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Improvement of steroid biotransformation with hydroxypropyl-beta-cyclodextrin induced complexation
Liting Zhang1, Min Wang, Yanbing Shen
1Key Laboratory of Industrial Microbiology, Ministry of Education, College of Biotechnology, Tianjin University of Science and Technology, Tianjin, People's Republic of China.
Applied Biochemistry and Biotechnology
|February 4, 2009
Summary
Hydroxypropyl-beta-cyclodextrin (HP-beta-CD) significantly enhances cortisone acetate solubility and dissolution rate. Unlike organic cosolvents, HP-beta-CD improves enzymatic stability for biotransformation applications.
Area of Science:
- Biotechnology
- Pharmaceutical Sciences
- Chemical Engineering
Background:
- Cyclodextrins and their derivatives are known to improve the biotransformation of hydrophobic compounds.
- Cortisone acetate is a hydrophobic drug with limited water solubility, posing challenges for pharmaceutical formulation and biotransformation.
Purpose of the Study:
- To evaluate the efficacy of hydroxypropyl-beta-cyclodextrin (HP-beta-CD) in enhancing the solubility and dissolution rate of cortisone acetate.
- To assess the impact of HP-beta-CD on the enzymatic stability and activity of Delta(1)-dehydrogenase from Arthrobacter simplex TCCC 11037 compared to organic cosolvents.
Main Methods:
- Solubility and dissolution rate studies of cortisone acetate in the presence of varying concentrations of HP-beta-CD at 32°C.
- Enzymatic stability assays of Delta(1)-dehydrogenase incubated with HP-beta-CD, dimethylformamide (DMF), and ethanol.
- Determination of inactivation constants and inactivation energy (Ea) for the enzyme under different conditions.
Main Results:
- HP-beta-CD dramatically increased cortisone acetate water solubility from 0.039 to 7.382 g L(-1), outperforming DMF and ethanol.
- The dissolution rate of cortisone acetate was significantly enhanced by HP-beta-CD.
- Enzyme stability was not affected by HP-beta-CD, whereas DMF and ethanol negatively impacted it, with inactivation constants of 1.216, 4.541, and 5.832, respectively.
- Inactivation energy (Ea) followed the order HP-beta-CD (55.1 kJ mol(-1)) > ethanol (39.9 kJ mol(-1)) > DMF (37.1 kJ mol(-1)).
Conclusions:
- HP-beta-CD is a superior solubilizing agent for cortisone acetate compared to common organic cosolvents.
- HP-beta-CD effectively enhances cortisone acetate solubility and dissolution without compromising the stability of key biotransformation enzymes like Delta(1)-dehydrogenase.
- These findings highlight the potential of HP-beta-CD in improving hydrophobic drug formulation and enzymatic biotransformation processes.
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