Ivermectin-loaded microparticles for parenteral sustained release: in vitro characterization and effect of some formulation variables.
Ivermectin (IVM) is a BCS II drug with potent antiparasitic activity in veterinary applications. In this study, poly(lactide-co-glycolide) (PLGA) and poly(DL-lactide) (PLA) Ivermectin-loaded microparticles were prepared by the simple emulsion (O/W) solvent evaporation method in order to obtain sustained release formulations for parenteral applications. The effects of polymer end-groups (ester or free acid) and the addition of the hydrophilic polyvinylpyrrolidone polymer (PVP) in in vitro drug release profiles were also studied. X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analysis showed that IVM was present in an amorphous state or as a molecular dispersion within the polymers or theirs mixtures with PVP and that a PVP-drug complex was formed. Drug entrapment efficiency in the microparticles (&gt;90%) was independent of the polymer composition, the end groups and the presence of PVP. However, microscopic (SEM) observations showed that the addition of PVP led to more porous microparticles accompanied by the increased rates of drug release.
Camargo
J A
JA
Nancy Universit&#x00E9;, Faculty of Pharmacy, Laboratory of Pharmaceutical Technology, 5, rue A. Lebrun, BP 80403, 54001 Nancy Cedex, France.
Sapin
A
A
Daloz
D
D
Maincent
P
P
D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems / Q000379:methods*; D004655:Emulsions / Q000737:chemistry / Q000494:pharmacology; D007306:Insecticides / Q000737:chemistry / Q000494:pharmacology; D007559:Ivermectin / Q000737:chemistry / Q000494:pharmacology*; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry / Q000494:pharmacology*; D011098:Polyglactin 910 / Q000737:chemistry / Q000494:pharmacology; D011100:Polyglycolic Acid / Q000737:chemistry / Q000494:pharmacology; D011205:Povidone / Q000737:chemistry / Q000494:pharmacology; D012997:Solvents / Q000737:chemistry; D013997:Time Factors; D014961:X-Ray Diffraction
D003692:Delayed-Action Preparations; D004655:Emulsions; D007306:Insecticides; D011091:Polyesters; D012997:Solvents; D011100:Polyglycolic Acid; D011098:Polyglactin 910; C033616:poly(lactide); D007559:Ivermectin; D011205:Povidone