Effect of Cyclodextrin Complexation on the Aqueous Solubility and Solubility/Dose Ratio of Praziquantel |
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Authors: | Stratos Maragos Helen Archontaki Panos Macheras Georgia Valsami |
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Institution: | (1) Laboratory of Biopharmaceutics and Pharmacokinetics, Faculty of Pharmacy, National & Kapodistrian University of Athens, Athens, 15771, Greece;(2) Laboratory of Analytical Chemistry, Department of Chemistry, National & Kapodistrian University of Athens, Athens, 15771, Greece; |
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Abstract: | Praziquantel (PZQ), the primary drug of choice in the treatment of schistosomiasis, is a highly lipophilic drug that possesses
high permeability and low aqueous solubility and is, therefore, classified as a Class II drug according to the Biopharmaceutics
Classification System (BCS). In this work, β-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) were used in order
to determine whether increasing the aqueous solubility of a drug by complexation with CDs, a BCS-Class II compound like PZQ
could behave as BCS-Class I (highly soluble/highly permeable) drug. Phase solubility and the kneading and lyophilization techniques
were used for inclusion complex preparation; solubility was determined by UV spectroscopy. The ability of the water soluble
polymer polyvinylpyrolidone (PVP) to increase the complexation and solubilization efficiency of β-CD and HP-β-CD for PZQ was
examined. Results showed significant improvement of PZQ solubility in the presence of both cyclodextrins but no additional
effect in the presence of PVP. The solubility/dose ratios values of PZQ-cyclodextrin complexes calculated considering the
low (150 mg) and the high dose (600 mg) of PZQ, used in practice, indicate that PZQ complexation with CDs may result in drug
dosage forms that would behave as a BCS-Class I depending on the administered dose. |
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