Abstract
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.
Highlights
Ibuprofen, 2-(4-Isobutylphenyl)propionic acid, is a NSAID that inhibits the cyclooxygenase system
IBU has poor water solubility (~ 1 mg/mL) [2], when given orally it is well absorbed. It is rapidly eliminated from systemic circulation displaying a relatively short half-life (1.7-2 h), and requiring several dosages for an effective and prolonged pharmacological activity [5]
The aim of the work described was to develop IBU-loaded Poly(lactic acid) (PLA) nanoparticles as a proof of concept of the value of this formulation as a delivery systems for NSAIDs, in general
Summary
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
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