Related Experiment Video
Updated: Feb 27, 2026
05:08
Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
Published on: September 20, 2017
17.8K
Viewing Molecular and Interface Interactions of Curcumin Amorphous Solid Dispersions for Comprehending Dissolution
Jing Li1, Xin Wang1, Chang Li1
1Wuya College of Innovation, Shenyang Pharmaceutical University , Shenyang 110016, China.
Molecular Pharmaceutics
|June 30, 2017
Summary
Investigating tautomeric curcumin amorphous solid dispersions (Cur ASDs) revealed that polymer interactions dictate curcumin
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Physical Chemistry
Background:
- Amorphous solid dispersions (ASDs) enhance drug solubility and bioavailability.
- Curcumin (Cur) exhibits poor aqueous solubility and stability.
- Understanding tautomeric forms and dissolution mechanisms of Cur ASDs is crucial for formulation development.
Purpose of the Study:
- To probe tautomeric curcumin (Cur) in amorphous solid dispersions (ASDs) formulated with various polymers.
- To elucidate the dissolution mechanisms of Cur ASDs based on molecular and interfacial interactions.
- To evaluate the role of polymers in improving Cur loading, dissolution, and supersaturation.
Main Methods:
- In situ Raman imaging and spectroscopy to analyze tautomeric forms.
- Molecular modeling to understand drug-polymer interactions.
- Contact angle measurements to assess wetting effects.
- Turbidimetry to evaluate polymer performance.
Main Results:
- Curcumin's tautomeric form (keto or enol) in ASDs depends on polymer interactions (e.g., keto in Cur-PEG, enol in Cur-PVP).
- Hydrogen bonding interactions were identified between Curcumin and polymers (PEG, HPMC, PVP, Eudragit EPO).
- Eudragit EPO-based ASDs showed an erosion dissolution pattern, superior to PVP-based ASDs with diffusion mechanisms.
- Wetting effects and contact angle profiles significantly influence dissolution behavior.
Conclusions:
- Polymer selection critically influences curcumin's tautomeric state and dissolution behavior in ASDs.
- Molecular and interfacial interactions govern the performance of Cur ASDs.
- Turbidimetry is an effective method for assessing polymer efficacy in ASD formulations.
- Elucidating tautomerism and dissolution mechanisms provides valuable insights for optimizing Cur ASDs.
Related Concept Videos
01:09Theories of Dissolution: The Danckwerts' Model and Interfacial Barrier Model
876
Various dissolution theories provide insight into the factors that influence the dissolution rate. Danckwerts' Model suggests that turbulence, rather than a stagnant layer, characterizes the dissolution medium at the solid-liquid interface. In this model, the agitated solvent contains macroscopic packets that move to the interface via eddy currents, facilitating the absorption and delivery of the drug to the bulk solution. The regular replenishment of solvent packets maintains the...
876
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
791
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...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
791
01:27Factors Influencing Drug Absorption: Drug Dissolution
1.4K
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...
1.4K
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
664
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
664
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
1.8K
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...
1.8K
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
624
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...
624