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Expert Opinion on Drug Delivery Volume 9, 2012 - Issue 8
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Targeted prodrugs in oral drug delivery: the modern molecular biopharmaceutical approach

Arik DahanBen-Gurion University of the Negev, School of Pharmacy, Faculty of Health Sciences, Department of Clinical Pharmacology, P.O. Box 653, Beer-Sheva 84105, Israel+972 8 6479483; +972 8 6479303; [email protected]
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Mustafa KhamisAl-Quds University, Faculty of Pharmacy, Department of Bioorganic Chemistry, P.O. Box 20002 Jerusalem, Palestine
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Riad AgbariaBen-Gurion University of the Negev, School of Pharmacy, Faculty of Health Sciences, Department of Clinical Pharmacology, P.O. Box 653, Beer-Sheva 84105, Israel+972 8 6479483; +972 8 6479303; [email protected]
&
Rafik KaramanAl-Quds University, Faculty of Pharmacy, Department of Bioorganic Chemistry, P.O. Box 20002 Jerusalem, Palestine
Pages 1001-1013 | Published online: 18 Jun 2012

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Wajd Amly & Rafik Karaman. (2016) Recent updates in utilizing prodrugs in drug delivery (2013–2015). Expert Opinion on Drug Delivery 13:4, pages 571-591.
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Omri Wolk, Riad Agbaria & Arik Dahan. (2014) Provisional in-silico biopharmaceutics classification (BCS) to guide oral drug product development. Drug Design, Development and Therapy 8, pages 1563-1575.
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Rafik Karaman. (2014) Using predrugs to optimize drug candidates. Expert Opinion on Drug Discovery 9:12, pages 1405-1419.
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Omri Wolk, Svetlana Epstein, Viktoriya Ioffe-Dahan, Shimon Ben-Shabat & Arik Dahan. (2013) New targeting strategies in drug therapy of inflammatory bowel disease: mechanistic approaches and opportunities. Expert Opinion on Drug Delivery 10:9, pages 1275-1286.
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Rafik Karaman, Beesan Fattash & Alaa Qtait. (2013) The future of prodrugs – design by quantum mechanics methods. Expert Opinion on Drug Delivery 10:5, pages 713-729.
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Articles from other publishers (43)

Wenzhan Yang, Maya Lipert & Rebecca Nofsinger. (2023) Current screening, design, and delivery approaches to address low permeability of chemically synthesized modalities in drug discovery and early clinical development. Drug Discovery Today 28:9, pages 103685.
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Kyoung Sub Kim, Kun Na & You Han Bae. (2023) Nanoparticle oral absorption and its clinical translational potential. Journal of Controlled Release 360, pages 149-162.
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Gergely Gyimesi & Matthias A. Hediger. (2023) Transporter-Mediated Drug Delivery. Molecules 28:3, pages 1151.
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Milica Markovic, Shimon Ben‐Shabat & Arik Dahan. 2022. Targeted Drug Delivery. Targeted Drug Delivery 169 192 .
Milica Markovic, Shimon Ben-Shabat, Jagadeesh Nagendra Manda, Karina Abramov-Harpaz, Clil Regev, Yifat Miller, Aaron Aponick, Ellen M. Zimmermann & Arik Dahan. (2022) PLA2-Triggered Activation of Cyclosporine-Phospholipid Prodrug as a Drug Targeting Approach in Inflammatory Bowel Disease Therapy. Pharmaceutics 14:3, pages 675.
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Aurelia S. Elz, Natalie L. Trevaskis, Christopher J.H. Porter, Joanne M. Bowen & Clive A. Prestidge. (2022) Smart design approaches for orally administered lipophilic prodrugs to promote lymphatic transport. Journal of Controlled Release 341, pages 676-701.
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Saurabh Shah, Mahavir Bhupal Chougule, Arun K. Kotha, Rama Kashikar, Chandraiah Godugu, Rajeev Singh Raghuvanshi, Shashi Bala Singh & Saurabh Srivastava. (2021) Nanomedicine based approaches for combating viral infections. Journal of Controlled Release 338, pages 80-104.
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Zeinab Breijyeh & Rafik Karaman. (2021) Enzyme Models—From Catalysis to Prodrugs. Molecules 26:11, pages 3248.
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Utkarsh Bhutani, Tithi Basu & Saptarshi Majumdar. (2021) Oral Drug Delivery: Conventional to Long Acting New-Age Designs. European Journal of Pharmaceutics and Biopharmaceutics 162, pages 23-42.
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Yimu Li, Xuling Chen, Jianbo Ji, Lingbing Li & Guangxi Zhai. (2021) Redox-responsive nanoparticles based on Chondroitin Sulfate and Docetaxel prodrug for tumor targeted delivery of Docetaxel. Carbohydrate Polymers 255, pages 117393.
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Sahil Kumar, Bandna Sharma, Tilak R. Bhardwaj & Rajesh K. Singh. (2021) Design, Synthesis and Studies on Novel Polymeric Prodrugs of Erlotinib for Colon Drug Delivery. Anti-Cancer Agents in Medicinal Chemistry 21:3, pages 383-392.
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Ashutosh Pal & Bimal Krishna Banik. (2020) Highly Efficient Prodrugs: Design and Therapeutic Applications. Oriental Journal Of Chemistry 36:6, pages 985-1000.
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Feiyang Deng & You Han Bae. (2020) Bile acid transporter-mediated oral drug delivery. Journal of Controlled Release 327, pages 100-116.
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Milica Markovic, Shimon Ben-Shabat & Arik Dahan. (2020) Prodrugs for Improved Drug Delivery: Lessons Learned from Recently Developed and Marketed Products. Pharmaceutics 12:11, pages 1031.
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Milica Markovic, Shimon Ben-Shabat & Arik Dahan. (2020) Computational Simulations to Guide Enzyme-Mediated Prodrug Activation. International Journal of Molecular Sciences 21:10, pages 3621.
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Buthaina Jubeh, Zeinab Breijyeh & Rafik Karaman. (2020) Antibacterial Prodrugs to Overcome Bacterial Resistance. Molecules 25:7, pages 1543.
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Lalehan Akyuz. (2020) An imine based COF as a smart carrier for targeted drug delivery: From synthesis to computational studies. Microporous and Mesoporous Materials 294, pages 109850.
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Milica Markovic, Shimon Ben-Shabat, Shahar Keinan, Aaron Aponick, Ellen M. Zimmermann & Arik Dahan. (2019) Molecular Modeling-Guided Design of Phospholipid-Based Prodrugs. International Journal of Molecular Sciences 20:9, pages 2210.
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Milica Markovic, Shimon Ben‐Shabat, Shahar Keinan, Aaron Aponick, Ellen M. Zimmermann & Arik Dahan. (2018) Lipidic prodrug approach for improved oral drug delivery and therapy. Medicinal Research Reviews 39:2, pages 579-607.
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Milica Markovic, Shimon Ben-Shabat, Shahar Keinan, Aaron Aponick, Ellen Zimmermann & Arik Dahan. (2018) Prospects and Challenges of Phospholipid-Based Prodrugs. Pharmaceutics 10:4, pages 210.
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Ashok K. Shakya, Belal O. Al-Najjar, Pran Kishore Deb, Rajashri R. Naik & Rakesh K. Tekade. 2018. Dosage Form Design Considerations. Dosage Form Design Considerations 259 286 .
Bei Yang & David E. Smith. (2017) In Silico Absorption Analysis of Valacyclovir in Wildtype and Pept1 Knockout Mice Following Oral Dose Escalation. Pharmaceutical Research 34:11, pages 2349-2361.
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Arik Dahan, Milica Markovic, Shahar Keinan, Igor Kurnikov, Aaron Aponick, Ellen M. Zimmermann & Shimon Ben-Shabat. (2017) Computational modeling and in-vitro/in-silico correlation of phospholipid-based prodrugs for targeted drug delivery in inflammatory bowel disease. Journal of Computer-Aided Molecular Design 31:11, pages 1021-1028.
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Arik Dahan, Milica Markovic, Svetlana Epstein, Noa Cohen, Ellen M. Zimmermann, Aaron Aponick & Shimon Ben-Shabat. (2017) Phospholipid-drug conjugates as a novel oral drug targeting approach for the treatment of inflammatory bowel disease. European Journal of Pharmaceutical Sciences 108, pages 78-85.
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Ayman F. El-Kattan. 2017. Oral Bioavailability Assessment. Oral Bioavailability Assessment 139 171 .
Ksenia S. Egorova, Evgeniy G. Gordeev & Valentine P. Ananikov. (2017) Biological Activity of Ionic Liquids and Their Application in Pharmaceutics and Medicine. Chemical Reviews 117:10, pages 7132-7189.
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Arik Dahan & Shimon Ben-Shabat. 2017. Drug Delivery. Drug Delivery 47 64 .
Stefanie D. Krämer, Hélène E. Aschmann, Maja Hatibovic, Katharina F. Hermann, Claudia S. Neuhaus, Cyrill Brunner & Sara Belli. (2016) When barriers ignore the “rule-of-five”. Advanced Drug Delivery Reviews 101, pages 62-74.
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Zuzana Hricov?niov?Michal Hricov?ni, Vlasta Brezov?Peter Magdolen. (2016) New series of N-aryl- and N-heteroaryl-d-glucuronamides as potential anticancer agents: synthesis and spectroscopic analysis. Tetrahedron: Asymmetry 27:7-8, pages 361-368.
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Nicole J. Yang & Marlon J. Hinner. 2015. Site-Specific Protein Labeling. Site-Specific Protein Labeling 29 53 .
Arik Dahan, Omri Wolk, Peihua Yang, Sachin Mittal, Zhiqian Wu, Christopher P. Landowski & Gordon L. Amidon. (2014) Dipeptidyl Peptidase IV as a Potential Target for Selective Prodrug Activation and Chemotherapeutic Action in Cancers. Molecular Pharmaceutics 11:12, pages 4385-4394.
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Arik Dahan, Ellen Zimmermann & Shimon Ben-Shabat. (2014) Modern Prodrug Design for Targeted Oral Drug Delivery. Molecules 19:10, pages 16489-16505.
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Haruka Nishimuta, J. Brian Houston & Aleksandra Galetin. (2014) Hepatic, Intestinal, Renal, and Plasma Hydrolysis of Prodrugs in Human, Cynomolgus Monkey, Dog, and Rat: Implications for In Vitro–In Vivo Extrapolation of Clearance of Prodrugs. Drug Metabolism and Disposition 42:9, pages 1522-1531.
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Serena Marchetti & Jan H. M. Schellens. 2014. Drug Transporters. Drug Transporters 433 471 .
Rebecca Nofsinger, Sophie-Dorothee Clas, Rosa Sanchez, Abbas Walji, Kimberly Manser, Becky Nissley, Jaume Balsells, Amrithraj Nair, Qun Dang, David Bennett, Michael Hafey, Junying Wang, John Higgins, Allen Templeton, Paul Coleman, Jay Grobler, Ronald Smith & Yunhui Wu. (2014) Design of Prodrugs to Enhance Colonic Absorption by Increasing Lipophilicity and Blocking Ionization. Pharmaceuticals 7:2, pages 207-219.
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Sophie-Dorothee Clas, Rosa I. Sanchez & Rebecca Nofsinger. (2014) Chemistry-enabled drug delivery (prodrugs): recent progress and challenges. Drug Discovery Today 19:1, pages 79-87.
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Alexander B. Rozhenko. 2014. Application of Computational Techniques in Pharmacy and Medicine. Application of Computational Techniques in Pharmacy and Medicine 207 240 .
Omri Wolk & Arik Dahan. 2014. Focal Controlled Drug Delivery. Focal Controlled Drug Delivery 343 357 .
Rafik Karaman. (2013) Prodrugs Design Based on Inter- and Intramolecular Chemical Processes. Chemical Biology & Drug Design 82:6, pages 643-668.
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Arik Dahan, Omri Wolk, Young Hoon Kim, Chandrasekharan Ramachandran, Gordon M. Crippen, Toshihide Takagi, Marival Bermejo & Gordon L. Amidon. (2013) Purely in Silico BCS Classification: Science Based Quality Standards for the World’s Drugs. Molecular Pharmaceutics 10:11, pages 4378-4390.
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Rafik Karaman, Wajd Amly, Laura Scrano, Gennaro Mecca & Sabino A. Bufo. (2013) Computationally designed prodrugs of statins based on Kirby’s enzyme model. Journal of Molecular Modeling 19:9, pages 3969-3982.
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Hairat Sabit, Arik Dahan, Jing Sun, Chester J. Provoda, Kyung-Dall Lee, John H. Hilfinger & Gordon L. Amidon. (2013) Cytomegalovirus Protease Targeted Prodrug Development. Molecular Pharmaceutics 10:4, pages 1417-1424.
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Margaret S Landis. (2013) Physicochemical property trends of marketed prodrugs. Therapeutic Delivery 4:2, pages 225-237.
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