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. 2013 Fall;12(4):623-34.

Anticancer Activity of Nanoparticles Based on PLGA and its Co-polymer: In-vitro Evaluation

Issa Amjadi, Mohammad Rabiee, Motahare-Sadat Hosseini  1
Affiliations

Anticancer Activity of Nanoparticles Based on PLGA and its Co-polymer: In-vitro Evaluation

Issa Amjadi et al. Iran J Pharm Res. 2013 Fall.

Abstract

Attempts have been made to prepare nanoparticles based on poly(lactic-co-glycolic acid) (PLGA) and doxorubicin. Biological evaluation and physio-chemical characterizations were performed to elucidate the effects of initial drug loading and polymer composition on nanoparticle properties and its antitumor activity. PLGA nanoparticles were formulated by sonication method. Lactide/glycolide ratio and doxorubicin amounts have been tailored. Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) were employed to identify the presence of doxorubicin within nanospheres. The in vitro release studies were performed to determine the initial ant net release rates over 24 h and 20 days, respectively. Furthermore, cytotoxicity assay was measured to evaluate therapeutic potency of doxorubicin-loaded nanoparticles. Spectroscopy and thermal results showed that doxorubicin was loaded into the particles successfully. It was observed that lactide/glycolide content of PLGA nanoparticles containing doxorubicin has more prominent role in tuning particle characteristics. Doxorubicin release profiles from PLGA 75 nanospheres demonstrated that the cumulative release rate increased slightly and higher initial burst was detected in comparison to PLGA 50 nanoparticles. MTT data revealed doxorubicin induced antitumor activity was enhanced by encapsulation process, and increasing drug loading and glycolide portion. The results led to the conclusion that by controlling the drug loading and the polymer hydrophilicity, we can adjust the drug targeting and blood clearance, which may play a more prominent role for application in chemotherapy.

Keywords: Antitumor activity; Doxorubicin; Nanoparticle; Poly(lactic-co-glycolic acid); Sustained release.

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Figures

Figure 1
Figure 1
Absorption and emission spectra of Dox
Figure 2
Figure 2
FTIR-transmission spectrum of Dox loaded-PLGA NPs
Figure 3
Figure 3
DSC thermogram of (a) empty NPs and (b) Dox-loaded NPs
Figure 4
Figure 4
Effect of drug loading on the size of PLGA NPs
Figure 5
Figure 5
Effect of drug loading on the PDI of Dox- loaded PLGA NPs
Figure 6
Figure 6
Effect of polymer characteristics on the surface potential
Figure 7
Figure 7
SEM micrographs of (a) Dox-loaded PLGA 50:50 and (b) Dox loaded-PLGA 75:25
Figure 8
Figure 8
In-vitro release of Dox-loaded PLGA 50:50 NPs (blue) and Dox-loaded PLGA 75:25 NPs (red) in phosphate buffer pH 7.4
Figure 9
Figure 9
Viability of L929 cells according to MTT test with different concentrations of Dox solutions.
Figure 10
Figure 10
Proliferation percent of cells treated by Dox and NPs at twice concentration of the LC50.
Figure 11
Figure 11
Cellular response to the different amounts of drug loading and PLGA compositions
See this image and copyright information in PMC

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