Custom Enzyme Responsive Liposome Service
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Enzyme-responsive liposomes have garnered significant interest as an innovative drug delivery system that responds to stimuli. CD Formulation is dedicated to leveraging cutting-edge technology and expertise to support the development of intelligent liposomes, which exhibit high-performance responses to enzymes.
Mechanism of Enzyme Responsive Liposomes
In various pathological conditions such as inflammation, infection, and cancer, the levels of multiple enzymes increase. This biochemical abnormality can be utilized to design nanocarriers that release their payload through structural transformation. Enzymatic reactions in liposomes result in the release of their cargo through several unstable mechanisms involving interaction with enzymes: (a) disrupting the primary structure of liposomes, (b) detaching PEG shells, and (c) activating liposome-associated prodrugs.
Fig.1 Schematic representation of enzyme-responsive liposomes for drug delivery. (Wei Y, et al., 2024)
Our Enzyme Responsive Liposome Customization Service
Study on the mechanism of Enzyme-triggered
We categorize enzyme-responsive liposomes into two primary groups: extracellular and intracellular enzyme-triggered mechanisms. We conduct comprehensive investigations on intracellular enzyme-triggered mechanisms (such as Cathepsin B) and extracellular enzymes (secreted phospholipase A2 (sPLA2), matrix metalloproteinases (MMPs), urokinase plasminogen activator (uPA), elastase, prostate-specific antigen (PSA), etc.) triggered mechanisms to offer innovative ideas for liposome development.
Study on the enzyme distribution in various diseases
Dysregulation of enzymes at different levels is widespread in various diseases (such as different types of cancer) at different stages of a disease and among patients with the same disease. Therefore, we provide a study on the spatial and temporal distribution of enzymes, which will greatly help in designing more precise and effective liposomes.
Study of enzyme-responsive specificity
Different subtypes of enzymes have overlapping substrates for different subtypes (e.g., the MMP family). Therefore, when a short substrate peptide is incorporated into a liposome, it is difficult to determine whether it is cleaved by a specific enzyme or a family of enzymes. We offer chemical design services to improve substrate specificity for enzyme-specific reactions.
Characterization analysis
We provide physical and chemical characterization (particle size, charge distribution, charge load and encapsulation rate, viscosity, rheology, appearance, stability, etc.). In vitro characterization services include cell uptake rate assay, cytotoxicity assay, and in vitro enzyme-induced release studies. In vivo characterization services such as in vivo distribution analysis, in vivo bioactivity analysis, in vivo stability analysis, etc.
Our Platforms for Enzyme Responsive Liposome Customization
| Techniques and Platforms |
Specifics |
| Mechanism study of enzyme-triggered platform |
- To study the trigger mechanism of enzyme stimuli (classification).
- To study the multi-responsive trigger mechanisms with enzyme triggers.
|
| Enzyme distribution study platform in various diseases |
- Investigating the distribution of enzyme levels in different diseases (type, level, and characteristics).
|
| In vitro and in vivo characterization platform |
- Advanced analytical instruments for in vitro and in vivo analysis.
- Enzyme-triggered in vivo and in vitro release characteristics and response sensitivity.
|
| Enzyme-responsive specificity platform |
- Designing specific reaction substrates.
- Improve targeting.
|
Why Choose CD Formulation?
- Intelligent enzyme-responsive delivery platform. The platform facilitates the development of innovative enzyme-responsive liposome products, allowing for in-depth exploration of enzyme reaction mechanisms and offering customers more cutting-edge concepts.
- Techniques for the specific study of enzymatic reactions. Specific research techniques can aid customers in enhancing the specificity of their products, facilitating systematic analysis of the specificity of homologous enzymes for different substrates, as well as discerning the specificity between different enzymes.
- The proficient teams. The technical team is spearheaded by experienced and highly skilled experts proficient in enzyme-responsive liposomes, showcasing extensive expertise and a diverse interdisciplinary background.
Published Data
Technology: matrix metalloproteinase-2 (MMP-2) responsive peptide-hybrid liposome technique
Journal: ACS Nano
IF: 15.8
Published: 2017
Results: To regulate PSCs, matrix metalloproteinase-2 (MMP-2) responsive peptide-hybrid liposomes (MRPL) were constructed by co-assembly of customized MMP-2 responsive amphiphilic peptides and phospholipids. By utilizing a pathological environment rich in MMP-2, MRPL (MRPL-PFD) loaded with pirfenidone (PFD) can specifically release PFD at the pancreatic tumor site and down-regulate multiple components of ECM expressed by PSCs. This led to a significant increase in the penetration of gemcitabine into tumor tissue and enhanced the efficacy of gemcitabine in pancreatic tumors. The authors' tailored design for pancreatic cancer anti-fibrosis may provide a practical way to construct functional liposomes through supramolecular assembly, and modulating ECM may be a promising adjunctive therapeutic strategy for pancreatic and other ECM-rich tumors.
Fig.2 Schematic representation of the preparation and dual stimuli-triggered drug release. (Ji T, et al., 2017)
As a leading company in nanoparticle development, CD Formulation is dedicated to providing smart liposome products responsive to enzyme stimuli. Please do not hesitate to contact us if you require any assistance.
References
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Wei Y, Lv J, et al. Enzyme-responsive liposomes for controlled drug release. Drug Discovery Today. 2024, May 3: 104014.
- Ji T, Lang J, et al. Designing liposomes to suppress extracellular matrix expression to enhance drug penetration and pancreatic tumor therapy. ACS Nano. 2017; 11(9):8668-78.
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