Transferrin mediated solid lipid nanoparticles containing curcumin: Enhanced in vitro anticancer activity by induction of apoptosis

• Published in: International journal of pharmaceutics Vol. 398; no. 1; pp. 190 - 203
• Main Authors: Mulik, Rohit S., Mönkkönen, Jukka, Juvonen, Risto O., Mahadik, Kakasaheb R., Paradkar, Anant R.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 15-10-2010; Elsevier
• Subjects: Antineoplastic Agents - administration & dosage; Antineoplastic Agents - pharmacology; Antitumor activity; Apoptosis; Apoptosis - drug effects; Apoptosis - physiology; Biological and medical sciences; Breast cancer; Cell Line, Tumor; Curcumin; Curcumin - administration & dosage; Curcumin - pharmacology; Cytotoxicity; Flow cytometry; General pharmacology; Humans; Lipids - administration & dosage; Lipids - physiology; Medical sciences; Nanoparticles - administration & dosage; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Transferrin - administration & dosage; Transferrin - physiology; Flow cytometry; Cytotoxicity; Curcumin; Breast cancer; Apoptosis; Antineoplastic agent; Transferrin; Breast disease; Pharmaceutical technology; Tyrosine kinase inhibitor; Induction; Malignant tumor; In vitro; Biological activity; Mammary gland diseases; Cell death; Cancer
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2010.07.021

Photodegradation and low bioavailability are major hurdles for the therapeutic use of curcumin. Aim of the present study was to formulate transferrin-mediated solid lipid nanoparticles (Tf-C-SLN) to increase photostability, and enhance its anticancer activity against MCF-7 breast cancer cells. Tf-C-SLN were prepared by homogenization method and characterized by size, zeta potential, entrapment efficiency and stability, transmission electron microscopy (TEM), X-ray diffraction (XRD) and
in vitro release study. Microplate analysis and flow cytometry techniques were used for cytotoxicity and apoptosis study. The physical characterization showed the suitability of method of preparation. TEM and XRD study revealed the spherical nature and entrapment of curcumin in amorphous form, respectively. The cytotoxicity, ROS and cell uptake was found to be increased considerably with Tf-C-SLN compared to curcumin solubilized surfactant solution (CSSS) and curcumin-loaded SLN (C-SLN) suggesting the targeting effect. AnnexinV-FITC/PI double staining, DNA analysis and reduced mitochondrial potential confirmed the apoptosis. The flow cytometric studies revealed that the anticancer activity of curcumin is enhanced with Tf-C-SLN compared to CSSS and C-SLN, and apoptosis is the mechanism underlying the cytotoxicity. The present study indicated the potential of Tf-C-SLN in enhancing the anticancer effect of curcumin in breast cancer cells
in vitro.