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Related Concept Videos

Antifungal Agents01:15

Antifungal Agents

29
Amphotericin B is a broad-spectrum antifungal agent that exploits structural differences between fungal and mammalian cell membranes. Its amphipathic structure—featuring a hydrophobic polyene-lactone ring and a hydrophilic region containing mycosamine and carboxylic acid groups—enables selective binding to ergosterol, a sterol predominantly found in fungal plasma membranes. This selective interaction underlies the drug’s antifungal activity, although weak binding to...
29
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

305
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...
305
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

651
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...
651
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH01:21

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

4.1K
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...
4.1K
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

827
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...
827
Oral Drug Delivery Systems: Continuous-Release Systems01:26

Oral Drug Delivery Systems: Continuous-Release Systems

193
Continuous-release drug delivery systems offer a strategic approach to maintaining therapeutic drug levels over extended periods following oral administration. By modulating the release rate of active pharmaceutical ingredients, these systems minimize fluctuations in plasma concentrations, which enhances clinical efficacy and reduces the need for frequent dosing. Such characteristics make them particularly advantageous in managing chronic diseases where patient adherence and stable drug...
193

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Updated: Mar 25, 2026

Small-Scale Plasma Membrane Preparation for the Analysis of Candida albicans Cdr1-mGFPHis
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Posaconazole/hydroxypropyl-β-cyclodextrin host-guest system: Improving dissolution while maintaining antifungal

Peixiao Tang1, Xiaoli Ma1, Di Wu1

  • 1College of Chemical Engineering, Sichuan University, Chengdu 610065, China.

Carbohydrate Polymers
|February 27, 2016
PubMed
Summary

This study developed a posaconazole (POS) and hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex, significantly improving POS solubility and dissolution for better antifungal drug delivery.

Keywords:
Acetone (PubChem CID: 180)CharacterizationDissolutionHeavy water (PubChem CID: 24602)Hydroxypropyl-beta-cyclodextrin (PubChem CID: 14049689)Hydroxypropyl-β-cyclodextrinIn vitro anti-fungalInclusion complexMethanol (PubChem CID: 887)PosaconazolePosaconazole (PubChem CID: 468595)

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Supramolecular Chemistry

Background:

  • Posaconazole (POS) is a broad-spectrum antifungal agent with poor aqueous solubility, limiting its oral bioavailability.
  • Hydroxypropyl-β-cyclodextrin (HP-β-CD) is a cyclodextrin derivative known for its ability to form inclusion complexes with poorly soluble drugs, enhancing their physicochemical properties.

Purpose of the Study:

  • To prepare and characterize the inclusion complex of posaconazole (POS) with hydroxypropyl-β-cyclodextrin (HP-β-CD).
  • To evaluate the impact of complexation on the solubility, dissolution rate, and antifungal activity of posaconazole.

Main Methods:

  • Phase solubility studies to determine drug-solubilizer interactions, stoichiometry, and stability constants.
  • Characterization of the solid inclusion complex using Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), NMR spectroscopy, differential scanning calorimetry (DSC), and scanning electron microscopy (SEM).
  • Solubility and dissolution rate measurements compared to free POS.
  • Preliminary in vitro antifungal susceptibility testing.

Main Results:

  • Phase solubility studies confirmed drug-CD interaction and provided data on stoichiometry and stability.
  • Spectroscopic and analytical techniques (FTIR, PXRD, NMR, DSC, SEM) verified the formation of the HP-β-CD-POS inclusion complex.
  • The HP-β-CD-POS inclusion complex demonstrated an 82-fold increase in water solubility compared to free POS.
  • The complex exhibited a significantly higher dissolution rate, with approximately 90% of the drug dissolving within 10 minutes.
  • In vitro antifungal testing indicated that the complex retained potent antifungal activity.

Conclusions:

  • The hydroxypropyl-β-cyclodextrin complexation effectively enhances the aqueous solubility and dissolution rate of posaconazole.
  • The prepared inclusion complex maintains the antifungal efficacy of posaconazole.
  • HP-β-CD complexation represents a promising strategy for improving the oral delivery and therapeutic potential of posaconazole.