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Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

439
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...
439
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH01:21

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

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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...
4.3K
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

666
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...
666
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

848
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
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Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

2.0K
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...
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Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

1.6K
The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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Related Experiment Video

Updated: Apr 3, 2026

Synthesis and Characterization of Multi-Modal Phase-Change Porphyrin Droplets
07:59

Synthesis and Characterization of Multi-Modal Phase-Change Porphyrin Droplets

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Propofol solubilization and structural transformations in dilutable microemulsion.

My Perlstein1, Abraham Aserin1, Ellen J Wachtel2

  • 1The Ratner Chair of Chemistry, Casali Institute of Applied Chemistry, The Institute of Chemistry, The Hebrew University of Jerusalem, Edmond J. Safra Campus, Givat Ram, Jerusalem 9190401, Israel.

Colloids and Surfaces. B, Biointerfaces
|September 28, 2015
PubMed
Summary

New propofol microemulsions offer a stable, safe, and water-dilutable alternative to current anesthetic formulations. These advanced systems ensure drug stability and safe administration for anesthesia induction and maintenance.

Keywords:
Drug deliveryMicroemulsionsPropofolSAXSSD-NMR

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Physical Chemistry

Background:

  • Propofol, an anesthetic, faces formulation challenges due to poor water solubility and instability in current emulsions.
  • Existing propofol emulsions are prone to oxidation and bacterial contamination, posing risks during medical procedures.

Purpose of the Study:

  • To develop and characterize novel, thermodynamically stable, and microbiologically safe propofol-loaded microemulsions.
  • To investigate the structural transformations of these microemulsions upon water dilution for improved drug delivery.

Main Methods:

  • Utilized advanced analytical techniques including SD-NMR, SAXS, cryo-TEM, DSC, electrical conductivity, and viscosity.
  • Characterized both empty and propofol-loaded microemulsion systems across varying water concentrations.

Main Results:

  • Propofol-loaded microemulsions form stable, water-dilutable systems, transitioning from reverse micelles to bicontinuous phases and finally to O/W nanodroplets.
  • Drug-surfactant interactions were confirmed, influencing nanodroplet size but not overall microemulsion behavior.
  • Water, ethanol, and propylene glycol are crucial for structure but do not directly interact with propofol.

Conclusions:

  • Developed stable, safe, and water-dilutable propofol microemulsions suitable for anesthesia.
  • Demonstrated the structural adaptability of these microemulsions, maintaining drug integrity during dilution.
  • These findings offer a promising advancement in anesthetic drug formulation and delivery.