Design, Development, Physicochemical Characterization, and In Vitro Drug Release of Formoterol PEGylated PLGA Polymeric Nanoparticles

Abstract

Polymeric nanoparticles’ drug delivery systems represent a promising platform for targeted controlled release since they are capable of improving the bioavailability and tissue localization of drugs compared to traditional means of administration. Investigation of key parameters of nanoparticle preparation and their impact on performance, such as size, drug loading, and sustained release, is critical to understanding the synthesis parameters surrounding a given nanoparticle formulation. This comprehensive and systematic study reports for the first time and focuses on the development and characterization of formoterol polymeric nanoparticles that have potential application in a variety of acute and chronic diseases. Nanoparticles were prepared by a variety of solvent emulsion methods with varying modifications to the polymer and emulsion system with the aim of increasing drug loading and tuning particle size for renal localization and drug delivery. Maximal drug loading was achieved by amine modification of polyethylene glycol (PEG) conjugated to the poly(lactic-co-glycolic acid) (PLGA) backbone. The resulting formoterol PEGylated PLGA polymeric nanoparticles were successfully lyophilized without compromising size distribution by using either sucrose or trehalose as cryoprotectants. The physicochemical characteristics of the nanoparticles were examined comprehensively, including surface morphology, solid-state transitions, crystallinity, and residual water content. In vitro formoterol drug release characteristics from the PEGylated PLGA polymeric nanoparticles were also investigated as a function of both polymer and emulsion parameter selection, and release kinetics modeling was successfully applied.

Freeze Drying of Polymer Nanoparticles and Liposomes Exploiting Different Saccharide-Based Approaches

“…Freeze drying allows drug delivery systems, such as nanoparticles and liposomes, to be obtained and stored as dry forms, thus avoiding chemical and physical instability and improving long-term storage [ 33 , 34 ]. However, several factors can lead to colloidal instability during the freeze-drying process, and many strategies are considered to avoid particle aggregation [ 7 ].…”

Targeting the Kidneys at the Nanoscale: Nanotechnology in Nephrology

“…Furthermore, basic pharmacology has been studied in both healthy and diseased rodents, with original discovery and validation of MNPs occurring in hairless immunocompetent and wild type mouse strains. 97 , 101 , 106 , 107 Interestingly, kidney-specific targeting has been demonstrated in nude and nod-scid gamma mice bearing flank and orthotopic lung tumors in work designed to avoid NP localization to tumors in chemotherapy-associated AKI. 109 It should be noted that most studies have been performed in mice to date, with one initial work in rats.…”

Optimization and modeling of PEGylated, hydrocortisone‐17‐butryate‐loaded poly(lactic‐co‐glycolic acid) microspheres

“…However, the effects of PEGylation on corticosteroid release and overall characteristics of PLGA nanospheres has not been quantified and accurately computationally modeled. [15][16][17][18] Therefore it is proposed, through formulation optimization and modeling this corticosteroid delivery platform can extend therapeutic duration, alleviate high corticosteroid concentration effects, and be more effectively dosed through application of a biphasic release model for the PEGylated nanocarriers.…”