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Solubilization of cyclosporin A
1Department of Pharmaceutical Sciences, College of Pharmacy, University of Arizona, Tucson, AZ 85721, USA. ran@pharmacy.arizona.edu
AAPS Pharmscitech
|January 20, 2004
Summary
Surfactants like Tween 20, Tween 80, and Cremophor EL significantly enhanced cyclosporin A (CsA) solubility by 60-160 fold. Cyclodextrins also improved solubility, with alpha-cyclodextrin being more effective than hydroxypropyl-beta-cyclodextrin.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Physical Chemistry
Background:
- Cyclosporin A (CsA) is a neutral undecapeptide with poor aqueous solubility, limiting its therapeutic applications.
- Effective solubilization strategies are crucial for improving CsA bioavailability and formulation development.
Purpose of the Study:
- To investigate and compare the efficacy of cosolvency, micellization, and complexation in enhancing the aqueous solubility of cyclosporin A (CsA).
Main Methods:
- Evaluated various cosolvents (e.g., ethanol, glycerin), surfactants (Tween 20, Tween 80, Cremophor EL), and cyclodextrins (alphaCD, HPbetaCD) as CsA solubilizing agents.
- Quantified the increase in CsA solubility using different formulation approaches.
Main Results:
- Surfactants demonstrated significant CsA solubilization, increasing solubility by 60-160 fold at 20% concentrations.
- Cyclodextrins enhanced CsA solubility, with alpha-cyclodextrin showing greater efficacy than HPbetaCD.
- Cosolvents provided less significant increases in CsA solubility than anticipated based on its LOGP value.
Conclusions:
- Micellization using specific surfactants is a highly effective method for solubilizing CsA.
- Cyclodextrin complexation offers a viable alternative, with alphaCD being a preferred agent over HPbetaCD for CsA.
- Cosolvency is less effective for CsA solubilization compared to micellization and complexation.