LIPOSOMAL NANODELIVERY SYSTEM FOR PROTEASOME
INHIBITOR ANTICANCER DRUG BORTEZOMIB
ALINA BUTU1, STELIANA RODINO1*, DIANA GOLEA1, MARIAN BUTU1, MONICA
BUTNARIU2, CONSTANTA NEGOESCU2, CRISTINA-ELENA DINU-PÎRVU3
1National Institute of Research and Development for Biological Sciences, Splaiul independentei 296, 060031, Bucharest,
Romania
2Banat’s University of Agricultural Sciences and Veterinary Medicine "Regele Mihai I al Romaniei" from Timisoara, Calea
Aradului 119, 300645, Timisoara, Romania
3“Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Physical and Colloidal Chemistry Department,
Traian Vuia 6, 020956, Bucharest, Romania
*corresponding author: steliana.rodino@yahoo.com
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Abstract:
Bortezomib is the first therapeutic agent designed to inhibit mainly the activity of the 26S proteasome. It is used for the
treatment of multiple myeloma. The objective of this study was to develop and optimize liposomal formulation of bortezomib
in order to improve the encapsulation efficiency. For evaluating the encapsulation efficiency it was investigated the effect of
two parameters: the drug/lipid molar ratio and the pH of the medium. The liposomal formulation of bortezomib was obtained
by mixing a solution of bortezomib with SUV liposomes (small unilamellar vesicle). A transmembrane pH gradient was
obtained by creating a difference of pH between internal medium of the liposomes and the external medium in which the
liposomes were suspended. When preparing the liposomes by using a pH gradient it was obtained an encapsulation efficiency
of 48 % for the molar ratio bortezomib:lipid 1:5.

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