Prasant Nahak1, Rahul L Gajbhiye2, Gourab Karmakar1, Pritam Guha1, Biplab Roy1, Shila Elizabeth Besra3, Alexey G Bikov4, Alexander V Akentiev4, Boris A Noskov4, Kaushik Nag5, Parasuraman Jaisankar6, Amiya Kumar Panda7. 1. Department of Chemistry, University of North Bengal, Darjeeling, West Bengal, 734 013, India. 2. Organic and Medicinal Chemistry Division, CSIR-Indian Institute of Chemical Biology, 4, Raja S. C. Mullcik Road, Jadavpur, Kolkata, West Bengal, 700032, India. 3. Cancer Biology and Inflammatory Disorder Division, CSIR-Indian Institute of Chemical Biology, 4, Raja S. C. Mullcik Road, Jadavpur, Kolkata, West Bengal, 700032, India. 4. Department of Colloid Chemistry, Saint Petersburg State University, Universitetsky pr. 26, Saint Petersburg, 198504, Russia. 5. Department of Biochemistry, Memorial University of Newfoundland, St. John's, Newfoundland and Labrador, Canada. 6. Organic and Medicinal Chemistry Division, CSIR-Indian Institute of Chemical Biology, 4, Raja S. C. Mullcik Road, Jadavpur, Kolkata, West Bengal, 700032, India. jaisankar@iicb.res.in. 7. Department of Chemistry and Chemical Technology, Vidyasagar University, Midnapore, West Bengal, 721 102, India. akpanda@mail.vidyasagar.ac.in.
Abstract
PURPOSE: Orcinol glucoside (OG) - loaded nanostructured lipid carrier (NLC), coated with polyethylene glycol-25/55-stearate (PEG-25/55-SA), were explored for delivering OG to improve in vitro cytotoxicity against gastrointestinal tract (GIT), colon and hepatoma carcinoma cell lines. It is being expected that the PEGylated formulations would possess the sustainability in withstanding the adverse physiological extremities like the most significant metabolic activities and phase I / II enzymatic activities in the intestines. METHODS: NLCs were prepared using tristearin, oleic acid and PEG-25/55-stearate by hot homogenization-ultrasonic dispersion; characterized by DLS, TEM, SEM, AFM, entrapment efficiency and drug loading capacity studies. RESULTS: NLC diameter ranged from 160 to 230 nm with negative zeta potential of -8 to -20 mV. TEM/SEM and AFM studies suggest spherical and smooth surface morphologies. Differential scanning calorimetry studies reveal the loss of crystallinity when OG was incorporated into the NLC. NLCs showed initial burst release, followed by sustained release of OG. PEG-NLC exhibited superior anticancer activity against GIT and also in hepatoma cancer cell lines. CONCLUSIONS: This is the first report demonstrating a practical approach for possible oral delivery of OG in GIT and targeting hepatoma cancer, warranting further in vivo studies for superior management of GIT cancer.
PURPOSE:Orcinol glucoside (OG) - loaded nanostructured lipid carrier (NLC), coated with polyethylene glycol-25/55-stearate (PEG-25/55-SA), were explored for delivering OG to improve in vitro cytotoxicity against gastrointestinal tract (GIT), colon and hepatoma carcinoma cell lines. It is being expected that the PEGylated formulations would possess the sustainability in withstanding the adverse physiological extremities like the most significant metabolic activities and phase I / II enzymatic activities in the intestines. METHODS: NLCs were prepared using tristearin, oleic acid and PEG-25/55-stearate by hot homogenization-ultrasonic dispersion; characterized by DLS, TEM, SEM, AFM, entrapment efficiency and drug loading capacity studies. RESULTS: NLC diameter ranged from 160 to 230 nm with negative zeta potential of -8 to -20 mV. TEM/SEM and AFM studies suggest spherical and smooth surface morphologies. Differential scanning calorimetry studies reveal the loss of crystallinity when OG was incorporated into the NLC. NLCs showed initial burst release, followed by sustained release of OG. PEG-NLC exhibited superior anticancer activity against GIT and also in hepatoma cancer cell lines. CONCLUSIONS: This is the first report demonstrating a practical approach for possible oral delivery of OG in GIT and targeting hepatoma cancer, warranting further in vivo studies for superior management of GIT cancer.
Authors: Amit K Jain; Ashay Jain; Neeraj K Garg; Abhinav Agarwal; Atul Jain; Som Akshay Jain; Rajeev K Tyagi; Rakesh K Jain; Himanshu Agrawal; Govind P Agrawal Journal: Colloids Surf B Biointerfaces Date: 2014-06-06 Impact factor: 5.268