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Factors Influencing Bioavailability: First-Pass Elimination01:23

Factors Influencing Bioavailability: First-Pass Elimination

When a drug is taken orally, it undergoes a journey starting from the gastrointestinal (GI) tract, passing through the portal vein, reaching the liver, and finally entering the systemic circulation. This process involves the absorption of the drug across the GI tract. The liver is the primary site for metabolizing the drug, with some metabolism also occurring in the gut wall. This journey significantly reduces the quantity of the drug that reaches the systemic circulation, a phenomenon known as...
Drug Distribution: Tissue Binding01:21

Drug Distribution: Tissue Binding

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.
For...
Bioavailability: Influencing Factors01:22

Bioavailability: Influencing Factors

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...
Drug Distribution: Overview01:11

Drug Distribution: Overview

Drug distribution within the body is a dynamic process involving the movement of a drug in two directions across various compartments: from the bloodstream into tissues (tissue uptake) and from tissues back into the bloodstream (tissue release or redistribution). This process is passive and primarily driven by two variables: the concentration gradient between the bloodstream and the extravascular tissues and the drug's ability to cross the cell membrane.
Initially, the free drug in the...
Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems01:22

Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems

Bioavailability is a critical pharmacological concept that measures the extent and rate at which an active drug ingredient or therapeutic moiety enters the systemic circulation, remaining unchanged. It's a pivotal factor in determining a drug's efficacy and safety.The Biopharmaceutics Classification System (BCS) plays an essential role in drug development by categorizing drugs into four classes based on their solubility and permeability. This classification aids in understanding drug absorption...
Bioavailability: Overview01:13

Bioavailability: Overview

Bioavailability refers to the proportion of an unaltered drug that, after administration, enters the systemic circulation and can be distributed to the desired action site. Factors such as gastrointestinal (GI) absorption and liver biotransformation influence the bioavailability of a drug when it is administered orally. When a drug is administered intravenously, it enters the systemic circulation directly; by definition, its bioavailability is assumed to be 100%. The bioavailability of an...

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Related Experiment Video

Updated: May 21, 2026

Registered Bioimaging of Nanomaterials for Diagnostic and Therapeutic Monitoring
17:16

Registered Bioimaging of Nanomaterials for Diagnostic and Therapeutic Monitoring

Published on: December 9, 2010

Biodistribution of nanoparticles: initial considerations.

Lucas Torres Miranda Sa1, Marta de Souza Albernaz, Beatriz Ferreira de Carvalho Patricio

  • 1Laboratory of Nanoradiopharmaceuticals, Nuclear Engineering Institute, Brazil.

Journal of Pharmaceutical and Biomedical Analysis
|June 30, 2012
PubMed
Summary

This study used technetium-99m labeling and biodistribution in mice to reveal distinct nanoparticle behaviors. Different nanoparticle compositions showed varied tissue affinities and clearance rates, impacting their biological mechanisms.

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Area of Science:

  • Nanomedicine and Materials Science
  • Biomedical Engineering
  • Radiopharmacology

Background:

  • Nanotechnology is a rapidly growing field with significant potential in various biological applications.
  • Understanding the in vivo behavior of nanoparticles is crucial for developing effective nanomedicines.
  • Current knowledge gaps exist regarding the differential biodistribution and metabolic fate of diverse nanoparticle formulations.

Purpose of the Study:

  • To investigate the biological behavior of six distinct nanoparticles using advanced labeling techniques.
  • To elucidate the biodistribution patterns and clearance mechanisms of various nanoparticle compositions in a preclinical model.
  • To correlate nanoparticle physicochemical properties with their in vivo interactions and potential mechanisms of action.

Main Methods:

  • Labeling of six different nanoparticles with technetium-99m ((99m)Tc) achieving high labeling efficiency (>99%).
  • Comprehensive biodistribution studies in mice to track nanoparticle localization and retention over time.
  • Analysis of tissue-specific accumulation (e.g., lung, liver) and renal clearance rates.

Main Results:

  • Significant variations in nanoparticle biodistribution were observed based on composition and formulation.
  • Mesoporous silica nanoparticles exhibited high lung affinity, while polymeric nanoparticles were primarily cleared by the liver.
  • Differential renal clearance times indicated that nanoparticle interaction and solubility influence their pharmacokinetic profiles.

Conclusions:

  • Biodistribution studies are essential for predicting the in vivo behavior and potential therapeutic mechanisms of nanoparticles.
  • Nanoparticle properties, such as composition and formulation, critically dictate their biological fate and target engagement.
  • This research provides a foundation for rational design of nanoparticles with tailored pharmacokinetic and pharmacodynamic properties.