Solid lipid nanoparticles as intracellular drug transporters: An investigation of the uptake mechanism and pathway

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

Authors

Martins, S (Author) Other; Costa Lima, S (Author) Other; Carneiro, T (Author) Other; Cordeiro da Silva, A (Author) FFUP; Souto, EB (Author) Other; Ferreira, DC (Author) FFUP

Journal

Title: International Journal of Pharmaceutics

Vol. 430

Pages: 216-227

ISSN: 0378-5173

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 82 Citations

Scopus - 103 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-002-8SE

DOI: 10.1016/j.ijpharm.2012.03.032

Abstract (EN): The aim of this work was to develop a systematic analysis of the cellular internalisation mechanism and pathway of solid lipid nanoparticles (SLN) internalisation. To evaluate if SLN show cell uptake and to understand the mechanism of internalisation, four human glioma cell lines (A172, U251, U373 and U87) and a human macrophage cell line (THP1) were used. For this purpose rhodamine 123 (R123) was loaded into SLN coated with polysorbate 60 and 80. Fluorescence microscopy and flow cell cytometry techniques were assessed to study internalisation of these systems within the cells. MTT studies were performed to evaluate the cytotoxicity of the R123-loaded SLN. To assess the SLN internalisation mechanism and intracellular pathway, excluding endocytosis mechanisms were applied. Our results revealed that R123-loaded SLN with mean size below 200 nm and slight negative surface charge (around -20 mV) have the ability to be internalised by gliomas in a higher amount than by macrophages. The mechanism of internalisation was found to be mainly through a clathrin-dependent endocytic pathway. In addition, the cytotoxicity of SLN was higher for gliomas than for macrophages. These results suggest that SLN can be a promising alternative in brain tumours treatment.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 12