Doxorubicin Liposomal
Online InquiryDoxorubicin liposomal formulations significantly improved the efficacy and safety of the parental compound, doxorubicin-an intensely used anthracycline antibiotic. BOC Sciences is committed to providing quality liposomal Doxorubicin products for basic experimental research, including chemotherapy-related cellular experiments and experimental animal injections. The formulation of our Liposomal Doxorubicin is constantly optimized by professionals, and multiple product forms can be chosen according to project needs to help improve your R&D efficiency. In addition, we offer a range of custom liposome services for you to choose from. At BOC Sciences, you're sure to make a difference in liposomes.
What is Doxorubicin Liposomal?
Doxorubicin liposomal is a formulation in which doxorubicin is entrapped inside of liposomes-nanosized vesicles surrounded by lipid bilayers. Such encapsulation remarkably improves the pharmacokinetic profile of doxorubicin, prolonging its sojourn in the blood and, hence, its permeation at tumor sites. The liposomal structure enhances not only the delivery of the drug in a more targeted manner but also reduces systemic toxicity associated with conventional doxorubicin. This encapsulation was reported to be associated with improved therapeutic outcomes because it maximized the drug's concentration at the tumour site while simultaneously protecting normal tissues from exposure, thus enhancing the overall safety profile of doxorubicin.
Modifications of PEGylated liposomal doxorubicin (PLD) surface. (K, Aloss.; et al, 2023)
What is Doxorubicin?
Doxorubicin, commercially known by its brand name Adriamycin, is one of the most potent anthracycline drugs developed for use in humans against the most widespread range of neoplastic diseases such as breast cancer, cancer of the bladder, Kaposi's sarcoma, lymphoma, and acute lymphoblastic leukemia. The mechanism of doxorubicin actions involves an anticancer effect by intercalation into the DNA to inhibit DNA replication and transcription, and the inhibition of topoisomerase II, an enzyme important for DNA replication. Though clinically effective against many malignancies, doxorubicin causes significant side effects, most notably cardiotoxicity, which may result in long-term heart damage. These challenges necessitate the development of new drug delivery systems that enhance the efficacy of doxorubicin with minimal adverse effects associated with its administration.
Chemical structural formula of Doxorubicin.
Doxorubicin Liposomal Products from BOC Sciences
At BOC Sciences, we offer a diverse range of Doxil formulations tailored to meet specific research needs. Our Doxil products are subjected to rigorous quality testing to ensure high purity and stability, making them suitable for a variety of experimental applications.
| Types of Doxorubicin Liposomal | Descrption | Quote |
|---|---|---|
| Pegylated Liposomal Doxorubicin | Pegylated liposomal doxorubicin represents a novel formulation of doxorubicin with the incorporation of PEG in the drug molecule, augmenting hydrophilicity and pharmacokinetics. Reduced recognition of drugs by MPS leads to increased circulation time and tumor accumulation of drugs. | Inquiry |
| Doxorubicin Lyophilized Liposomes | Lyophilization of doxorubicin liposomes involves the removal of water under vacuum to result in a dry powder that may be convenient for reconstitution. By using advanced techniques, BOC Sciences produces high-quality lyophilized products that ensure stable formulation with extended shelf life for the researchers. | Inquiry |
| Thermosensitive Liposomal Doxorubicin | Thermosensitive liposomal doxorubicin is a special formulation of Doxorubicin, encapsulated into liposomes with the unique property of becoming more permeable at high temperatures. Thermosensitive liposomal Doxorubicin is normally combined with heat therapy. Due to localized high temperatures, the phase transition of liposomes will allow them to be more permeable. This property may make controlled drug release possible and enhance the therapeutic effect of the drug. These liposomes within the formulation are temperature-sensitive. | Inquiry |
| pH-Sensitive Doxorubicin Liposome | The tumor microenvironment (TME) has lower pH, with pH=6.5-6.8, compared to normal tissues, which has a pH=7.4. In addition, the lysosomal pH is as low as pH 5-6 compared with others. According to the different pH, acid-responsive Doxorubicin liposome nanoparticles can be prepared. Extra pH sensitivity is achieved by incorporating pH-sensitive lipids, pH-sensitive peptides, and pH-sensitive polymers. | Inquiry |
| Antibody-Conjugated Doxorubicin Liposome | Generally, antibodies represent common molecules used for targeted drug delivery due to their high specificity and affinity. Their application for functionalization has been extended to different liposomes, including Doxorubicin lipids. The approach is aimed at combining the advantages of liposomal Doxorubicin, which includes improved drug delivery and reduced side effects, with the specificity of antibodies targeting the cancer cells. | Inquiry |
| Peptide-Conjugated Doxorubicin Liposome | Due to their small size, synthetic peptides as targeting ligands possess several advantages compared to antibodies, enhancing their penetration and distribution. Besides that, unlike antibodies, peptides are not immunogenic. Therefore, peptides represent the more suitable method of liposomal modification of Doxorubicin. | Inquiry |
| Aptamer-Conjugated Doxorubicin Liposome | Aptamers usually consist of small, single-stranded DNA or RNA sequences that, due to their lack of immunogenicity, ease of preparation and handling, and small size for better penetration, hold great promise as active targeting agents to overcome obstacles to tissues observed in antibody-based systems. The aptamer is usually affixed with a PEG strand and then inserted into liposomes. | Inquiry |
| Carbohydrate-Conjugated Doxorubicin Liposome | Carbohydrates represent one of the major classes of molecules used in liposome decoration. Preparing modified Doxorubicin liposomes, carbohydrates refer to such sugars or sugar-like molecules which have been preponderantly attached on the surface of liposomes encapsulating Doxorubicin. This binding is actually done with a view to enhance selectivity in drug delivery into cancerous cells. The binding of carbohydrates on the surface of liposomes can serve in targeting cancerous cells overexpressing certain carbohydrate-binding proteins or receptors. Carbohydrates commonly employed in coupling are folic acid, mannose, galactose, and hyaluronic acid. | Inquiry |
| CPE-Conjugated Doxorubicin Liposome | Caco-2 cell-penetrating peptides (CPEs) enhance the cellular uptake of liposomal formulations. In this connection, CPE-conjugated doxorubicin liposomes, through their facilitating action in transporting across cellular membranes, present better bioavailability and efficacy. This again is an innovative approach that underlines the need for modification of liposomal systems in order to achieve optimum therapeutic outcomes. | Inquiry |
Doxorubicin Liposome Preparation
The preparation of doxorubicin liposomes involves sophisticated techniques designed to achieve optimal encapsulation and stability. Common methods include:
- Thin-Film Hydration: Lipids are dissolved in organic solvents, then evaporated to form a thin film. This film is subsequently hydrated, forming multilamellar vesicles that can be downsized through sonication or extrusion.
- Extrusion: This method refines liposome size, ensuring uniformity and enhancing the drug's encapsulation efficiency. Liposomes are forced through membrane filters of defined pore sizes to achieve the desired size distribution.
- Dialysis: This process can help remove unencapsulated doxorubicin, ensuring that the liposomes contain the maximum amount of the drug.
At BOC Sciences, we utilize advanced formulations to optimize these processes, ensuring high-quality doxorubicin liposomal products that are both stable and effective.
Liposomal Doxorubicin vs Doxorubicin
The main difference between liposomal doxorubicin and conventional doxorubicin lies in realizing their respective roles in cancer therapy. Conventional doxorubicin is known for its efficiency in treating a wide range of malignancies; however, these drugs were found to be associated with serious adverse drug reactions such as cardiotoxicity, nausea, myelosuppression, among many others. However, the liposomal formulation of doxorubicin was designed to improve its therapeutic index, such as in the case of Doxil.
Doxil Mechanism of Action
Doxil is the first FDA-approved liposomal formulation of doxorubicin, which utilizes a novel stealth technology incorporating PEG to improve the pharmacokinetic profile of the liposome. Coating with PEG reduces opsonization by the immune system, allowing the liposome to circulate longer in the bloodstream and increasing its accumulation in tumor tissues through the enhanced permeability and retention effect. The reason this occurs is that tumor vasculature is generally more permeable than that of normal tissues, allowing the macromolecules-which, in this case, would include liposomes-to preferentially accumulate in the tumor microenvironment. This form of targeted delivery reduces systemic exposure to doxorubicin and, in doing so, it significantly mitigates cardiotoxicity as well as general toxicities associated with conventionally administered doxorubicin. Several studies have proved the clinical efficacy of Doxil, where improved tumor response rates and a favorable safety profile were observed compared to the conventional formulation of doxorubicin.
Advantages of Liposomal Doxorubicin
Liposomal doxorubicin offers several significant advantages over traditional doxorubicin formulations, making it a preferred choice in oncology:
Enhanced Drug Delivery
The pharmacokinetic profile of doxorubicin is improved by liposomes, which prolong the circulation time within the bloodstream. The lipid bilayer protects this drug from degradation and thereby enables its accumulation in tumor tissues through the EPR effect. The aim of this kind of delivery would be to increase the local concentration of the drug at the tumor site with minimum systemic exposure.
Reduced Systemic Toxicity
One of the most important disadvantages to the classical use of doxorubicin is its well-known cardiotoxicity, which is often dose-limiting. The liposomal formulations reduce the cardiotoxicity by a change in the distribution of doxorubicin that decreases the accumulation of the drug in the heart. This allows higher doses for therapeutic purpose with lessened side effects.
Controlled and Sustained Release
The liposomal formulation of such drugs can be engineered to provide a controlled and sustained release of the drug, such as doxorubicin, over an extended period and prolong its action in therapy. This approach minimizes peak and trough concentrations of the drug, thus minimizing peaks and troughs in the therapeutic action and less frequent dosing.
Compatibility with Combination Therapies
Liposomal doxorubicin can also be efficaciously combined in a multi-modality approach with other therapeutic modalities, including immunotherapy, targeted therapies, and radiation. The versatility to be part of multi-modal treatment regimens enhances the effectiveness of the agent with reduced toxicity.
Applications of Liposomal Doxorubicin
- • Research into Oncology: Liposomal doxorubicin finds broad applications in cancer studies. It serves as a tool in tumor biology studies, studies of drug resistance mechanisms, and formulation of new therapeutic approaches. Due to its ability to inhibit the proliferation of cancer cells, it is suitable for preclinical and experimental studies.
- Combination Cancer Therapies: This complex often forms a part of combination therapies of drugs to enhance efficacy. These combination therapies are especially of value in overcoming drug resistance and improving outcomes in advanced cancers.
- Novel Delivery Systems Development: Various modifications of liposomal doxorubicin include thermosensitivity and pH-sensitivity, which are under investigation for advanced delivery systems sensitive to certain tumor microenvironments. Such development increases the localization of the drug with higher efficacy and reduces systemic toxicity.
- Treatment of Specific Cancers: Liposomal doxorubicin has been licensed for use in certain cancers, including breast cancer, ovarian cancer, and Kaposi's sarcoma. Indeed, because of its special properties, different treatment approaches to these malignancies can be developed based on it, ensuring higher response rates and overall effectiveness.
- Animal Studies: Liposomal formulations are also extensively used in preclinical animal models to evaluate therapeutic efficacy and safety before broader application. This research is crucial for understanding how liposomal doxorubicin behaves in vivo and its potential impacts on tumor progression.
Advantages of Doxorubicin Liposomal Products from BOC Sciences
BOC Sciences provides a comprehensive range of liposomal doxorubicin products, characterized by several unique advantages:
- Customization Capabilities: BOC Sciences provides tailored liposomal formulations to meet the specific research needs of customers. This ability of the scientists to tune features like drug loading, surface characteristics, and release kinetics widens the product relevance and applicability in a wide experimental context.
- Rigorous Quality Control: BOC Sciences produces the product by a very strict quality control. Extensive testing is done on each batch of liposomal doxorubicin to ensure high purity, consistency, and stability that meets the requirements of advanced research.
- Expertise and Innovation: With over two decades of experience in the biopharmaceutical industries, BOC Sciences is at the forefront when it comes to the technology of liposomes. It prides itself on a team of experts who continuously seek new ways in which the formulations and delivery methods of doxorubicin are improved, hence making BOC Sciences an industry leader.
- Comprehensive Support: BOC Sciences provides excellent customer support through its technical support and consultation services. Thus, the company is of help to researchers faced with challenges in the selection of formulation and optimization of experimental designs.
Liposomal formulations of Doxorubicin is one of the most important advances in cancer therapy due to its higher efficacy and lower toxicity. BOC Sciences has always kept the leading role in providing innovative solutions with a range of high-quality products for research and preclinical use.
Reference
- K, Aloss.; et al. Modifications of PEGylated liposomal doxorubicin (PLD) surface. Pharmaceutics. 2023, 15(3): 893.
