Preeti M. Chabukswar and Swati C. Jagdale 1. The prodrug approach using various carriers has evolved as a significant tool in surmounting different obstacles in relation to drug formulation and targeting. Properties and selection of carriers or promoeities is a very important parameter in successful prodrug design.
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Published on Oct 30, The presentation provides the brief description about bioiprecursor prodrugs and site specific drug delivery approach.
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Show related SlideShares at end. WordPress Shortcode. SobhiGaba Follow. Full Name Comment goes here. Are you sure you want to Yes No. Padma Kumar. Deepali Sammal. No Downloads. Views Total views. Actions Shares. Embeds 0 No embeds. No notes for slide. The activation of these prodrugs can be by following pathways:- I.
The various types of oxidation occurring in the compounds are as follows:- 1. N and O Dealkylation 2. Oxidative Deamination 3. N-Oxidation 4. S-Oxidation Pralidoxime chloride after crossing the BBB gets converted to Pralidoxime through N Oxidation which further acts with phosphorous to treat organophophorous poisoning Acyclovir itself is inactive but it is selectively phosphorylated by a viral thymidine kinase to corresponding monophosphate uninfected cells do not phosphorylate acyclovir and this accounts for the selective toxicity towards viral cells.
The conversion of monophosphate to diphosphate catalysed by guanylate kinase. The conversion of diphosphate to triphosphate catalysed by phosphoglycerate kinase Acyclovir triphosphate is a substrate for the viral alpha DNA polymerase but not for human cellular alpha DNA polymerase Incorporation of acyclovir triphosphate into the viral DNA leads to the formation of dead and complex and result in viral cell death.
STEP 3- The prodrug is actively converted into the the active anticancer drug in high local concentration inside the tumour cells The prodrug-activating enzyme should be either of non human origin or a human protein that is absent or expressed only at lower concentrations in normal tissues.
The prodrug-activating enzyme must achieve adequate expression in the targeted tumour cells and have high catalytic activity III. The prodrug should be a good substrate for the enzyme incorporated in the tumours but nit be activated by endogeneous enzymes outside the tumours The prodrug must be able to cross the tumour cell membrane for intracellular activation. The cytotoxicity difference between the prodrug and its corresponding active drug should be high. Advantage is only evident if enough time is allowed for the clearance of antibdody enzyme conjugate that is not bound to tumor cells.
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Bioprecursor Prodrugs: Molecular Modification of the Active Principle