Nanoparticle drug delivery characterization for fluticasone propionate and in vitro testing

Abstract

Glucocorticoids, such as fluticasone propionate (FP), are used for the treatment of inflammation and alleviation of nasal symptoms and allergies, and as an antipruritic. However, both short- and long-term therapeutic use of glucocorticoids can lead to muscle weakness and atrophy. In the present study, we evaluated the feasibility of the nanodelivery of FP with poly(dl-lactide-co-glycolide) (PLGA) and tested in vitro function. FP-loaded PLGA nanoparticles were prepared via nanoprecipitation and morphological characteristics were studied via scanning electron microscopy. FP-loaded nanoparticles demonstrated an encapsulation efficiency of 68.6% ± 0.5% with a drug loading capacity of 4.6% ± 0.04%, were 128.8 ± 0.6 nm in diameter with a polydispersity index of 0.07 ± 0.008, and displayed a zeta potential of –19.4 ± 0.7. A sustained in vitro drug release pattern was observed for up to 7 days. The use of fluticasone nanoparticle decreased lipopolysaccharide (LPS)-induced lactate dehydrogenase release compared with LPS alone in C2C12 treated cells. FP also decreased expression of LPS-induced inflammatory genes in C2C12 treated cells as compared with LPS alone. Taken together, the present study demonstrates in vitro feasibility of PLGA-FP nanoparticle delivery to the skeletal muscle cells, which may be beneficial for treating inflammation.

Nanoparticles/nanoplatform to carry and deliver the drug molecules to the target site

“…The obtained particles have a size of 128 nm, a zeta potential of -19 mV, and the encapsulation efficiency and drug loading capacity were 68% and 4% respectively. The invitro studies showed a sustained release over a 10 days period, and cell assays on C2C12 myoblast cells show a decrease in inflammation, and effectiveness at 10 times lower concentration of the encapsulated form compared with the free form of the drug [31]. In another study, PEGylated PLGA nanoparticles loaded with paclitaxel, an anticancer agent, were synthesized with the aim of in-vivo administration.…”