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[EXPERIMENTAL STUDY OF PHARMACOKINETICS OF KETOPROFEN NANOSYSTEM FOR INHALATION ADMINISTRATION.]

M V Karlina, V M Kosman, O N Pozharitskaya

    Eksperimental'Naia I Klinicheskaia Farmakologiia
    |May 22, 2018
    PubMed
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    This summary is machine-generated.

    Ketoprofen nanosystem administered via endotracheal route rapidly enters bloodstream, peaking in 15 minutes. The drug concentrates in lung tissue, with limited spread to other organs and minimal blood-brain barrier penetration.

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    Area of Science:

    • Pharmacology
    • Drug Delivery Systems
    • Nanotechnology

    Background:

    • Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) used for pain and inflammation.
    • Nanosystems offer potential for targeted drug delivery and improved pharmacokinetic profiles.
    • Endotracheal administration is an alternative route for drug delivery, particularly for lung-targeted therapies.

    Purpose of the Study:

    • To investigate the pharmacokinetics of ketoprofen delivered via a nanosystem after endotracheal administration in rats.
    • To determine the absorption, distribution, and penetration of ketoprofen from the nanosystem into systemic circulation and various tissues.
    • To assess the extent of blood-brain barrier penetration following endotracheal nanosystem administration.

    Main Methods:

    • Pharmacokinetic study in outbred rats following a single endotracheal administration of ketoprofen nanosystem.
    • Quantification of ketoprofen in blood serum and tissue samples using High-Performance Liquid Chromatography (HPLC) with UV detection.
    • Analysis of drug distribution and concentration-time profiles in different organs.

    Main Results:

    • Ketoprofen rapidly entered systemic circulation after endotracheal nanosystem administration, reaching peak serum concentrations within 15 minutes.
    • The highest drug concentrations were found in lung tissue, near the administration site.
    • Ketoprofen demonstrated moderate tissue penetration in highly vascularized areas and weak penetration in moderately vascularized tissues.
    • Only a small amount of ketoprofen was found to cross the blood-brain barrier.

    Conclusions:

    • Endotracheal administration of ketoprofen nanosystem leads to rapid systemic absorption and high local concentration in the lungs.
    • The nanosystem facilitates targeted delivery to lung tissue with limited systemic distribution to other organs.
    • Blood-brain barrier penetration of ketoprofen from this nanosystem formulation is minimal.