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Related Concept Videos

Methods for Studying Drug Absorption: In situ01:09

Methods for Studying Drug Absorption: In situ

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In situ experiments, such as the Doluisio method and Single-Pass Perfusion technique, provide critical insights into drug uptake by simulating in vivo conditions for drug absorption.
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
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Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
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Methods for Studying Drug Absorption: In vitro01:16

Methods for Studying Drug Absorption: In vitro

509
In vitro experiments are crucial for understanding the transport and absorption of drugs through biological materials. These studies employ varied methods such as the diffusion cell method, the everted sac technique, and the everted ring technique.
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
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Non-Oral Extravascular Drug Absorption Routes01:15

Non-Oral Extravascular Drug Absorption Routes

434
Non-oral extravascular routes, which encompass sublingual, buccal, topical, intramuscular, and inhalation methods, primarily utilize passive diffusion to transport drugs into the systemic circulation. The absorption rates and effectiveness of these routes depend on the drug's physicochemical properties, as well as the patient's anatomical and pathophysiological state.
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more...
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Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance01:07

Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance

196
Drug transporters are critical in drug absorption, distribution, and excretion processes. They should be included in physiological-based pharmacokinetic (PBPK) models, which help predict human drug disposition. However, predicting this is challenging during drug development, especially when liver transport is involved. However, with a realistic representation of body transport processes, an accurate model may be possible.
A recent model describes pravastatin's hepatobiliary excretion,...
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Model Approaches for Pharmacokinetic Data: Compartment Models01:14

Model Approaches for Pharmacokinetic Data: Compartment Models

431
Compartmental analysis is a widely adopted approach to characterizing drug pharmacokinetics. It uses compartment models that conceptualize the body as a collection of reversibly communicating compartments, each representing a group of tissues exhibiting similar drug distribution characteristics. The movement rate of the drug between these compartments is typically described by first-order kinetics.
Two primary types of compartment models are recognized: mammillary and catenary. The more...
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Related Experiment Video

Updated: Dec 17, 2025

Visualizing and Quantifying Pharmaceutical Compounds within Skin using Coherent Raman Scattering Imaging
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Visualizing and Quantifying Pharmaceutical Compounds within Skin using Coherent Raman Scattering Imaging

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Modeling percutaneous absorption for successful drug discovery and development.

Hanumanth Srikanth Cheruvu1, Xin Liu1, Jeffrey E Grice1

  • 1Therapeutics Research Centre, The University of Queensland Diamantina Institute, The University of Queensland , Woolloongabba, Australia.

Expert Opinion on Drug Discovery
|June 26, 2020
PubMed
Summary

Designing topical drugs requires understanding skin absorption. Advanced computational models combining quantitative structure-activity relationships (QSAR/QSPR) with physiologically based pharmacokinetic/pharmacodynamic (PBPKPD) models improve drug discovery for dermal delivery.

Keywords:
in silico modelingClearancePBPKPDQSAR/QSPRexposurepercutaneous absorptionphysicochemical propertiespotencyskin irritancytoxicity

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Area of Science:

  • Dermal drug delivery and formulation science.
  • Computational modeling in drug discovery.
  • Pharmacokinetics and pharmacodynamics of topical agents.

Background:

  • Skin has been a route for drug administration for centuries.
  • Percutaneous absorption and efficacy depend on formulation and solute properties.
  • Current computational models for skin permeation have limitations.

Purpose of the Study:

  • To review market trends, skin physiology, and formulation factors relevant to topical drug discovery.
  • To summarize in silico model strategies for topical product design.
  • To highlight the limitations of current models and emerging trends.

Main Methods:

  • Review of market trends and skin physiology.
  • Analysis of solute permeability and formulation properties.
  • Summary of in silico modeling approaches, including QSAR/QSPR and PBPKPD.

Main Results:

  • In silico models are often limited by data from aqueous solutions.
  • Formulation, skin physiology, and solute properties significantly impact dermal delivery.
  • Combined QSAR/QSPR and PBPKPD models are emerging for effective drug design.

Conclusions:

  • Effective topical drug design necessitates considering multiple factors beyond simple solute properties.
  • Advanced computational strategies are crucial for optimizing percutaneous absorption.
  • Integrated in silico models offer a promising direction for topical drug discovery.