Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	Curcumin loaded pH-sensitive hybrid lipid/block copolymer nanosized drug delivery systems
Δημιουργός/Συγγραφέας:	Jelezova I. Drakalska E. Momekova D. Shalimova N. Momekov G. Konstantinov S. Rangelov S. [EL] Πίσπας, Στέργιος[EN] Pispas, Stergios
Εκδότης:	Elsevier
Ημερομηνία:	2015
Γλώσσα:	Αγγλικά
ISSN:	0928-0987
DOI:	10.1016/j.ejps.2015.07.005
Άλλο:	PubMed ID: 26159739
Περίληψη:	Curcumin is a perspective drug candidate with pleiotropic antineoplastic activity, whose exceptionally low aqueous solubility and poor pharmacokinetic properties have hampered its development beyond the preclinical level. A possible approach to overcome these limitations is the encapsulation of curcumin into nano-carriers, incl. liposomes. The present contribution is focused on feasibility of using hybrid pH-sensitive liposomes, whereby curcumin is entrapped as a free drug and as a water soluble inclusion complex with PEGylated tert-butylcalix[4]arene, which allows the drug to occupy both the phospholipid membranes and the aqueous core of liposomes. The inclusion complexes were encapsulated in dipalmithoylphosphathydilcholine:cholesterol liposomes, whose membranes were grafted with a poly(isoprene-b-acrylic acid) diblock copolymer to confer pH-sensitivity. The liposomes were characterized by DLS, ζ-potential measurements, cryo-TEM, curcumin encapsulation efficacy, loading capacity, and in vitro release as a function of pH. Free and formulated curcumin were further investigated for cytotoxicity, apoptosis-induction and caspase-8, and 9 activation in chemosensitive HL-60 and its resistant sublines HL-60/Dox and HL-60/CDDP. Formulated curcumin was superior cytotoxic and apoptogenic agent vs. the free drug. The mechanistic assay demonstrated that the potent proapoptotic effects of pH-sensitive liposomal curcumin presumably mediated via recruitment of both extrinsic and intrinsic apoptotic pathways in both HL-60 and HL-60/CDDP cells.
Τίτλος πηγής δημοσίευσης:	European Journal of Pharmaceutical Sciences
Τόμος/Κεφάλαιο:	78
Σελίδες:	67-78
Θεματική Κατηγορία:	[EL] Φυσική και θεωρητική χημεία[EN] Physical and theoretical chemistry
Λέξεις-Κλειδιά:	Apoptosis Curcumin Inclusion complex pH-sensitive hybrid liposomes Poly(isoprene-b-acrylic acid) Polyoxyethylated tert-buthylcalix[4]arenes
Αξιολόγηση από ομότιμους (peer reviewed):	Ναι
Κάτοχος πνευματικών δικαιωμάτων:	© 2015 Elsevier B.V. All rights reserved.
Όροι και προϋποθέσεις δικαιωμάτων:	All Open Access, Green
Σημειώσεις:	B01/25 2012 Financial support from DFNI ( B01/25 2012 ) is gratefully acknowledged. We are grateful to Dr. Jonny Eriksson for performing the cryo-TEM analysis.
Εμφανίζεται στις συλλογές:	Ινστιτούτο Θεωρητικής και Φυσικής Χημείας (ΙΘΦΧ) - Επιστημονικό έργο