Evaluation of Apparatus for Obtaining PLGA Nanoparticles by Injection Nanoprecipitation

Rosario

Congreso; 7 MA REUNIÓN INTERNACIONAL DE CIENCIAS FARMACÉUTICAS; 2023

Due to its simplicity, injection nanoprecipitation is a widely utilized methodology in the pharmaceutical field. This method for the preparation of nanoparticles (NPs) requires two phases, one of which is an organic phase composed of a solvent that solubilizes the drug, and then it is added drop by drop in an aqueous phase. As a result, this technique is highly valuable for Class II or Class IV Biopharmaceutical Classification System drug substances, with the potential to achieve encapsulation efficiencies close to 100%. Therefore, the objective of this study was compare two apparatus for the preparation of polymeric NPs composed of poly (lactic-co-glycolic acid) (PLGA) using Albendazole (ABZ) as a model drug, a broad-spectrum antiparasitic with extremely low aqueous solubility, and then characterize the optimal NPs obtained. The particle size and Zeta potential of the NPs were determined by Dynamic Light Scattering. Then, the optimal NPs were obtained in solid-state through lyophilization, with the evaluation and testing of various cryoprotective agents. The solid samples were characterized using Powder X-ray Diffraction, Fourier Transform Infrared Spectroscopy, Differential Scanning Calorimetry, Thermogravimetry, and Scanning Electron Microscopy (SEM). Additionally, biopharmaceutical properties such as solubility in different media and dissolution percentage were determined. First, PLGA NPs were produced by nanoprecipitation using a syringe pump in Spain (Harvard Apparatus Ltd.; Edenbridge, United Kingdom) in horizontal position (HSP) and an open-source syringe pump (OSSP) designed for vertical use in Argentina. Then, the NPs obtained were compared using polydispersity index values, which indicated that all samples were monodisperse. Additionally, similar Zeta potential values were observed among them. However, the apparatus OSSP used in Argentina allowed for the preparation of ABZ-loaded NPs and empty NPs with smaller particle sizes. This could be attributed to the OSSP?s superior precision in regulating the drip rate compared to the HSP. These results revealed that NPs synthesis in Argentina was better. Furthermore, SEM analysis revealed that the NPs exhibited a spherical morphology with a smooth surface. Lastly, it was observed that the drug-loaded NPs exhibited an increase in solubility compared to the free drug in all the studied media, as well as a higher dissolution percentage after two hours. In conclusion, the OSSP implemented for the development of nanosystems is a beneficial methodology for obtaining therapeutic entities suitable for low aqueous solubility drugs such as ABZ.