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PRODRUGS Prepared By: R Sukesh Registration No:12CQ1R0051 Class: IV B. Pharmacy I Sem Under the guidance of Dr. Subhashis Debnath ., M. Pharm., Ph.D Professor and HOD Dept. of Pharmaceutics Seven Hills College of Pharmacy Tirupati 517561 1

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INTRODUCTION Prodrug (Inactive) Biological Barrier Inactive Form Active Form Biotransformation Pharmacological Action ( Rautio J, et al., 2008) 2


REASONS FOR PRODRUG 3 (Smith and Williams, et al., 2011)

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Ideal characteristics Rapid biotransformation Non toxic Should not have intrinsic pharmacological activity No drug interactions 4 IDEAL CHARACTERISTICS (Smith and Williams, et al., 2011)

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( Arik Dahan, et al .,2014) CLASSIFICATION Prodrug Type -II Type - I Type - IB Eg : Heroin Type -IIA Eg : Oxyphenisatin Type -IIB Eg : Bambuterol Type- IA Eg : Levodopa Mixed type

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6 Dopamine Levodopa Hydrophilic Lipophilic Dopa decarboxylase Carbidopa (-) Levodopa Dopamine Pharmacological Action Blood Brain Barrier Dopa decarboxylase Not cross through BBB Prodrug of Dopamine WORKING PRINCIPLE OF LEVODOPA

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7 APPROACHES TO PRODRUGS WITH LIPOPROTEINS Types HDL LDL VLDL CHYLOMICRON Fig no.1: Illustration of lipidic pro drug approach Types of Lipoprotiens

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8 Types of lipidic carriers Fattyacids in prodrug design 1 Glycerides in a Prodrug design Phospholipids in a prodrug design 3 2 Enteral delivery Targeting to the lymphatic system Central Nervous system targeting Liver targeting. ( Patil S.j ,et al .,2011)

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( Jolanta B ,et al.,2013) SITE SPECIFIC PRODRUG APPROACH BY CHEMICAL MODIFICATION Functional groups amenable to prodrug design Esters as prodrugs of carboxyl, hydroxyl and thiol functionalities . Carbonates and carbamates as prodrugs of carboxyl ,hydroxyl or amine functionalities. Amides as prodrugs of carboxylic acids and amines Oximes as derivatives of ketones , amidines and guanidines .


ANTIBODY BASED TARGETING 10 Schematic representation of ADEPT and GDEPT ( Bildstein ,et al2011)


APPLICATIONS ( Bhosle D, et al.,2006) 11


12 CONCLUSION Instead of synthesizing new compounds which is a time consuming and too costly an affair, the designing of derivatives of existing drug is definitely an interesting and promising area of research. Moreover, as the metabolic profile of the liberated parent drug (after cleavage of the derivative in the body) would be already known, it could be advantageous to design derivatives of parent drug. The prodrug design offers a very fruitful area of research and an efficient tool for improving the clinical and therapeutic effectiveness of drug that is suffering from some undesirable side-effects hindering its clinical usefulness otherwise.


13 REFERENCE Smith and Williams, Introduction to the Principles of Drug Design and Action, 4th Ed, Taylor and Francis Group, 2011, USA: 216-230. Brahmankar DM, Jaiswal SB, Biopharmaceutics and Pharmacokinetics- A Treatise, Vallabh Prakashan , Delhi, 1995. 162-168. Rautio J et al, Prodrug : design and clinical applications, Nature 7, 2008: 255-268 Bhosle D, Bharambe S, Gairola N, and Dhaneshwar SS, Mutual prodrug concept: Fundamentals and applications. Indian Journal of Pharmaceutical Sciences 68, 2006: 286-294 Gennaro , R., Alfanso , W., Remington: The science and practice of pharmacy, Lippincott Williams & Wilkins, 2003, 20, 1, 913-914. Jolanta B. Zawilska , Jakub Wojcieszak et al Prodrugs : A challenge for the drug development, 2013, 65, 1–14 Patil S.j ., P.J. Shirote,prodrug approach: an effective solution to overcome side- effects,IJMPS,vol 01 issue 07,11 Arik Dahan , Ellen M. Zimmermann et al,Modern Prodrug Design for Targeted Oral Drug Delivery,2014 Bildstein , L.; Dubernet , C.; Couvreur , P. Prodrug -based intracellular delivery of anticancer agents. Adv. Drug Deliv . Rev. 2011 , 63, 3–23. Huttunen , K.M.; Raunio , H.; Rautio , J. Prodrugs —From serendipity to rational design. Pharmacol . Rev. 2011 , 63, 750–771.

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