Long-term stability, biocompatibility and oral delivery potential of risperidone-loaded solid lipid nanoparticles

• Type: Article in International Scientific Journal
• Date: 2012

Authors

Silva, AC (Author) Other; Kumar, A (Author) Other; Wild, W (Author) Other; Ferreira, D (Author) FFUP; Santos, D (Author) Other; Forbes, B (Author) Other

Journal

Title: International Journal of Pharmaceutics

Vol. 436

Pages: 798-805

ISSN: 0378-5173

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 86 Citations

Scopus - 95 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-002-4F6

DOI: 10.1016/j.ijpharm.2012.07.058

Abstract (EN): A solid lipid nanoparticles (SLN) formulation to improve the oral delivery of risperidone (RISP), a poorly water-soluble drug, was designed and tested. Initially, lipid-RISP solubility was screened to select the best lipid for SLN preparation. Compritol (R)-based formulations were chosen and their long-term stability was assessed over two years of storage (at 25 degrees C and 4 degrees C) by means of particle size, polydispersity index (PI), zeta potential (ZP) and encapsulation efficiency (EE) measurements. SLN shape was observed by transmission electron microscopy (TEM) at the beginning and end of the study. The oxidative potential (OP) of the SLN was measured and their biocompatibility with Caco-2 cells was evaluated using the (4,5dimethylthiazol-2-yl) 2,5-dyphenyl-tetrazolium bromide (MTT) assay. In vitro drug release and transport studies were performed to predict the in vivo release profile and to evaluate the drug delivery potential of the SLN formulations, respectively. The RISP-loaded SLN systems were stable and had high EE and similar shape to the placebo formulations before and after storage. Classical Fickian diffusion was identified as the release mechanism for RISP from the SLN formulation. Biocompatibility and dose-dependent RISP transport across Caco-2 cells were observed for the prepared SLN formulations. The viability of SLN as formulations for oral delivery of poorly water-soluble drugs such as RISP was illustrated.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 8