Abstract
Peptide amphiphiles (PAs) are novel engineered biomaterials able to self-assemble into supramolecular systems that have shown significant promise in drug delivery across the cell membane and across challenging biological barriers showing promise in the field of brain diseases, regenerative medicine and cancer. PAs are amino-acid block co-polymers, with a peptide backbone composed usually of 8-30 amino acids, a hydrophilic block formed by polar amino acids, a hydrophobic block which usually entails either non-polar or aromatic amino acids and alkyl, acyl or aryl lipidic tails and in some cases a spacer or a conjugated targeting moiety. Finely tuning the balance between the hydrophilic and hydrophobic blocks results in a range of supramolecular structures that are usually stabilised by hydrophobic, electrostatic, β-sheet hydrogen bonds and π-π stacking interactions. In an aqueous environment, the final size, shape and interfacial curvature of the PA is a result of the complex interplay of all these interactions. Lanreotide is the first PA to be licensed for the treatment of acromegaly and neuroendocrine tumours as a hydrogel administered subcutaneously, while a number of other PAs are undergoing preclinical development. This review discusses PAs architecture fundamentals that govern their self-assembly into supramolecular systems for applications in drug delivery.
Keywords: Peptide amphiphiles, Peptide self-assembly, Driving forces, Drug delivery, Nanofibers.
Current Topics in Medicinal Chemistry
Title:Peptide Self-Assemblies for Drug Delivery
Volume: 15 Issue: 22
Author(s): Diana M. Leite, Eugen Barbu, Geoffrey J. Pilkington and Aikaterini Lalatsa
Affiliation:
Keywords: Peptide amphiphiles, Peptide self-assembly, Driving forces, Drug delivery, Nanofibers.
Abstract: Peptide amphiphiles (PAs) are novel engineered biomaterials able to self-assemble into supramolecular systems that have shown significant promise in drug delivery across the cell membane and across challenging biological barriers showing promise in the field of brain diseases, regenerative medicine and cancer. PAs are amino-acid block co-polymers, with a peptide backbone composed usually of 8-30 amino acids, a hydrophilic block formed by polar amino acids, a hydrophobic block which usually entails either non-polar or aromatic amino acids and alkyl, acyl or aryl lipidic tails and in some cases a spacer or a conjugated targeting moiety. Finely tuning the balance between the hydrophilic and hydrophobic blocks results in a range of supramolecular structures that are usually stabilised by hydrophobic, electrostatic, β-sheet hydrogen bonds and π-π stacking interactions. In an aqueous environment, the final size, shape and interfacial curvature of the PA is a result of the complex interplay of all these interactions. Lanreotide is the first PA to be licensed for the treatment of acromegaly and neuroendocrine tumours as a hydrogel administered subcutaneously, while a number of other PAs are undergoing preclinical development. This review discusses PAs architecture fundamentals that govern their self-assembly into supramolecular systems for applications in drug delivery.
Export Options
About this article
Cite this article as:
Leite M. Diana, Barbu Eugen, Pilkington J. Geoffrey and Lalatsa Aikaterini, Peptide Self-Assemblies for Drug Delivery, Current Topics in Medicinal Chemistry 2015; 15 (22) . https://dx.doi.org/10.2174/1568026615666150605120456
DOI https://dx.doi.org/10.2174/1568026615666150605120456 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
- Announcements
Related Articles
-
Recent Advances of Small Molecule Focal Adhesion Kinase (FAK) Inhibitors as Promising Anticancer Therapeutics
Current Medicinal Chemistry Renal Development: A Complex Process Dependent on Inductive Interaction
Current Pediatric Reviews Alpha-1 Antitrypsin: It’s Role in Health and Disease
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Hypothyroidism and Nephrotic Syndrome: Why, When and How to Treat
Current Vascular Pharmacology Functional Improvement of Chimeric Antigen Receptor Through Intrinsic Interleukin-15Rα Signaling
Current Gene Therapy Malignancy and Radiation-Induced Cardiotoxicity
Cardiovascular & Hematological Disorders-Drug Targets RUNX2 and Osteosarcoma
Anti-Cancer Agents in Medicinal Chemistry Potential of Selected Antioxidants for Influenza Chemotherapy
Anti-Infective Agents in Medicinal Chemistry Recent Advances in Delivery Through the Blood-Brain Barrier
Current Topics in Medicinal Chemistry Influence of a Novel Inhibitor (UM8190) of Prolylcarboxypeptidase (PRCP) on Appetite and Thrombosis
Current Medicinal Chemistry PEDF in Angiogenic Eye Diseases
Current Molecular Medicine Molecular Pathways Associated with Aggressiveness of Papillary Thyroid Cancer
Current Genomics An Insight into Molecular Mechanisms and Novel Therapeutic Approaches in Epileptogenesis
CNS & Neurological Disorders - Drug Targets Redox State, Oxidative Stress, and Molecular Mechanisms of Protective and Toxic Effects of Bilirubin on Cells
Current Pharmaceutical Design Patent on Biomarkers in Medical Research: A Focus on Neuropsychiatric Disorders
Recent Patents on Biomarkers Genetic Polymorphisms of Drug Metabolising Enzymes and Drug Transporters in Relation to Cancer Risk
Current Cancer Therapy Reviews Targeting DNA Topoisomerase I with Non-Camptothecin Poisons
Current Medicinal Chemistry Biomarkers Linking PCB Exposure and Obesity
Current Pharmaceutical Biotechnology Transporter-Based Delivery of Anticancer Drugs to the Brain: Improving Brain Penetration by Minimizing Drug Efflux at the Blood-Brain Barrier
Current Pharmaceutical Design CD14-Dependent Innate Immunity-Mediated Neuronal Damage in Vivo is Suppressed by NSAIDs and Ablation of a Prostaglandin E2 Receptor, EP2
Current Medicinal Chemistry - Central Nervous System Agents