FA-loaded lipid drug delivery systems: preparation, characterization and biological studies.

The main purpose of this research was to prepare and to characterize ferulic acid-loaded nanostructured lipid carrier (FA-NLC) to evaluate the cytotoxic effect on human glioblastoma cancer U87MG cells. First of all, the influence of different materials on mean size and homogeneity of NLC prepared by a low energy organic solvent-free method was investigated. Technological characterization (encapsulation efficiency, mean particle size, homogeneity and in vitro release profile) was performed on the selected NLC in comparison to others lipid carriers, nanoemulsion and SLN. Furthermore, the thermal behavior of NLC and SLN was investigated using Differential Scanning Calorimetry (DSC) in order to evaluate their structure. Biological studies (MTT bioassay and caspase-3 cleavage) on the selected NLC showed no cytotoxic effects of the unloaded tested NLC. Besides, the effectiveness of FA-loaded NLC was higher compared to the free drug. Cells treated with FA or FA-loaded NLC showed a greater effect compared to idebenone (IDE) or IDE-loaded NLC, respectively. These results strongly support that FA-loaded NLC could be potentially used for the treatment of glioblastoma.

[1]  S. Karthikeyan,et al.  Radiosensitizing effect of ferulic acid on human cervical carcinoma cells in vitro. , 2011, Toxicology in vitro : an international journal published in association with BIBRA.

[2]  R. Bhandari,et al.  Potential of solid lipid nanoparticles in brain targeting. , 2008, Journal of controlled release : official journal of the Controlled Release Society.

[3]  D. Truong,et al.  Idebenone Induces Apoptotic Cell Death in the Human Dopaminergic Neuroblastoma SHSY-5Y Cells , 2011, Neurotoxicity Research.

[4]  R. Acquaviva,et al.  Technological and Biological Characterization of Idebenone-Loaded Solid Lipid Nanoparticles Prepared by a Modified Solvent Injection Technique , 2006 .

[5]  Fernanda Borges,et al.  Lipophilic caffeic and ferulic acid derivatives presenting cytotoxicity against human breast cancer cells. , 2011, Chemical research in toxicology.

[6]  J. Kasbohm,et al.  Crystallographic investigation of cetylpalmitate solid lipid nanoparticles. , 2000, International journal of pharmaceutics.

[7]  J. Benoit,et al.  Nano-emulsions and nanocapsules by the PIT method: an investigation on the role of the temperature cycling on the emulsion phase inversion. , 2007, International journal of pharmaceutics.

[8]  M. Gulisano,et al.  Lyoprotected nanosphere formulations for paclitaxel controlled delivery. , 2006, Journal of nanoscience and nanotechnology.

[9]  V. Shah,et al.  Determination of in vitro drug release from hydrocortisone creams , 1989 .

[10]  R. Gannu,et al.  Formulation and in vitro characterization of domperidone loaded solid lipid nanoparticles and nanostructured lipid carriers , 2011, Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences.

[11]  Erwin G. Van Meir,et al.  Exciting New Advances in Neuro‐Oncology: The Avenue to a Cure for Malignant Glioma , 2010, CA: a cancer journal for clinicians.

[12]  G. Raciti,et al.  Glutamate-induced increases in transglutaminase activity in primary cultures of astroglial cells , 2003, Brain Research.

[13]  M. Brandl,et al.  Brain delivery of camptothecin by means of solid lipid nanoparticles: formulation design, in vitro and in vivo studies. , 2012, International journal of pharmaceutics.

[14]  Rainer H. Müller,et al.  20 Years of Lipid Nanoparticles (SLN & NLC): Present State of Development & Industrial Applications , 2011 .

[15]  Giuseppina Raciti,et al.  Expression of tissue transglutaminase on primary olfactory ensheathing cells cultures exposed to stress conditions , 2012, Neuroscience Research.

[16]  B. Ruozi,et al.  Preparation and optimization of PIT solid lipid nanoparticles via statistical factorial design. , 2012, European journal of medicinal chemistry.

[17]  M. H. Santana,et al.  Crystallinity of Dynasan®114 and Dynasan®118 matrices for the production of stable Miglyol®-loaded nanoparticles , 2012, Journal of Thermal Analysis and Calorimetry.

[18]  G. Hause,et al.  Application of atomic force microscopy and ultrasonic resonator technology on nanoscale: distinction of nanoemulsions from nanocapsules. , 2010, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[19]  G. Li Volti,et al.  Glutamate‐evoked redox state alterations are involved in tissue transglutaminase upregulation in primary astrocyte cultures , 2004, FEBS letters.

[20]  R. Müller,et al.  Polyhydroxy surfactants for the formulation of lipid nanoparticles (SLN and NLC): effects on size, physical stability and particle matrix structure. , 2011, International journal of pharmaceutics.

[21]  C. Mohanty,et al.  Antiglioma activity of curcumin-loaded lipid nanoparticles and its enhanced bioavailability in brain tissue for effective glioblastoma therapy. , 2012, Acta biomaterialia.

[22]  R. Acquaviva,et al.  In vitro evaluation of idebenone-loaded solid lipid nanoparticles for drug delivery to the brain , 2011, Drug development and industrial pharmacy.

[23]  Xing Tang,et al.  The influence of lipid characteristics on the formation, in vitro release, and in vivo absorption of protein-loaded SLN prepared by the double emulsion process , 2011, Drug development and industrial pharmacy.

[24]  C. Carbone,et al.  Effect of Oil Phase Lipophilicity on In Vitro Drug Release from O/W Microemulsions with Low Surfactant Content , 2006, Drug development and industrial pharmacy.

[25]  R. Müller,et al.  Nanostructured lipid matrices for improved microencapsulation of drugs. , 2002, International journal of pharmaceutics.

[26]  Venkata Reddy Bandugula,et al.  2-Deoxy-d-glucose and ferulic acid modulates radiation response signaling in non-small cell lung cancer cells , 2013, Tumor Biology.

[27]  R. Pignatello,et al.  Chemical and technological delivery systems for idebenone: a review of literature production , 2012, Expert opinion on drug delivery.