4.7 Article

Preparation and characterization of pH-sensitive nanoparticles of budesonide for the treatment of ulcerative colitis

Journal

DRUG DESIGN DEVELOPMENT AND THERAPY
Volume 12, Issue -, Pages 2601-2609

Publisher

DOVE MEDICAL PRESS LTD
DOI: 10.2147/DDDT.S170676

Keywords

budesonide; nanoparticles; ES100/PLGA; in vitro release; pharmacodynamic

Ask authors/readers for more resources

Objective: The aim of this study was to develop pH sensitive nanoparticles of budesonide for the treatment of ulcerative colitis. Methods: The NPs system was characterized by the transmission electron microscopy (TEM), particle size, drug loading and encapsulation efficiency. In addition, in vitro drug release properties and pharmacokinetics were also investigated in detail. The optimized formulation was examined for its in-vivo targeting potential using 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced colitis in a rat model. Results: Dynamic light-scattering results showed that the particle size of budesonide-Eudragit S100/poly(lactic-co-glycolic acid) nanoparticles was around 110.5 nm, with a polydispersity index of 0.098. Transmission electron microscopy images showed that BUD-ES100/PLGA NPs were spherical with uniform size and relatively smooth surfaces. In vitro release showed that BUD-ES100/PLGA NPs required minimal release of drugs during its transit in the stomach and the upper small intestine to ensure that a maximum dose reached the colon. After the pharmacodynamic treatment, the myeloperoxidase value of BUD-ES100/PLGA NPs was close to the normal group. The histopathological examination of rectum showed that no sign of damages such as epithelial necrosis and sloughing epithelial cells was detected. Conclusion: Our findings suggested that BUD-ES100/PLGA NPs were a promising alternative to single pH-dependent systems for colitis therapy.

Authors

I am an author on this paper
Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.7
Not enough ratings

Secondary Ratings

Novelty
-
Significance
-
Scientific rigor
-
Rate this paper

Recommended

No Data Available
No Data Available