Preparation and Characterization of Monensin Loaded PLGA Nanoparticles: <I>In Vitro</I> Anti-Malarial Activity Against Plasmodium Falciparum

Abstract

PLGA nanoparticles loaded with monensin (carboxylic ionophore) were prepared by emulsion solvent evaporation method using PLGA of molecular weight (Mw.) 19 000 and 110 000 Da. The nanoparticles were characterized by applying dynamic light scattering (DLS), atomic force microscopy (AFM), differential scanning calorimetry (DSC) and Fourier transformed infrared spectroscopy (FTIR). Negatively charged and spherical smooth surfaced nanoparticles of size range between 147-167 nm were obtained. The nanoparticles of monensin-PLGA showed no chemical interaction between monensin and the polymer molecules. The release kinetics in vitro studies exhibited biphasic release profile characterized by an initial fast release followed by a slower release. The antimalarial efficacy of monensin-PLGA nanoparticles was also examined. Monensin loaded in nanoparticles was 10-fold more effective in inhibiting the growth of P. falciparum in vitro as compared to free monensin. The antimalarial efficacy of monensin-PLGA nanoparticles was significantly dependent on the Mw. of the polymer.

Evaluation of Surfactants-Assisted Folic Acid-Loaded Pectin Submicrospheres: Characterization and Hemocompatibility Assay

“…Another major absorption band at 3417.38 cm -1 corresponded to free amino group (-NH 2 ) a major peak present in pectin. Generally, the spectral analysis measures the selective absorption of light by the vibration modes of specific chemical bonds in the compounds interacting [39]. While evaluating the experiment, any interaction occurring between the folic acid and pectin polymer would produce altered vibrations of their atoms involved in the interaction.…”

Salinomycin and Other Ionophores as a New Class of Antimalarial Drugs with Transmission-Blocking Activity

“…Salinomycin exhibits an IC 50 similar to that of mefloquine when tested against HepG2 cells, whereas monensin showed no significant toxicity at the highest tested concentration (46 M) (15). The narrow therapeutic index of salinomycin as a potential anticancer drug has already boosted the development of chemically modified derivatives or innovative drug delivery systems (66)(67)(68), which should be considered in their future development as new antimalarials.…”

A potential in situ gel formulation loaded with novel fabricated poly(lactide-co-glycolide) nanoparticles for enhancing and sustaining the ophthalmic delivery of ketoconazole

“…The same finding has been previously reported for PLGA NP-loaded capecitabine 32 and monensinloaded PLGA NPs. 33 The authors attributed this behavior to the existence of the drug in an amorphous or disorderedcrystalline phase, which is distributed as a molecular dispersion or a solid solution state in the polymeric matrix.…”