PEG-Modified tert-Octylcalix[8]arenes as Drug Delivery Nanocarriers of Silibinin

Autor:	Hristo Penchev, Denitsa Momekova, Pavletta Shestakova, Stanislav Rangelov, Georgi Momekov, Desislava Budurova
Rok vydání:	2021
Předmět:	silibinin Chemistry Supramolecular chemistry calix[8]arenes inclusion complexes PEGylation cytotoxicity Pharmaceutical Science Silibinin Combinatorial chemistry Article RS1-441 chemistry.chemical_compound Pharmacy and materia medica PEG ratio Drug delivery Calixarene Nanocarriers Solubility
Zdroj:	Pharmaceutics, Vol 13, Iss 2025, p 2025 (2021) Pharmaceutics; Volume 13; Issue 12; Pages: 2025 Pharmaceutics
Popis:	The hepatoprotective properties of silibinin, as well its therapeutic potential as an anticancer and chemo-preventive agent, have failed to progress towards clinical development and commercialization due to this material’s unfavorable pharmacokinetics and physicochemical properties, low aqueous solubility, and chemical instability. The present contribution is focused on the feasibility of using PEGylated calixarene, in particular polyoxyethylene-derivatized tert-octylcalix[8]arene, to prepare various platforms for the delivery of silibinin, such as inclusion complexes and supramolecular aggregates thereof. The inclusion complex is characterized by various instrumental methods. At concentrations exceeding the critical micellization concentration of PEGylated calixarene, the tremendous solubility increment of silibinin is attributed to the additional solubilization and hydrophobic non-covalent interactions of the drug with supramolecular aggregates. PEG-modified tert-octylcalix[8]arenes, used as drug delivery carriers for silibinin, were additionally investigated for cytotoxicity against human tumor cell lines.
Databáze:	OpenAIRE
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