Hybrid liposomal PEGylated calix[4]arene systems as drug delivery platforms for curcumin

Drakalska, Elena and Momekova, Denitsa and Manolova, Yana and Budurova, Desislava and Momekov, Georgi and Genova, Margarita and Antonov, Liudmil and Lambov, Nikolay and Rangelov, Stanislav (2014) Hybrid liposomal PEGylated calix[4]arene systems as drug delivery platforms for curcumin. International Journal of Pharmaceutics, 472. pp. 165-174.

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The tremendous therapeutic potential of curcumin as a chemopreventive, antineoplastic and chemosensitizing agent has failed to progress towards clinical development and commercialization due to its unfavorable physicochemical properties, low aqueous solubility, chemical instability, and pharmacokinetics. The present contribution is focused on the feasibility of using PEGylated calixarene, in particular polyoxyethylene-derivatized tert-butylcalix[4]arene, to prepare various platforms for delivery of curcumin such as inclusion complex, supramolecular aggregates, and hybrid liposomal systems. The inclusion complex is characterized by UV–vis and FT-IR spectroscopy as well as thermal gravimetrical analysis and differential scanning calorimetry. At concentrations exceeding the critical micellization concentration of PEGylated calixarene, the tremendous solubility enhancement of curcumin is attributed to additional solubilization and hydrophobic non-covalent interactions of the drug with supramolecular aggregates. A hybrid liposomal system is created via encapsulation of the inclusion complex in dipalmitoylphosphatidylcholine:cholesterol liposomes. Bare and liposomal curcumin:BEC-X inclusion complexes, as well as free curcumin were additionally investigated for cytotoxicity and apoptogenic activity against human tumor cell lines.

Item Type: Article
Subjects: Medical and Health Sciences > Other medical sciences
Divisions: Faculty of Medical Science
Depositing User: Elena Drakalska
Date Deposited: 30 Jun 2014 09:43
Last Modified: 30 Jun 2014 09:43
URI: https://eprints.ugd.edu.mk/id/eprint/10273

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