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Poor solubility of crocetin has limited its use as a potential chemotherapeutic agent. In this study, a crocetin nanocarrier was formulated based on poly(lactic-co-glycolic acid) (PLGA) polymer. The effect of preparation conditions on the size and entrap efficiency of PLGA nanoparticles (NPs) via single emulsion/solvent evaporation method was evaluated. Cytotoxicity of crocetin and crocetin-encapsulated PLGA NPs was assayed in MCF-7 cell line. In PLGA formulations, the optimal condition was found to be 5% polyvinyl alcohol (PVA), crocetin:polymer ratio 1:20 and dichloromethane as organic solvent. Obtained results demonstrated that the encapsulation of crocetin in PLGA significantly increased the cytotoxicity of this compound.

Objective(s): The current study reports investigation of codelivery by PLGA nanoparticles (NPs) loaded with crocetin (Cro), a natural carotenoid dicarboxylicHYPERLINK "http://en.wikipedia.org/wiki/Carboxylic_acid" acid that is found in the crocus flower, and Doxorubicin (DOX). Materials and Methods: Double emulsion/solvent evaporation method was used for preparation of PLGA nanoparticles containing Dox and Cro. Characterizations of prepared NPs were investigated by atomic force microscopy (AFM) and dynamic light scattering analysis. In vitro Cytotoxicity of DOX and Cro loaded PLGA NPs (PLGA-DOX-Cro) on MCF-7 cell line was evaluated using MTT test. Flow cytometry experiments were implemented to distinguish cells undergoing apoptosis from those undergoing necrosis. Furthermore the expression of caspase 3 was examined by western blot analysis. Results: The prepared formulations had size of 150- 300 nm. Furthermore, PLGA-DOX-Cro nanoparticles inhibited MCF-7 tumor cells growth more efficiently than either DOX or Cro alone at the same concentrations, as quantified by MTT assay and flow cytometry. Studies on cellular uptake of DOX-Cro-NPs demonstrated that NPs were effectively taken up by MCF-7 tumor cells. Conclusion: This study suggested that DOX-Cro-NPs may have promising applications in breast cancer therapy. [ABSTRACT FROM AUTHOR]