OPTIMASI DAN KARAKTERISASI MIKROSKOPIK NANOPARTIKEL POLY(LACTIC-CO-GLYCOLIC ACID) RIFAMPISIN BERLABEL FLUORESCEINAMINE DENGAN VARIASI POLY(VINYL ALCOHOL) DAN WAKTU SONIKASI
Daftar Isi:
- According to Biopharmaceutics Classification System (BCS), rifampicin is classified in class II which means it has low solubility in water but high permeability towards biological membrane. Low solubility will affect drug’s bioavailability hence, preparation and characterization of nano rifampicin was done to improve the solubility in order to improve the bioavailability and reduce the risk of side effects from rifampicin in large doses. The resulting nanoparticles can increase penetration into the macrophages so that a faster macrophage uptake occurs. Preparation of rifampicin into nanoparticle, using poly(lactic-co-glycolic acid) as encapsulation polymer and poly(vinyl alcohol) as stabilizer with emulsion solvent evaporation method in single emulsion type process. These nanoparticles were consisted of rifampicin, fluoresceinamine, PLGA, PVA, and ethyl acetate with variation of PVA 40 mg and 50 mg and 30 seconds and 60 seconds of sonication time. The determination of percentage of encapsulation efficiency (% EE) obtained result for optimum formula is 90.58 ± 0.15% with PVA 50 mg and time of sonication 60 seconds. The optimum formula was determined by using 22 factorial design method in estimating the dominant effect to decide its respon using Design Expert® version 10. The result of nanoparticles characterization such as diameter and particles distribution (Poly Dispersity Index/PDI) and potential zeta using Particle Size Analyzer (PSA) were 384 nm; 0.032; and +2.6 mV. Morphology particle of optimum formula was observed using Transmission Electron Microscope (TEM) showed spheric particles and homogen which PDI of 0.111. Uptake observation of macrophages using confocal laser scanning microscopy. PLGA-rifampicin-labeled fluoresceinamine nanoparticles produce a green color on microscopic observations while macrophages are red when fluorescence occurs. In the uptake of macrophages, the observed nanoparticles are yellow in color indicating a macrophage uptake occurs in nanoparticles whereas the nanoparticles attached to the macrophage surface are green when fluorescence occurs.