Journal de la nanomédecine et de la découverte biothérapeutique

Journal de la nanomédecine et de la découverte biothérapeutique
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ISSN: 2155-983X


Ibuprofen Nanoparticles for Oral Delivery: Proof of Concept

Catarina Pinto Reis, João Pinto Ferreira, Sara Candeias, Cátia Fernandes, Nuno Martinho, Natália Aniceto, António Silvério Cabrita and Isabel V. Figueiredo

Background: Using nanoparticles to improve non-steroidal anti-inflammatory drugs therapeutic profile is an interesting approach, especially concerning their gastric toxicity.

Objective: The aim of this work was to present a proof of concept for a nanoparticulate formulation composed of a biodegradable polymer poly (DL-lactic acid) (PLA) meant for oral delivery of ibuprofen (IBU) to systemic circulation with reduced gastric toxicity.

Materials and methods: IBU-loaded nanoparticles composed of PLA and poloxamer 188 were prepared by an emulsion/solvent diffusion method. The particles obtained were characterized for size, zeta potential and morphology, as well as encapsulation efficiency. Nanoparticles were given to Wistar rats at an equivalent dose of 12 mg/kg (t.i.d.) of ibuprofen for a period of 10 days. Both concentration of IBU in the plasma and toxicity in different tissues were evaluated.

Results: Nanoparticles displayed a size of 281.1 ± 66.7 nm with a zeta potential of -4.3 mV. Scanning electron microscopic images showed spherical shape particles with low polydispersity index. IBU concentration in blood samples indicated that nanoparticles were able to deliver IBU to systemic circulation. A significant reduction in toxicity was observed for nanoparticles in gastric mucosa compared to free ibuprofen. This may be due to controlled release of IBU from the nanoparticles, which decreases the mucosal contact to IBU. In summary, we designed a proof of concept for PLA nanoparticles as suitable carrier for IBU allowing reduced gastric toxicity of the drugs. This strategy can eventually be applied to other non-steroidal anti-inflammatory drugs.