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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,...
Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are employed to...
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

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

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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...

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Updated: Jun 4, 2026

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

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Published on: March 3, 2020

Decrease of liposomal size and retarding effect on fluconazole skin permeation by lysine derivatives.

Julia C Schwarz1, Hanspeter Kählig, Nadejda B Matsko

  • 1Research Platform Characterisation of Drug Delivery Systems on Skin and Investigation of Involved Mechanisms, University of Vienna, Vienna, Austria.

Journal of Pharmaceutical Sciences
|February 15, 2011
PubMed
Summary

Lysine derivatives Lys-5 and Lys-7 were used to optimize liposomes for drug delivery. These peptides modified liposome structure, reducing particle size and slowing fluconazole skin permeation for improved dermal delivery.

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Preparation, Administration, and Assessment of In Vivo Tissue-Specific Cellular Uptake of Fluorescent Dye-Labeled Liposomes
08:44

Preparation, Administration, and Assessment of In Vivo Tissue-Specific Cellular Uptake of Fluorescent Dye-Labeled Liposomes

Published on: July 30, 2020

Area of Science:

  • Pharmaceutics
  • Materials Science
  • Biochemistry

Background:

  • Liposomes are effective dermal drug delivery vehicles due to their ability to modify drug biodistribution.
  • Optimizing liposomal microstructure is key to enhancing drug delivery efficiency.
  • Lysine derivatives offer a novel approach to fine-tune liposomal properties.

Purpose of the Study:

  • To investigate the impact of lysine derivatives (Lys-5 and Lys-7) on liposome structure.
  • To evaluate the effect of these oligopeptides on the skin permeation of fluconazole.
  • To characterize the microstructural changes in 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) vesicles.

Main Methods:

  • Nuclear Magnetic Resonance (NMR) spectroscopy with praseodymium(III)chloride shift reagent to determine liposome structure.
  • (31)P NMR measurements to analyze liposomal composition.
  • Cryo-transmission electron microscopy (Cryo-TEM) for structural confirmation.
  • Skin permeation studies to assess drug diffusion.

Main Results:

  • Liposomes were primarily unilamellar vesicles, confirmed by NMR and Cryo-TEM.
  • Addition of Lys-5 and Lys-7 induced significant structural changes in the liposomes.
  • A particle size reduction of 10%–40% was observed upon addition of lysine derivatives.
  • Lysine derivatives demonstrated a retarding effect on the skin permeation of fluconazole.

Conclusions:

  • Lysine derivatives Lys-5 and Lys-7 effectively modify liposome microstructure.
  • These modifications lead to smaller vesicle sizes and altered drug permeation characteristics.
  • The findings suggest potential for lysine-modified liposomes in optimizing dermal delivery of drugs like fluconazole.