The DBCO groups on these liposomes enable the use of copper-free click chemistry to conjugate azide-bearing targeting molecules, such as antibodies or peptides. This technology allows for precise targeting of the liposomes to specific cells or tissues, potentially enhancing the therapeutic efficacy of the encapsulated doxorubicin.
These liposomes allow for targeted delivery of doxorubicin, which can lead to higher drug concentrations at the tumor site while reducing systemic exposure and toxicity. Additionally, the encapsulation in liposomes can improve the solubility and stability of doxorubicin in the bloodstream.
The preparation involves mixing DBCO-functionalized lipids with doxorubicin-loaded liposomes under specific conditions that facilitate the conjugation of DBCO with azide-tagged molecules. This typically includes incubation at controlled temperatures and may involve dialysis to remove unreacted components.
DBCO-Doxorubicin liposomes should be stored at 4°C and protected from light. Freezing should be avoided as it can disrupt the liposome structure and release the encapsulated drug prematurely.
Yes, these liposomes can be tailored for different research applications by varying the type and density of azide-modified targeting molecules conjugated to the surface. This allows researchers to target different types of cells or tissues depending on the therapeutic needs.
Assessment of p700 coupling to PEGylated liposomes
This research investigates the enhanced targeting and cytotoxicity of doxorubicin encapsulated in PEGylated liposomes modified with a dibenzocyclooctyl (DBCO) functional group and linked to a TIMP3-derived peptide, p700. The modification aims to target the liposomes specifically to tumor cells, utilizing p700's affinity for multiple angiogenesis-related receptors highly expressed on tumor and vascular cells.
The experimental results demonstrated that p700-conjugated liposomes significantly improved the binding and internalization of doxorubicin in tumor cells compared to non-conjugated liposomes. In human and mouse breast cancer cell lines, the p700-conjugated complex facilitated a roughly 100-fold increase in drug uptake, resulting in heightened cytotoxic effects. This targeting strategy not only promises to enhance the efficacy of doxorubicin against tumors but also to reduce its cardiotoxic side effects by limiting systemic exposure. Overall, the use of p700 to direct the delivery of liposomal doxorubicin marks a pivotal advancement in cancer therapy, focusing on increasing the drug's tumor specificity and therapeutic index while mitigating associated risks.
Aldughaim, M. S., Muthana, M., et al. Specific targeting of PEGylated liposomal doxorubicin (Doxil®) to tumour cells using a novel TIMP3 peptide. Molecules. 2020, 26(1): 100. Under Open Access license CC BY 4.0, without modification.
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