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Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
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Upon entering the systemic circulation, drugs can distribute into the interstitial and intracellular fluid of various tissue cells. This distribution is facilitated by the binding of drugs to different cellular components within tissues, which may lead to drug accumulation in specific areas. Drugs bound to tissue components serve as reservoirs that release free drugs back into the system, prolonging the drug's overall action. However, this accumulation can also result in local toxicity.
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Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
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Bioavailability refers to the extent and rate at which a drug reaches systemic circulation in its active form. Extent refers to the amount of the drug that makes it into circulation, while rate is the speed at which it enters circulation. It is influenced by several factors critical for optimizing drug formulations, dosing regimens, and therapeutic outcomes.Physicochemical properties of drugs and formulationsThe solubility, stability, and dissolution rate of a drug significantly impact its...
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[Biodistribution of Rifabutin Polymeric Transport Form].

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    Vestnik Rossiiskoi Akademii Meditsinskikh Nauk
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    This study shows that encapsulating the antibiotic rifabutin in a biodegradable polymer significantly alters its biodistribution in rats. The polymer form leads to higher concentrations in the lungs and liver compared to the pure drug.

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    Area of Science:

    • Pharmacology
    • Biomaterials Science
    • Drug Delivery Systems

    Background:

    • Drug efficacy can be enhanced via targeted delivery systems.
    • Biodegradable polymers are used to create nanosized drug carriers.
    • Rifabutin's tissue biodistribution using a lactic and glycolic acid copolymer was investigated.

    Purpose of the Study:

    • To investigate the tissue biodistribution of rifabutin delivered via a lactic and glycolic acid copolymer.
    • To compare the biodistribution of polymer-bound rifabutin with pure rifabutin.

    Main Methods:

    • Two groups of Wistar rats received intragastric doses of rifabutin (10 mg/kg) – one group received the polymer form, the other the pure substance.
    • Animals were sacrificed at various time points (10 min to 24 h) post-administration.
    • Tissue samples (liver, lung, spleen, kidney, intestines, stomach, heart, brain) were analyzed for rifabutin concentration using high-performance liquid chromatography after liquid-liquid extraction.

    Main Results:

    • Rifabutin was detected in most tissues within 10 minutes, with peak concentrations at 1.5-3.5 hours.
    • The polymer form of rifabutin showed significantly higher concentrations in the lungs (p < 0.05).
    • Higher distribution coefficients for the polymer form were observed in the liver and lungs (15.83 and 10.14 µg/g, respectively).

    Conclusions:

    • Incorporating rifabutin into a polymeric form significantly alters its organ and tissue localization.
    • Extensive biodistribution of nanorifabutin was established in lung tissue, liver, and spleen.
    • The polymer-based delivery system shows potential for targeted antibiotic delivery.