Formulasi dan Evaluasi Sediaan Gastroretentif Mukoadhesif Mikrokapsul Metronidazole dengan Menggunakan Kombinasi Alginat dan Kitosan

Abstract

The oral conventional metronidazole dosage forms have a short duration of action due to gastric emptying process, hence the treatment of ulcus pepticum using metronidazole become less effective. Due to retaining the dosage form in the stomach, a preparation form of gastroretentive drug delivery systems has been developed. The aim of this study was to developed a gastroretentive drug delivery systems of metronidazole using alginate and chitosan as polymers that could last longer in stomach so that it releases metronidazole in a sustained release and provides an anti-bacterial activity. The preparation were formulated into microcapsules using alginate and chitosan by ionotropic gelation method. Microcapsules were made in two forms, coated and uncoated. The dissolution tesest was carried out using paddle method in gastric medium at 37°C. Metronidazole content were measured using an ultra violet spectrophotometer at a wavelength of 277 nm. The moisture content of microcapsules was measured using moisture balance. The surface morphology of was examined by Scanning Electron Microscopy (SEM). The interaction of alginate and chitosan was tested using Fourier Transform Infrared (FTIR) and Differential Scanning Calorimetry (DSC). The mucoadhesive test was carried out in vitro using disintegration tester in gastric medium using animal stomachs. The antibacterial activity was carried out by the agar diffusion method using Eschericia coli and Staphyloccocus aureus. The test results showed that the coated microcapsule (2:1) and uncoated microcapsule (2:0.75) turns out to have the greatest dissolution and mucoadhesive properties. The drug released was sustained and gastroretentive followed Higuchi kinetics. The results of FTIR and DSC analysis showed that there was no interaction between metronidazole and the alginate-chitosan matrix. The dissolution aliquots from the drug release showed that metronidazole microcapsules were effective in inhibiting the growth of Eschericia coli and Staphylocous aureus since 5 minutes. Based on the results, it can be concluded that metronidazole gastroretentive microcapsules with a combination of alginate-chitosan coated (2:1) and uncoated (2:0.75) polymers are potential to be used as gastroretentive drugs for the treatment of gastric ulcers. Based on the results of the study, it can be concluded that gastroretentive microcapsules of metronidazole with a combination of alginate-chitosan polymers (2:1) and (2:0.75) have the potential to be used as an effective anti-bacterial drugs.