Abstract
Poor absorption, short half-life and resistance development are some of the major factors responsible for reduced drug efficacy. Lipophilic prodrugs can offer certain advantages to overcome these challenges. Chemical derivatization of hydrophilic agents with lipophilic pro-moieties can significantly elevate drug diffusion across absorptive membranes. Moreover, the desired linkage (ester vs. amide) may be selected to improve stability in vivo. Importantly, an appropriate selection of pro-moiety (targeting ligand) may promote drug specificity and selectivity. In this review article, an attempt has been made to summarize lipophilic prodrugs employed to improve delivery and efficacy of a wide range of poorly permeable but highly potent therapeutic agents. In addition, a brief overview on recent application of lipophilic prodrugs to promote encapsulation of hydrophilic agents in nano-sized drug carriers has been provided.
Keywords: Absorption, formulation and delivery, lipophilic, lipids, linkages, prodrugs.
Current Drug Targets
Title:Design of Lipophilic Prodrugs to Improve Drug Delivery and Efficacy
Volume: 17 Issue: 15
Author(s): Abhirup Mandal, Mitesh Patel, Ye Sheng and Ashim K. Mitra
Affiliation:
Keywords: Absorption, formulation and delivery, lipophilic, lipids, linkages, prodrugs.
Abstract: Poor absorption, short half-life and resistance development are some of the major factors responsible for reduced drug efficacy. Lipophilic prodrugs can offer certain advantages to overcome these challenges. Chemical derivatization of hydrophilic agents with lipophilic pro-moieties can significantly elevate drug diffusion across absorptive membranes. Moreover, the desired linkage (ester vs. amide) may be selected to improve stability in vivo. Importantly, an appropriate selection of pro-moiety (targeting ligand) may promote drug specificity and selectivity. In this review article, an attempt has been made to summarize lipophilic prodrugs employed to improve delivery and efficacy of a wide range of poorly permeable but highly potent therapeutic agents. In addition, a brief overview on recent application of lipophilic prodrugs to promote encapsulation of hydrophilic agents in nano-sized drug carriers has been provided.
Export Options
About this article
Cite this article as:
Mandal Abhirup, Patel Mitesh, Sheng Ye and Mitra K. Ashim, Design of Lipophilic Prodrugs to Improve Drug Delivery and Efficacy, Current Drug Targets 2016; 17 (15) . https://dx.doi.org/10.2174/1389450117666151209115431
DOI https://dx.doi.org/10.2174/1389450117666151209115431 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Call for Papers in Thematic Issues
New drug therapy for eye diseases
Eyesight is one of the most critical senses, accounting for over 80% of our perceptions. Our quality of life might be significantly affected by eye disease, including glaucoma, diabetic retinopathy, dry eye, etc. Although the development of microinvasive ocular surgery reduces surgical complications and improves overall outcomes, medication therapy is ...read more
- 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
-
Targeting DNA Minor Groove by Hybrid Molecules as Anticancer Agents
Current Medicinal Chemistry microRNAs and Esophageal Cancer - Implications for Pathogenesis and Therapy
Current Pharmaceutical Design Cancer Drug Discovery Targeting Histone Methyltransferases: An Update
Current Medicinal Chemistry Nuclear Hormone Receptors and Female Reproduction
Current Molecular Medicine Role of Chemokines and Their Receptors in Cancer
Current Pharmaceutical Design Palifermin in theManagement of Mucositis in Hematological Malignancies: Current Evidences and Future Perspectives
Cardiovascular & Hematological Agents in Medicinal Chemistry Transcription Factors as Potential Targets for Therapeutic Drugs
Current Pharmaceutical Biotechnology Stem Cell Defects in Philadelphia Chromosome Negative Chronic Myeloproliferative Disorders: A Phenotypic and Molecular Puzzle?
Current Stem Cell Research & Therapy Signal Transduction Therapy for Cancer - Whither Now?
Current Signal Transduction Therapy Signal Transduction Therapy: Challenges to Clinical Trial Design
Current Signal Transduction Therapy Noncovalent Binding to DNA: Still a Target in Developing Anticancer Agents
Current Medicinal Chemistry An Antileukemic Glutaminase Free L-Asparaginase from Bacillus brevis
Current Biotechnology Foamy Virus Vectors: An Awaited Alternative to Gammaretro- and Lentiviral Vectors
Current Gene Therapy Application of Stem Cell Therapy During the Treatment of HIV/AIDS and Duchenne Muscular Dystrophy
Current Stem Cell Research & Therapy Ribozymes, DNAzymes and Small Interfering RNAs as Therapeutics
Current Drug Targets Pro-apoptotic Activity of BH3-only Proteins and BH3 Mimetics: from Theory to Potential Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Enhancing the Cytotoxic Activity of Novel Targeted Therapies – Is There a Role for a Combinatorial Approach?
Current Clinical Pharmacology Nanotherapeutics in Tumour Microenvironment for Cancer Therapy
Nanoscience & Nanotechnology-Asia Current Treatment Options for HCC: From Pharmacokinetics to Efficacy and Adverse Events in Liver Cirrhosis
Current Drug Metabolism Quassinoids from Brucea Javanica Seeds Inhibiting the Replication of Tobacco Mosaic Virus
Current Bioactive Compounds