Author/Authors :
Abedi Gaballu, Fereydoon Immounology Research Center - Tabriz University of Medical Sciences, Tabriz, Iran , Abbaspour Ravasjani, Soheil Drug Applied Research Center - Tabriz University of Medical Sciences, Tabriz, Iran , Mansoori, Behzad Immounology Research Center - Tabriz University of Medical Sciences, Tabriz, Iran , Yekta, Reza Department of Biology - Faculty of Natural Sciences - University of Tabriz, Tabriz, Iran , Hamishehkar, Hamed Drug Applied Research Center - Tabriz University of Medical Sciences, Tabriz, Iran , Mohammadi, Ali Immounology Research Center - Tabriz University of Medical Sciences, Tabriz, Iran , Dehghan, Gholamreza Department of Biology - Faculty of Natural Sciences - University of Tabriz, Tabriz, Iran , Shokouhi, Behrooz Department of Pathology - Tabriz University of Medical Sciences, Tabriz, Iran , Ghahremani Dehbokri, Shaho Immounology Research Center - Tabriz University of Medical Sciences, Tabriz, Iran , Baradaran, Behzad Immounology Research Center - Tabriz University of Medical Sciences, Tabriz, Iran
Abstract :
Erlotinib (ELT) as a small molecule with poor solubility, poor bioavailability, and
instability in gastrointestinal environment, has been considered as a therapeutic agent for Non-
Small-Cell Lung Cancer (NSCLC) therapy through oral administration. In the present study,
ELT-liposome and ELT-NLCs were successfully prepared and characterized by assessment
of the particle size, zeta potential (ZP), polydispersity index (PDI), encapsulation efficiency
(EE), and drug loading (DL). DAPI staining and Flow cytometry techniques were employed to
probe anticancer activities of the optimal formulations. The obtained results indicated that the
average size of optimized ELT-NLCs was 109 ± 2 nm, while the optimal formulation of ELTliposome
was 130 ± 4 nm. In addition, the values of EE, DL, and cellular uptake were higher in
ELT-NLCs than ELT-liposome. Moreover, the stability of ELT-NLCs and ELT-liposome were
not significantly changed (P > 0.05) within storage time. The results of anti-cancer assessment
indicated that ELT-NLCs caused more cell viability reduction than ELT-liposome and free
ELT. According to the Flow cytometry and DAPI staining results, the exposed A549 cells with
ELT-NLCs had more rates of apoptosis than ELT-liposome. The obtained data from this study
clearly showed that ELT-NLCs had better anti-cancer activity than ELT-liposome, which may
be related to the effective nano particle size, PDI, EE, and DL of ELT-NLCs.
Keywords :
A549 cells , NLCs , Erlotinib , Liposome