Formulation of functionalized PLGA polymeric nanoparticles for targeted drug delivery

Abstract Polymeric nanoparticles (PNPs) are emerging as promising carriers for controlled drug delivery. Poly(D,L-lactic- co -glycolic acid) (PLGA) is the most frequently used biodegradable and biocompatible polymer in the design nanoparticles for biomedical applications. Herein, we present PNPs prepared from the chemical modification of PLGA with sucrose and a cholic acid moieties (abbreviated as Suc-PLGA-Chol). The primary purpose was to study the influence of several processing parameters on particle size. The PNPs were prepared by nanoprecipitation and characterized by dynamic light scattering (DLS) and scanning electron microscopy (SEM). Under optimal experimental conditions, the prepared PNPs had a size of ca. 130 nm with a relatively narrow particle size distribution and a negative ζ-potential. The improvement of the freeze-drying process by the use of cryoprotectants was also studied. Drying of the PNPs under phosphorus pentoxide was explored as an alternative to lyophilization. Our research has demonstrated that formulation variables can be exploited in order to tailor particle size. In addition, glycosylated nanocarriers may become an essential aspect of nanoparticle design, enhancing both targeting and diagnostics.