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Updated: May 26, 2026
10:22
In Vitro and In Vivo Approaches to Determine Intestinal Epithelial Cell Permeability
Published on: October 19, 2018
Preparation, characterization, and in vitro intestinal permeability evaluation of
Jadel M Kratz1, Marina R Teixeira, Karine Ferronato
1Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina-UFSC, Florianópolis, SC, Brazil.
AAPS Pharmscitech
|December 14, 2011
Summary
Complexing thalidomide with hydroxypropyl-β-cyclodextrin significantly enhances its aqueous solubility and dissolution. This strategy improves gastrointestinal absorption of thalidomide, a drug with anti-inflammatory and antineoplastic properties.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Medicinal Chemistry
Background:
- Thalidomide exhibits anti-inflammatory, immunomodulatory, and antineoplastic properties, leading to renewed clinical interest.
- Poor aqueous solubility limits thalidomide's therapeutic efficacy and bioavailability.
- Cyclodextrin complexation is a known strategy to improve drug solubility and delivery.
Purpose of the Study:
- To investigate the complexation of thalidomide with hydroxypropyl-β-cyclodextrin (HP-β-CD).
- To enhance the aqueous solubility and in vitro dissolution of thalidomide.
- To evaluate the impact of complexation on thalidomide's physicochemical properties and intestinal permeability.
Main Methods:
- Thalidomide-HP-β-CD complexes were prepared using the kneading method.
- Complex formation was characterized by differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), and scanning electron microscopy (SEM).
- In vitro dissolution studies and Caco-2 cell permeability assays were performed.
Main Results:
- Complexation significantly increased thalidomide's aqueous solubility and in vitro dissolution rate.
- Physicochemical analyses indicated reduced crystallinity of thalidomide within the complexes.
- Thalidomide dissociated from the complexes and exhibited high intestinal permeability across Caco-2 cells, comparable to the free drug.
Conclusions:
- Thalidomide-HP-β-CD complexes offer a promising approach to overcome the poor aqueous solubility of thalidomide.
- The enhanced solubility and permeability suggest improved gastrointestinal absorption of thalidomide.
- This formulation strategy holds potential for optimizing thalidomide-based therapies.
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