polyethylene Oxide (PEO) and Polyvinyl Alcohol (PVA). Second method is using CS and Polyacrylic Acid (PAA) to form polyelectrolyte complex. The evaluation consisted of particle size, zeta potential, poly-dispersity index, entrapment efficiency and in-vitro drug release. Nanoparticles in ionotropic gelation method yielded result of particle size ranging from 171.1 — 294.4 nm, polydispersity index of 0.174 — 0.258, zeta potential of + 20.51 — +37.96 and entrapment efficiency 30.71% - 61.51%. Nanoparticles in polyelectrolyte complex method yields result of particle size of 221.3 — 320.1 nm, polydispersity index of 0.19 — 0.38, zeta potential of +20.31 - +38.33 and entrapment efficiency 18.41% - 66.71%. The drug release of ionotropic gelation method yielded result of 30.05% — 93.98 % in 12 hours while in polyelectrolyte complex method yielded result of 69.51% - 90.34%. It can be concluded that the SS gastroretentive nanoparticles of two methods has been developed. The best formula was F10 which was combination of chitosan-polyacrylic acid with size of 221.3mn, PI of 0.189, zeta potential of +20.96 and entrapment efficiency of 66.71°A and met all drug release requirements.