Eman A Ashour1, Soumyajit Majumdar1,2, Abdulla Alsheteli3, Sultan Alshehri4, Bader Alsulays3, Xin Feng1, Andreas Gryczke5, Karl Kolter6, Nigel Langley7, Michael A Repka1,2. 1. Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS, 38677, USA. 2. Pii Center for Pharmaceutical Technology, The University of Mississippi, University, MS, 38677, USA. 3. Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, AlKharj, Saudi Arabia. 4. Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia. 5. Global Development and Technical Marketing, BASF SE, Ludwigshafen, 67056, Germany. 6. R&D Product Management Excipients, BASF SE, Ludwigshafen, 67056, Germany. 7. BASF Corporation, 500 White Plains Road, Tarrytown, NY, USA.
Abstract
OBJECTIVE: The aims of the current research project were to investigate the efficiency of various polymers to enhance the solubility and increase the systemic absorption of piperine using hot melt extrusion technology. METHODS: Piperine 10-40% w/w and Eudragit(®) EPO/Kollidon(®) VA 64 or Soluplus(®) were mixed, and the resulting blends were extruded using a twin-screw extruder (Process 11, Thermo Fisher Scientific). Drug release profiles and piperine solubility studies of the extrudates were evaluated. A non-everted intestinal sac was employed for the most promising formulation, 10% w/w piperine/Soluplus(®) , and pure piperine to study the permeability characteristics. KEY FINDINGS: Dissolution studies demonstrated enhancement in piperine per cent release of 10% and 20% w/w piperine/Soluplus(®) extrudates up to 95% and 74%, respectively. The solubility of 10% and 20% piperine/Soluplus(®) increased more than 160- and 45-fold in water, respectively. Furthermore, permeability studies demonstrated the enhancement in piperine absorption of 10% w/w piperine/Soluplus(®) extrudates up to 158.9 μg/5 ml compared with pure piperine at 1.3 μg/5 ml within 20 min. CONCLUSION: These results demonstrated that increasing the bioavailability of piperine may be achieved as demonstrated by findings in this study.
OBJECTIVE: The aims of the current research project were to investigate the efficiency of various polymers to enhance the solubility and increase the systemic absorption of piperine using hot melt extrusion technology. METHODS:Piperine 10-40% w/w and Eudragit(®) EPO/Kollidon(®) VA 64 or Soluplus(®) were mixed, and the resulting blends were extruded using a twin-screw extruder (Process 11, Thermo Fisher Scientific). Drug release profiles and piperine solubility studies of the extrudates were evaluated. A non-everted intestinal sac was employed for the most promising formulation, 10% w/w piperine/Soluplus(®) , and pure piperine to study the permeability characteristics. KEY FINDINGS: Dissolution studies demonstrated enhancement in piperine per cent release of 10% and 20% w/w piperine/Soluplus(®) extrudates up to 95% and 74%, respectively. The solubility of 10% and 20% piperine/Soluplus(®) increased more than 160- and 45-fold in water, respectively. Furthermore, permeability studies demonstrated the enhancement in piperine absorption of 10% w/w piperine/Soluplus(®) extrudates up to 158.9 μg/5 ml compared with pure piperine at 1.3 μg/5 ml within 20 min. CONCLUSION: These results demonstrated that increasing the bioavailability of piperine may be achieved as demonstrated by findings in this study.
Authors: Yuliya E Borre; Theodora Panagaki; Pim J Koelink; Mary E Morgan; Hendrikus Hendriksen; Johan Garssen; Aletta D Kraneveld; Berend Olivier; Ronald S Oosting Journal: Neuropharmacology Date: 2013-11-25 Impact factor: 5.250
Authors: Sultan Alshehri; Syed Sarim Imam; Afzal Hussain; Mohammad A Altamimi; Nabil K Alruwaili; Fahad Alotaibi; Abdullah Alanazi; Faiyaz Shakeel Journal: Drug Deliv Date: 2020-11-09 Impact factor: 6.419