Nanosystems as modulators of intestinal dapsone and clofazimine delivery

• Type: Article in International Scientific Journal
• Date: 2018

Authors

Chaves, LL (Author) Other; Costa Lima, SAC (Author) Other; Vieira, ACC (Author) Other; Barreiros, L (Author) Other; Marcela A Segundo (Author) FFUP; Ferreira, DC (Author) FFUP; Sarmento, B (Author) Other; Salette Reis (Author) FFUP

Journal

Title: Biomedicine & Pharmacotherapy

Vol. 103

Pages: 1392-1396

ISSN: 0753-3322

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 1 Citation

Scopus - 4 Citations

Other information

Authenticus ID: P-00Q-E83

DOI: 10.1016/j.biopha.2018.04.195

Abstract (EN): The aim of this work was to assess the feasibility of drug nanosystems combination for oral therapy of multi bacillary leprosy. The anti-leprotic drugs dapsone (DAP) and clofazimine (CLZ) were incorporated within polymeric nanosystems and studied per se and in combination. DAP was loaded in Eudragit L100 nanoparticles (NPs-DAP) while CLZ was loaded in (poly(lactic-co-glycolic acid) (NPs-CLZ). The nanosystems exhibited around 200 nm in size and a drug loading of 12% for each drug. In vitro cytotoxicity on intestinal Caco-2 cells revealed that after 8 h incubation, DAP alone and within NPs were not toxic up to 100 mu g mL(-1), while CLZ per se was toxic, reducing cell viability to 30% at 50 mu g mL(-1). Caco-2 exposed to the combination of NPs-DAP (100 mu g mL(-1)) and NPs-CLZ (50 mu g mL(-1)) exhibited 80% of viability. Caco-2 monolayer permeability assays revealed that DAP and CLZ in the nanosystems per se or in NPs-DAP/NPs-CLZ combination crossed the intestinal barrier. No significant differences were observed between the single nanosystems or in combination with the apparent permeability values and the amount of permeated drug. Thus, the NPs-DAP/NPs-CLZ combination seems to be a promising platform to deliver both drugs in association, representing an important step towards the improvement of multibacillary leprosy therapy.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 5