![conference banner](/images/conference-banner.jpeg)
Abstract
Alternative formulations of paclitaxel were developed in order to improve its aqueous solubility, and characterized in vitro. A methacrylic acid based nanoconjugate of paclitaxel was synthesized by a simple esterification reaction with molecular weight of 1657 Da. The in vitro hydrolysis study on the prodrug of paclitaxel in presence of rat plasma has shown that the ester bond was quite stable (less than 1% of paclitaxel was liberated from prodrug in 24 h). This water-soluble prodrug was encapsulated into polyethylene glycol coated liposomes optimized with saturated lipids, to overcome the physical instability associated with paclitaxel. Under in vitro testing, prodrug liposomes seem very impressive with release of only 45% of payload in 180 h. Further, chemical as well as physical stability studies have shown that liposomes were stable without any signs of crystallization of paclitaxel. In addition, paclitaxel was covalently coupled to poloxamer via methacrylic acid linker to obtain a micelle forming conjugate. Evidence for self-assembly of this conjugate into micelles was provided by fluorescence spectroscopy, light scattering and differential scanning calorimetry techniques. Micellization of the conjugate was thermodynamically favored and the core of resulting micelles exhibited higher microviscosities (than poloxamer micelles). Release studies using dialysis technique along with high performance liquid chromatography revealed that paclitaxel is liberated from micelle in the form of methacrylic acid oligomer based prodrug in a gradual manner. These preliminary studies provided indication on the performance and feasibility of testing these carrier systems as a safer alternative to the Cremophor EL based paclitaxel formulation.
Keywords: paclitaxel, prodrug, liposomes, micelles, stability
Current Drug Delivery
Title: Preparation and Characterization of Water-Soluble Prodrug, Liposomes and Micelles of Paclitaxel
Volume: 2 Issue: 1
Author(s): Anand Babu Dhanikula and Ramesh Panchagnula
Affiliation:
Keywords: paclitaxel, prodrug, liposomes, micelles, stability
Abstract: Alternative formulations of paclitaxel were developed in order to improve its aqueous solubility, and characterized in vitro. A methacrylic acid based nanoconjugate of paclitaxel was synthesized by a simple esterification reaction with molecular weight of 1657 Da. The in vitro hydrolysis study on the prodrug of paclitaxel in presence of rat plasma has shown that the ester bond was quite stable (less than 1% of paclitaxel was liberated from prodrug in 24 h). This water-soluble prodrug was encapsulated into polyethylene glycol coated liposomes optimized with saturated lipids, to overcome the physical instability associated with paclitaxel. Under in vitro testing, prodrug liposomes seem very impressive with release of only 45% of payload in 180 h. Further, chemical as well as physical stability studies have shown that liposomes were stable without any signs of crystallization of paclitaxel. In addition, paclitaxel was covalently coupled to poloxamer via methacrylic acid linker to obtain a micelle forming conjugate. Evidence for self-assembly of this conjugate into micelles was provided by fluorescence spectroscopy, light scattering and differential scanning calorimetry techniques. Micellization of the conjugate was thermodynamically favored and the core of resulting micelles exhibited higher microviscosities (than poloxamer micelles). Release studies using dialysis technique along with high performance liquid chromatography revealed that paclitaxel is liberated from micelle in the form of methacrylic acid oligomer based prodrug in a gradual manner. These preliminary studies provided indication on the performance and feasibility of testing these carrier systems as a safer alternative to the Cremophor EL based paclitaxel formulation.
Export Options
About this article
Cite this article as:
Dhanikula Babu Anand and Panchagnula Ramesh, Preparation and Characterization of Water-Soluble Prodrug, Liposomes and Micelles of Paclitaxel, Current Drug Delivery 2005; 2 (1) . https://dx.doi.org/10.2174/1567201052772861
DOI https://dx.doi.org/10.2174/1567201052772861 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
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
![Wayfinder Image](/images/wayfinder.jpg)
- 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
-
Predictive QSAR Modeling Workflow, Model Applicability Domains, and Virtual Screening
Current Pharmaceutical Design Prediction of Gene Co-Expression by Quantifying Heterogeneous Features
Current Bioinformatics Targeting the HIF-1α/Cav-1 Pathway with a Chicory Extract/Daidzein Combination Plays a Potential Role in Retarding Hepatocellular Carcinoma
Current Cancer Drug Targets Exploring Single Nucleotide Polymorphisms in ITGAV for Gastric, Pancreatic and Liver Malignancies: An Approach Towards the Discovery of Biomarker
Combinatorial Chemistry & High Throughput Screening In vivo Optical Molecular Imaging of Cardiovascular Diseases: Long Road Ahead
Current Molecular Imaging (Discontinued) Separation Media in Affinity Chromatography of Proteins - A Critical Review
Current Proteomics Significance of Color Spaces and Their Selection for Image Processing: A Survey
Recent Advances in Computer Science and Communications Microwave-promoted Synthesis of S-substituted Quinazoline Derivatives using 1,4-dihydroquinazoline-2-thiol
Letters in Drug Design & Discovery ADME Optimization and Toxicity Assessment in Early- and Late-Phase Drug Discovery
Current Topics in Medicinal Chemistry Oleuropein Mediated Targeting of Signaling Network in Cancer
Current Topics in Medicinal Chemistry Refolding Additive, Dimethylbenzylammonium Propane Sulfonate (NDSB- 256), Accelerates Gly-Pro cis-trans Isomerization
Protein & Peptide Letters A Concise Review on Multidimensional Silver Nanoparticle Health Aids and Threats
Current Drug Therapy From Nanotechnology to Nanomedicine: Applications to Cancer Research
Current Molecular Medicine Membrane Fusion Mediated Targeted Cytosolic Drug Delivery Through scFv Engineered Sendai Viral Envelopes
Current Molecular Medicine Synthesis, Aromatase Inhibitory, Antiproliferative and Molecular Modeling Studies of Functionally Diverse D-Ring Pregnenolone Pyrazoles
Anti-Cancer Agents in Medicinal Chemistry Potential Health Benefits of Passion Fruit Peel Flour
The Natural Products Journal Curcumin, Resveratrol and Cannabidiol as Natural Key Prototypes in Drug Design for Neuroprotective Agents
Current Neuropharmacology Delivery of Neurotherapeutics Across the Blood Brain Barrier in Stroke
Current Pharmaceutical Design Gd-EOB-DTPA-enhanced MRI Image Characteristics and Radiomics Characteristics Combined with Machine Learning for Assessment of Functional Liver Reserve
Current Medical Imaging Imiquimod
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry