Abstract
Cetrorelix is a GnRH antagonist of the third generation. Its manifold therapeutic potential requires the adjustment of its resorption rates and effect profiles. The method of non-covalent complexation with suitable partner molecules enables the development of customized depot formulations. Investigating new partners and synthesis methods for Cetrorelix complexes we focused on maximal biocompatibility of the complexes. Compared to traditional depot forms the application of complexes aims at decreased aggregation of the peptide and increased biophily of the depots. The pharmacological properties of the new Cetrorelix complexes were analyzed by standardized dynamical in vitro liberation experiments. A new pharmacokinetic model has been developed and successfully applied for the quantitative analysis of the liberation profiles. With aromatic carboxylic acids and dipeptides we could synthesize stable complexes that have nearly linear release characteristics in aggregating environments close to in vivo conditions. The release rates were specific and very different for the complex partners. Thus several complexes have a great potential for a linear, characteristic release of the peptide in vivo and can be the basis for new depot forms for Cetrorelix.
Keywords: Cetrorelix, peptide hormone, complex, liberation, release, pharmacokinetics, aggregation
Call for Papers in Thematic Issues
Advancements in Robotic and AI-Based Drug Discovery and Delivery for Neurological Disorders
Neurological disorders, including Alzheimer's disease, Parkinson's disease, epilepsy, and brain tumors, pose significant challenges in drug delivery due to the blood-brain barrier's intricate structure and the complexity of neuronal networks. Traditional drug delivery methods often fall short in reaching therapeutic concentrations within the central nervous system, limiting treatment efficacy and ...read more
Electrospun Fibers as Drug Delivery Systems
In recent years, electrospun fibers have attracted considerable attention as potential platforms for drug delivery due to their distinctive properties and adaptability. These fibers feature a notable surface area-to-volume ratio and can be intentionally designed with high porosity, facilitating an increased capacity for drug loading and rendering them suitable for ...read more
Emerging Nanotherapeutics for Mitigation of Neurodegenerative Disorders
Conditions affecting the central nervous system (CNS) present a significant hurdle due to limited access to both treatments and diagnostic tools for the brain. The blood-brain barrier (BBB) acts as a barrier, restricting the passage of molecules from the bloodstream into the brain. The most formidable challenge facing scientists is ...read more
Extracellular Vesicles as Drug Delivery Systems.
Extracellular vesicles (EVs) are membranous vesicles released from almost all types of cells into extracellular space. EVs are categorized into different types including exosome (~30-150 nm), microvesicle or microparticle (~100-1,000 nm), apoptotic body (~1,000-5,000 nm), and others produced by different mechanisms. Since EVs bear the molecules (e.g., specific lipids, carbohydrates, ...read more
Related Journals
Anti-Cancer Agents in Medicinal Chemistry
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
Current Bioactive Compounds
Current Cancer Drug Targets
Combinatorial Chemistry & High Throughput Screening
Current Cancer Therapy Reviews
Current Diabetes Reviews
Current Drug Safety
Current Drug Targets
Current Drug Therapy
Related Books
The Roles and Responsibilities of Clinical Pharmacists in Hospital Settings
Bioactive Compounds from Medicinal Plants for Cancer Therapy and Chemoprevention
Nanotechnology in Drug Discovery
Drug Addiction Mechanisms in the Brain
Software and Programming Tools in Pharmaceutical Research
Objective Pharmaceutics: A Comprehensive Compilation of Questions and Answers for Pharmaceutics Exam Prep
Biotechnology and Drug Development for Targeting Human Diseases
Medicinal Chemistry of Drugs Affecting Cardiovascular and Endocrine Systems
Enzymatic Targets for Drug Discovery Against Alzheimer's Disease
Medicinal Plants, Phytomedicines and Traditional Herbal Remedies for Drug Discovery and Development against COVID-19
4