Single step encapsulation process of ivermectin in biocompatible polymer using a supercritical antisolvent system process

Abstract

This paper reports the production of ivermectin (IVM)‐encapsulated lecithin/poly (methyl methacrylate) (PMMA) nanoparticles via supercritical antisolvent system (SAS). Of a total of nine formulations, experimental condition R7 containing 10% lecithin relative to polymer (PMMA) resulted in the smallest average experimental particle diameter (dexp), more stable surface charges and high IVM encapsulation efficiency (75.9 ± 2.5%). Nanoparticles were morphologically, thermally, and conformationally characterized using scanning electron microscopy (SEM), thermogravimetric analysis/thermogravimetric derivative (TGA/DTG), and Fourier transform infrared–attenuated total reflectance (FTIR/ATR) techniques. In vitro release test showed that the drug has a controlled release of approximately 110 h. Peppas–Sahlin model (R2 = 0.99) was able to describe the diffusion of the drug correctly. Cytotoxicity analysis showed high compatibility of nanoparticles with epithelial cells, fibroblasts, and macrophages. Population balance equation was used to determine kinetic parameters from experimental data of average particle diameter. Synthesized nanoparticles showed high solution stability, good encapsulation capacity, and showed no adverse effects on cell viability, indicating their high potential as a new IVM carrier system for veterinary medicine and human applications.

Ivermectin-Loaded Mesoporous Silica and Polymeric Nanocapsules: Impact on Drug Loading, In Vitro Solubility Enhancement, and Release Performance

“…In the third region, at around 330 °C, molecular degradation begins, resulting in axial deformation of the O-H bonds and methyl groups, followed by unsaturated lactone breakage, between 350 and 400 °C. The total decomposition of the sample occurs above a temperature of 450 °C [ 49 ]. For MCM-41, the thermogram demonstrates a tiny decline in mass, indicating no organic residue in pure silica.…”

“…In the first region, around a temperature of 150 • C, the percentage mass loss is associated with the water desorption and alteration of the crystalline form of the drug. The second stage of thermal degradation occurs close to 300 • C and can be attributed to the degradation of the amphiphilic esters (C-O-C) of IVM due to the spatial configuration of the radical [49]. In the third region, at around 330 • C, molecular degradation begins, resulting in axial deformation of the O-H bonds and methyl groups, followed by unsaturated lactone breakage, between 350 and 400 • C. The total decomposition of the sample occurs above a temperature of 450 • C [49].…”

“…The second stage of thermal degradation occurs close to 300 • C and can be attributed to the degradation of the amphiphilic esters (C-O-C) of IVM due to the spatial configuration of the radical [49]. In the third region, at around 330 • C, molecular degradation begins, resulting in axial deformation of the O-H bonds and methyl groups, followed by unsaturated lactone breakage, between 350 and 400 • C. The total decomposition of the sample occurs above a temperature of 450 • C [49]. For MCM-41, the thermogram demonstrates a tiny decline in mass, indicating no organic residue in pure silica.…”