FORMULATION AND ANTIMALARIAL ACTIVITY TEST OF ARTEMETHER CONTAINED IN SOLID LIPID NANOPARTICLES (SLN) IN VITRO AND IN VIVO

• Main Author: Febyuli Ulya, Shella
• Format: Theses
• Language: Indonesia
• Online Access: https://digilib.itb.ac.id/gdl/view/36974
• Institution: Institut Teknologi Bandung

Malaria is an infectious disease caused by the Plasmodium parasite. The mortality rate of humans infected with malaria per year is so high that it becomes a public health problem. The WHO recommends the use of artemisinin-based combination therapies (ACTs) for the treatment of malaria caused by P. falciparum parasites in both combination and single use. One of the artemisinin derivatives, artemether, is a potent anti-malarial drug. However, artemether has several disadvantages, namely (i) short half-life, usually between 3 to 5 hours; (ii) poor water solubility, resulting in low oral bioavailability (~ 40%); and (iii) the risk of degradation under acidic conditions. To improve these problem Solid Lipid nanoparticles (SLN) was prepared drug delivery technology. The purpose of this study was to characterize the physical parameters of the SLN artemether formula and test anti-malaria activity in vitro and in vivo. There were four SLN artemether formulas (P9, P12, P14, P15) which had particle size characterization of less than 250 nm, loading drug in SLN more than 80%, physical and chemical stability stable for 14 days storage at room temperature. The four formulations were tested for activity in vitro using P. falciparum 3D7 culture. IC50 values of formula P9 and P12 are 3.67 nM and 5.37 nM. While the IC50 value obtained on artemether suspension is 3.38 nM. The IC50 value of artemether SLN was almost the same as that of the artemether suspension indicating that the SLN artemether formulation still had good antimalarial activity and the artemether could still be released from the preparation. To test the success of the SLN artemether formula given orally, the anti-malaria artemether SLN activity was tested in vivo using P. berghei ANKA which infected Swiss Webster female mice aged 6-8 weeks, weighing 25-30 grams. The test is carried out using a four-day suppression method, namely the administration of a test solution at a dose of 10 mg / kg / day for 4 consecutive days, which is a screening standard for anti-malaria drugs. From the results of the in vivo test, the percentage of malaria parasite growth inhibition was compared between the four test groups, namely (i) artemether SLN (ii) artemether suspension (iii) blank SLN (iv) group not given treatment (control). Compared to controls, SLN artemether and artemether suspension had a 100% chemosuppression and 12.26% mean. inhibits parasite growth. From the in vivo test it can be concluded that for oral administration of SLN artemether formula can increase efficacy compared to artemether suspension formula.