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Related Concept Videos

Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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 secretion,...
Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

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...
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
Oral Drug Delivery Systems: Delayed-Release Systems01:11

Oral Drug Delivery Systems: Delayed-Release Systems

Delayed-release drug delivery systems are specialized pharmaceutical formulations designed to postpone the release of active compounds until the drug reaches a specific region of the gastrointestinal (GI) tract, typically the intestine. These systems are essential for drugs that may cause gastric irritation, are unstable in acidic environments, or need to exert therapeutic effects locally in the intestinal or colonic regions.The core feature of delayed-release systems is the use of enteric...
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH01:21

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles in drug...

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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
08:18

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Published on: July 27, 2022

Enhancing intestinal drug solubilisation using lipid-based delivery systems.

Christopher J H Porter1, Colin W Pouton, Jean F Cuine

  • 1Department of Pharmaceutics, Victorian College of Pharmacy, Monash University (Parkville campus), Parkville, Victoria 3052, Australia. Chris.Porter@vcp.monash.edu.au

Advanced Drug Delivery Reviews
|December 25, 2007
PubMed
Summary
This summary is machine-generated.

Lipid-based delivery systems enhance oral drug absorption by improving drug solubility in the gastrointestinal tract. This review details formulation principles for optimizing these systems, focusing on solubilization and in vitro performance indicators.

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Microfluidic Production of Lysolipid-Containing Temperature-Sensitive Liposomes
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Last Updated: Jul 8, 2026

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
08:18

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Published on: July 27, 2022

Microfluidic Production of Lysolipid-Containing Temperature-Sensitive Liposomes
09:51

Microfluidic Production of Lysolipid-Containing Temperature-Sensitive Liposomes

Published on: March 3, 2020

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery

Background:

  • Lipid-based delivery systems are crucial for oral administration of poorly water-soluble drugs.
  • Enhanced gastrointestinal drug solubilization is a primary mechanism for improving oral bioavailability.

Purpose of the Study:

  • To review the mechanistic basis of lipid-based systems for drug solubilization.
  • To evaluate in vitro methods for predicting in vivo performance.
  • To propose formulation design principles for lipid-based delivery systems.

Main Methods:

  • Review of existing literature on lipid-based formulations and oral bioavailability.
  • Analysis of in vitro dispersion and lipolysis tests.
  • Examination of surfactant digestion effects on formulation performance.

Main Results:

  • Lipid systems significantly enhance drug solubilization and oral bioavailability.
  • In vitro lipolysis models correlate with in vivo drug absorption.
  • Surfactant digestion can influence the performance of lipid-based formulations.

Conclusions:

  • Optimized gastrointestinal solubilization is key for oral drug delivery using lipid systems.
  • In vitro methods, particularly lipolysis, are valuable for formulation assessment.
  • Seven guiding principles for designing effective lipid-based delivery systems are presented.