TY  - JOUR
AU  - Ignjatović, Nenad
AU  - Penov-Gasi, Katarina M.
AU  - Wu, Victoria M.
AU  - Ajduković, Jovana J.
AU  - Kojić, Vesna V.
AU  - Vasiljević-Radović, Dana
AU  - Kuzmanovic, Maja
AU  - Uskokovicć, Vuk
AU  - Uskoković, Dragan P.
PY  - 2016
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/1996
AB  - In an earlier study we demonstrated that hydroxyapatite nanoparticles coated with chitosan-poly(D,L)-lactide-co-glycolide (HAp/Ch-PLGA) target lungs following their intravenous injection into mice. In this study we utilize an emulsification process and freeze drying to load the composite HAp/Ch-PLGA particles with 17 beta-hydroxy-17 alpha-picolyl-androst-5-en-3 beta-yl-acetate (A), a chemotherapeutic derivative of androstane and a novel compound with a selective anticancer activity against lung cancer cells. H-1 NMR and C-13 NMR techniques confirmed the intact structure of the derivative A following its entrapment within HAp/Ch-PLGA particles. The thermogravimetric and differential thermal analyses coupled with mass spectrometry were used to assess the thermal degradation products and properties of A-loaded HAp/Ch-PLGA. The loading efficiency, as indicated by the comparison of enthalpies of phase transitions in pure A and A-loaded HAp/Ch-PLGA, equaled 7.47 wt.%. The release of A from HAp/Ch-PLGA was sustained, neither exhibiting a burst release nor plateauing after three weeks. Atomic force microscopy and particle size distribution analyses were used to confirm that the particles were spherical with a uniform size distribution of d(50) = 168 nm. In vitro cytotoxicity testing of A-loaded HAp/Ch-PLGA using MTT and trypan blue dye exclusion assays demonstrated that the particles were cytotoxic to the A549 human lung carcinoma cell line (46 +/- 2%), while simultaneously preserving high viability (83 +/- 3%) of regular MRC5 human lung fibroblasts and causing no harm to primary mouse lung fibroblasts. In conclusion, composite A-loaded HAp/Ch-PLGA particles could be seen as promising drug delivery platforms for selective cancer therapies, targeting malignant cells for destruction, while having a significantly lesser cytotoxic effect on the healthy cells.
PB  - Elsevier
T2  - Colloids and Surfaces B-Biointerfaces
T1  - Selective anticancer activity of hydroxyapatite/chitosan-poly(D,L)-lactide-co-glycolide particles loaded with an androstane-based cancer inhibitor
VL  - 148
SP  - 629
EP  - 639
DO  - 10.1016/j.colsurfb.2016.09.041
ER  - 

@article{
author = "Ignjatović, Nenad and Penov-Gasi, Katarina M. and Wu, Victoria M. and Ajduković, Jovana J. and Kojić, Vesna V. and Vasiljević-Radović, Dana and Kuzmanovic, Maja and Uskokovicć, Vuk and Uskoković, Dragan P.",
year = "2016",
abstract = "In an earlier study we demonstrated that hydroxyapatite nanoparticles coated with chitosan-poly(D,L)-lactide-co-glycolide (HAp/Ch-PLGA) target lungs following their intravenous injection into mice. In this study we utilize an emulsification process and freeze drying to load the composite HAp/Ch-PLGA particles with 17 beta-hydroxy-17 alpha-picolyl-androst-5-en-3 beta-yl-acetate (A), a chemotherapeutic derivative of androstane and a novel compound with a selective anticancer activity against lung cancer cells. H-1 NMR and C-13 NMR techniques confirmed the intact structure of the derivative A following its entrapment within HAp/Ch-PLGA particles. The thermogravimetric and differential thermal analyses coupled with mass spectrometry were used to assess the thermal degradation products and properties of A-loaded HAp/Ch-PLGA. The loading efficiency, as indicated by the comparison of enthalpies of phase transitions in pure A and A-loaded HAp/Ch-PLGA, equaled 7.47 wt.%. The release of A from HAp/Ch-PLGA was sustained, neither exhibiting a burst release nor plateauing after three weeks. Atomic force microscopy and particle size distribution analyses were used to confirm that the particles were spherical with a uniform size distribution of d(50) = 168 nm. In vitro cytotoxicity testing of A-loaded HAp/Ch-PLGA using MTT and trypan blue dye exclusion assays demonstrated that the particles were cytotoxic to the A549 human lung carcinoma cell line (46 +/- 2%), while simultaneously preserving high viability (83 +/- 3%) of regular MRC5 human lung fibroblasts and causing no harm to primary mouse lung fibroblasts. In conclusion, composite A-loaded HAp/Ch-PLGA particles could be seen as promising drug delivery platforms for selective cancer therapies, targeting malignant cells for destruction, while having a significantly lesser cytotoxic effect on the healthy cells.",
publisher = "Elsevier",
journal = "Colloids and Surfaces B-Biointerfaces",
title = "Selective anticancer activity of hydroxyapatite/chitosan-poly(D,L)-lactide-co-glycolide particles loaded with an androstane-based cancer inhibitor",
volume = "148",
pages = "629-639",
doi = "10.1016/j.colsurfb.2016.09.041"
}

Ignjatović, N., Penov-Gasi, K. M., Wu, V. M., Ajduković, J. J., Kojić, V. V., Vasiljević-Radović, D., Kuzmanovic, M., Uskokovicć, V.,& Uskoković, D. P.. (2016). Selective anticancer activity of hydroxyapatite/chitosan-poly(D,L)-lactide-co-glycolide particles loaded with an androstane-based cancer inhibitor. in Colloids and Surfaces B-Biointerfaces
Elsevier., 148, 629-639.
https://doi.org/10.1016/j.colsurfb.2016.09.041

Ignjatović N, Penov-Gasi KM, Wu VM, Ajduković JJ, Kojić VV, Vasiljević-Radović D, Kuzmanovic M, Uskokovicć V, Uskoković DP. Selective anticancer activity of hydroxyapatite/chitosan-poly(D,L)-lactide-co-glycolide particles loaded with an androstane-based cancer inhibitor. in Colloids and Surfaces B-Biointerfaces. 2016;148:629-639.
doi:10.1016/j.colsurfb.2016.09.041 .

Ignjatović, Nenad, Penov-Gasi, Katarina M., Wu, Victoria M., Ajduković, Jovana J., Kojić, Vesna V., Vasiljević-Radović, Dana, Kuzmanovic, Maja, Uskokovicć, Vuk, Uskoković, Dragan P., "Selective anticancer activity of hydroxyapatite/chitosan-poly(D,L)-lactide-co-glycolide particles loaded with an androstane-based cancer inhibitor" in Colloids and Surfaces B-Biointerfaces, 148 (2016):629-639,
https://doi.org/10.1016/j.colsurfb.2016.09.041 . .