Synthesis and characterization of pH-sensitive drinkable nanoparticles for oral delivery of ibuprofen

Autor: Davide Moscatelli, Umberto Capasso Palmiero, Monica Lupi, Sara D A Barbieri, Azzurra Agostini
Rok vydání: 2018
Předmět:
Drug
Materials science
Polymers
Proton Magnetic Resonance Spectroscopy
media_common.quotation_subject
Administration
Oral
Emulsion polymerization
Ibuprofen
Bioengineering
02 engineering and technology
010402 general chemistry
medicine.disease_cause
01 natural sciences
Drug Delivery Systems
Therapeutic index
Cell Line
Tumor
medicine
Humans
General Materials Science
Electrical and Electronic Engineering
Cell Proliferation
media_common
Chromatography
Cell Death
Mechanical Engineering
Chemistry (all)
pH-sensitive
General Chemistry
Hydrogen-Ion Concentration
controlled release
ibuprofen
polymeric nanoparticles
Materials Science (all)
Mechanics of Materials
021001 nanoscience & nanotechnology
Controlled release
0104 chemical sciences
Solvent
Emulsion
Nanoparticles
Spectrophotometry
Ultraviolet
Irritation
0210 nano-technology
medicine.drug
Zdroj: Nanotechnology. 29:225604
ISSN: 1361-6528
0957-4484
DOI: 10.1088/1361-6528/aab536
Popis: Ibuprofen (IBU) is a widespread drug used to treat both acute and chronic disorders. It is generally taken orally but the free drug can induce the irritation of the gastric mucosa due to its acid nature. In literature, different approaches have been adopted to prevent the release in the stomach, such as physical entrapment with film-coated tablets and drug-conjugates. Nevertheless, these solutions have many disadvantages, including the fast release of the drug and the difficulty to swallow the tablet, especially for children who may vomit or refuse the tablet. For this reason, in this work, novel formulations are proposed that do not require the encapsulation of the drug into a solid form and, in turn, their assumption as a pill. IBU has been linked to different types of methacrylates via ester bond in order to produce pH-responsive macromolecular monomers. The novelty is related to the use of these drug-conjugates macromonomer for the production of nanoparticles (NPs) via emulsion polymerization (EP), using water as solvent. The final emulsion is able to load up to 30 mg ml-1 of IBU, so less than 10 ml is required to be assumed to reach the minimum therapeutic dose of the drug (200 mg). Finally, the release of IBU from these novel drinkable formulations has been investigated in the gastric and intestinal simulated fluids to show the preferential release of IBU from the NPs in basic conditions. A comparison with an existing oral suspension has been performed to highlight the slower release in acid environment of these new formulations. Afterwards, the IBU loaded NPs were tested in vitro showing lower toxicity compared to the free drug.
Databáze: OpenAIRE
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