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Published on: October 10, 2016
[The complexation of prostaglandin E1 with hydroxylpropyl-beta-cyclodextrin in aqueous solution]
Fu-gen Gu1, Fu-de Cui, Yong-liang Gao
1Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
Prostaglandin E1 (PGE1) forms a 1:1 inclusion complex with hydroxylpropyl-beta-cyclodextrin (HP-beta-CD) in aqueous solutions, enhancing PGE1 solubility. This complexation occurs spontaneously, driven by favorable thermodynamics.
Area of Science:
- Pharmaceutical Sciences
- Physical Chemistry
Background:
- Prostaglandin E1 (PGE1) is a crucial lipid mediator with limited aqueous solubility.
- Hydroxylpropyl-beta-cyclodextrin (HP-beta-CD) is a widely used cyclodextrin derivative for drug solubilization.
Purpose of the Study:
- To investigate the complexation of PGE1 with HP-beta-CD in aqueous media.
- To determine the inclusion molar ratio and thermodynamic parameters of the PGE1-HP-beta-CD complex.
- To understand the mechanism of complex formation.
Main Methods:
- Phase solubility method
- UV absorption spectroscopy
- Circular dichroism spectroscopy
- Equimolar series method
- Thermodynamic analysis
Main Results:
- Phase solubility diagrams indicated a 1:1 molar ratio complex formation (AL-type).
- Spectroscopic methods confirmed the inclusion of PGE1's chromophore into the HP-beta-CD hydrophobic cavity.
- Thermodynamic data suggested spontaneous complexation with heat release and entropy decrease.
Conclusions:
- A 1:1 inclusion complex of PGE1 with HP-beta-CD is formed spontaneously, increasing PGE1 solubility.
- Optimal temperature and pH conditions likely enhance the complexation process.
- This complexation strategy offers a promising approach for improving PGE1 aqueous formulations.
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