Abstract
The present work is an agreement with simple and efficient method of improving the therapeutic efficacy of ibuprofen by masking its acidic moiety. It aims to reduce gastrointestinal side effects by controlling the rate, duration and site of release. This is achieved by synthesis and evaluation of polymeric prodrug of ibuprofen with natural polymer sodium alginate. The synthesis was supported by N-protected serine as spacer due to chemical incompatibility of drug and polymer. Synthesized prodrug was characterized for confirmation of said structures. The in-vitro dissolution profile of ibuprofen-alginate prodrug showed that the release of the drug is significantly higher in case of pH 7.2 buffer as compared to ibuprofen, which might be due to ester group adjacent to drug get hydrolyzed. The hydrolysis was found to be with faster rate in alkaline media than that of in acidic media.
Keywords: Ibuprofen, polymeric prodrug, sodium alginate, serine, dissolution, hydrolysis.
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
Title:Synthesis and in vitro Evaluation of Polymeric Prodrug of Ibuprofen with Amino Acid Spacer
Volume: 14 Issue: 1
Author(s): Vivekkumar K. Redasani and Sanjay B. Bari
Affiliation:
Keywords: Ibuprofen, polymeric prodrug, sodium alginate, serine, dissolution, hydrolysis.
Abstract: The present work is an agreement with simple and efficient method of improving the therapeutic efficacy of ibuprofen by masking its acidic moiety. It aims to reduce gastrointestinal side effects by controlling the rate, duration and site of release. This is achieved by synthesis and evaluation of polymeric prodrug of ibuprofen with natural polymer sodium alginate. The synthesis was supported by N-protected serine as spacer due to chemical incompatibility of drug and polymer. Synthesized prodrug was characterized for confirmation of said structures. The in-vitro dissolution profile of ibuprofen-alginate prodrug showed that the release of the drug is significantly higher in case of pH 7.2 buffer as compared to ibuprofen, which might be due to ester group adjacent to drug get hydrolyzed. The hydrolysis was found to be with faster rate in alkaline media than that of in acidic media.
Export Options
About this article
Cite this article as:
K. Redasani Vivekkumar and B. Bari Sanjay, Synthesis and in vitro Evaluation of Polymeric Prodrug of Ibuprofen with Amino Acid Spacer, Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry 2015; 14 (1) . https://dx.doi.org/10.2174/1871523014666150303121043
DOI https://dx.doi.org/10.2174/1871523014666150303121043 |
Print ISSN 1871-5230 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-614X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Supertargeted Chemistry: Identifying Relationships Between Molecular Structures and their Sub-Cellular Distribution
Current Topics in Medicinal Chemistry Cell-based Tolerogenic Therapy, Experience from Animal Models of Multiple Sclerosis, Type 1 Diabetes and Rheumatoid Arthritis
Current Pharmaceutical Design Bacterial Protein Mimetic of Peptide Hormone as a New Class of Protein- based Drugs
Current Medicinal Chemistry Active Tumor Targeting of Nanomaterials Using Folic Acid, Transferrin and Integrin Receptors
Current Drug Discovery Technologies Ellipticines as DNA-Targeted Chemotherapeutics
Current Medicinal Chemistry Targeting the Immune System in Cancer
Current Pharmaceutical Biotechnology Chronic Low Back Pain: Current Pharmacotherapeutic Therapies and a New Biological Approach
Current Medicinal Chemistry A Systematic Review on Preclinical and Clinical Studies on the Use of Scaffolds for Bone Repair in Skeletal Defects
Current Stem Cell Research & Therapy Management of Hypertension in Relation to Acute Coronary Syndromes and Revascularisation
Current Pharmaceutical Design Acknowledgements to Contributors
Recent Patents on Inflammation & Allergy Drug Discovery Pharmacological and Clinical Applications of Natriuretic Peptides: Accepted Knowledges or Changing Views?
Current Pharmaceutical Analysis Structure and Function of MPN (Mpr1/Pad1 N-terminal) Domain- Containing Proteins
Current Protein & Peptide Science Metabolism of Peptide Drugs and Strategies to Improve their Metabolic Stability
Current Drug Metabolism Anti-Cancer Properties of Nigella spp. Essential Oils and their Major Constituents, Thymoquinone and β-Elemene
Current Clinical Pharmacology Prediction of Citrullination Sites on the Basis of mRMR Method and SNN
Combinatorial Chemistry & High Throughput Screening Role of the Peroxynitrite - Poly (ADP-Ribose) Polymerase Pathway in the Pathogenesis of Liver Injury
Current Pharmaceutical Design Disruption of Circadian Rhythms and Sleep in Critical Illness and its Impact on Innate Immunity
Current Pharmaceutical Design Cutting the Limits of Aminobisphosphonates: New Strategies for the Potentiation of their Anti-Tumour Effects
Current Cancer Drug Targets Insights into Immunophilin Structure and Function
Current Medicinal Chemistry Insights into Angiogenesis in Non-Small Cell Lung Cancer: Molecular Mechanisms, Polymorphic Genes, and Targeted Therapies
Recent Patents on Anti-Cancer Drug Discovery