Synthesis and characterization of curcumin loaded polymer/lipid based nanoparticles and evaluation of their antitumor effects on MCF-7 cells Sathish Sundar Dhilip Kumar a , Ayyavu Mahesh b , Surianarayanan Mahadevan a, ⁎, Asit Baran Mandal a a Thermochemical Lab, Chemical Engineering Department, Central Leather Research Institute, Chennai 600 020, India b School of Biological Sciences, Madurai Kamaraj University, Madurai 625 021, India abstract article info Article history: Received 9 October 2013 Received in revised form 7 January 2014 Accepted 10 January 2014 Available online 16 January 2014 Keywords: Polyhydroxyethyl methacrylate Stearic acid Curcumin Drug delivery system Polymeric lipid nanoparticle Background: Hybrid materials are synthesized using hydrophilic polymer and lipids which ensure their long term systemic circulation through intravenous administration and enhance loading of hydrophobic drugs. The purpose of this study is to prepare, characterize and evaluate the in vitro efficacy of curcumin loaded poly- hydroxyethyl methacrylate/stearic acid nanoparticles in MCF-7. Methods: C-PSA-NPs, prepared using the emulsification–solvent evaporation method were characterized by dynamic laser scattering, SEM, AFM, FT-IR, X-ray diffraction, and TGA. The in vitro release behavior was observed in PBS pH 7.4, the anticancer potential was analyzed by MTT assay, cell cycle and apoptosis studies were performed through flow cytometry. C-PSA-NPs drug localization and cancer cell morphological changes were analyzed in MCF-7 cell line. Results: C-PSA-NPs exhibited the mean particle size in the range of 184 nm with no aggregation. The surface charge of the material was around -29.3 mV. Thermal studies (TGA) and surface chemistry studies (FT-IR, XRD) showed the existence of drug curcumin in C-PSA-NPs. The MTT assay indicated higher anticancer proper- ties and flow cytometry studies revealed that there were better apoptotic activity and maximum localization of C-PSA-NPs than curcumin. Conclusions: Polymer lipid based drug delivery appeared as one of the advancements in drug delivery systems. Through the present study, a novel polymer lipid based nanocarrier delivery system loaded with curcumin was demonstrated as an effective and potential alternative method for tumor treatment in MCF-7 cell line. General significance: C-PSA-NPs exhibited potent anticancer activity in MCF-7 cell line and it indicates that C-PSA- NPs are a suitable carrier for curcumin. © 2014 Elsevier B.V. All rights reserved. 1. Introduction Nanotechnology is the term commonly used now to refer to the fabrication of new materials such as “solid colloidal particles” with nano- scale dimensions. In the field of drug delivery there has been substantial interest in developing nanoparticles as effective drug carriers, wherein the drug or biologically active material is entrapped, encapsulated, adsorbed or attached [1,2]. Polyhydroxyethyl methacrylate (PHEMA), a hydrophilic polymer is widely used as a drug carrier molecule [3,4]. The hydrogels are used in biomedical applications because of their distinctive biocompatibility like absence of toxicity and compatibility with blood [5–8]. Some of its applications include eye contact lenses, scaffold mate- rials in tissue engineering, artificial skin, and tube-shaped structure grafts [9–12]. Curcumin (Diferuloylmethane), a low molecular weight, lipophilic, natural yellow polyphenolic compound of Indian spice turmeric (Curcuma longa), has the chemical structure of (1,7-bis(4-hydroxy-3- methoxyphenyl)-1,6-heptadiene-3,5-dione). It has been used in tradi- tional medicine for many centuries in India and China [13–18]. It possesses a wide range of biological and pharmacological properties, and is used for the treatment of neurodegenerative, cardiovascular, pulmonary, autoimmune and neoplastic diseases [14], biliary disorders, hepatic disorders, diabetic wounds, rheumatism [16], and skin cancer [19] and it is an antioxidant, antiviral, and anticancer [20,21] showing anti-inflammatory drug properties [13,22,23]. Though curcumin has good therapeutic efficacy (topical & oral), the problem related to curcumin is its low solubility in aqueous solution, degradation at alka- line pH, photodegradation and its poor oral bioavailability [16,24,25]. Carrier mediated curcumin delivery is the potential way to overcome these problems without affecting its efficacy [26]. Recent research has concentrated on delivering curcumin [27] through different carrier mol- ecules such as polymeric micelles, polymeric nanoparticles, liposomes, lipid based nanoparticles, hydrophilic polymers or hydrogels, and cyclodextrin. Stearic acid (SA), an endogenous long-chain fatty acid is biocompati- ble with low toxicity. It is biocompatible with human tissues and neutral with relevance to physiological fluids. Lipids in combination with a Biochimica et Biophysica Acta 1840 (2014) 1913–1922 ⁎ Corresponding author at: Thermochemical Lab, Chemical Engineering Department, Central Leather Research Institute (CLRI), Adyar, Chennai 20, Tamilnadu, India. Tel.: +91 44 24437207; fax: +91 44 24911589. E-mail address: msuri1@vsnl.com (S. Mahadevan). 0304-4165/$ – see front matter © 2014 Elsevier B.V. All rights reserved. http://dx.doi.org/10.1016/j.bbagen.2014.01.016 Contents lists available at ScienceDirect Biochimica et Biophysica Acta journal homepage: www.elsevier.com/locate/bbagen