Rifabutin-Loaded Nanostructured Lipid Carriers as a Tool in Oral Anti-Mycobacterial Treatment of Crohn’s Disease
Helena Rouco,
Patricia Diaz-Rodriguez,
Diana P. Gaspar,
Lídia M. D. Gonçalves,
Miguel Cuerva,
Carmen Remuñán-López,
António J. Almeida,
Mariana Landin
Affiliations
Helena Rouco
R+D Pharma Group (GI-1645), Strategic Grouping in Materials (AEMAT), Department of Pharmacology, Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Universidade de Santiago de Compostela-Campus Vida, 15782 Santiago de Compostela, Spain
Patricia Diaz-Rodriguez
Drug Delivery Systems Group, Department of Chemical Engineering and Pharmaceutical Technology, School of Sciences, Universidad de La Laguna (ULL), Campus de Anchieta, 38200 La Laguna (Tenerife), Spain
Diana P. Gaspar
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisbon, Portugal
Lídia M. D. Gonçalves
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisbon, Portugal
Miguel Cuerva
Department of Physical Chemistry, Nanomag laboratory, Universidade de Santiago de Compostela-Campus Vida, 15782 Santiago de Compostela, Spain
Carmen Remuñán-López
Nanobiofar Group (GI-1643), Department of Pharmacology, Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Universidade de Santiago de Compostela-Campus Vida, 15782 Santiago de Compostela, Spain
António J. Almeida
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisbon, Portugal
Mariana Landin
R+D Pharma Group (GI-1645), Strategic Grouping in Materials (AEMAT), Department of Pharmacology, Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Universidade de Santiago de Compostela-Campus Vida, 15782 Santiago de Compostela, Spain
Oral anti-mycobacterial treatment of Crohn’s disease (CD) is limited by the low aqueous solubility of drugs, along with the altered gut conditions of patients, making uncommon their clinical use. Hence, the aim of the present work is focused on the in vitro evaluation of rifabutin (RFB)-loaded Nanostructured lipid carriers (NLC), in order to solve limitations associated to this therapeutic approach. RFB-loaded NLC were prepared by hot homogenization and characterized in terms of size, polydispersity, surface charge, morphology, thermal stability, and drug payload and release. Permeability across Caco-2 cell monolayers and cytotoxicity and uptake in human macrophages was also determined. NLC obtained were nano-sized, monodisperse, negatively charged, and spheroidal-shaped, showing a suitable drug payload and thermal stability. Furthermore, the permeability profile, macrophage uptake and selective intracellular release of RFB-loaded NLC, guarantee an effective drug dose administration to cells. Outcomes suggest that rifabutin-loaded NLC constitute a promising strategy to improve oral anti-mycobacterial therapy in Crohn’s disease.
