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publicationNumber US-2008227722-A1
titleOfInvention Targeted Drug Delivery of Pain and Addiction Therapies Using Opioid Receptor-Mediated Internalization
abstract Drug delivery is targeted to new opioid receptors using receptor-mediated internalization. Dermorphin was successfully conjugated to DSPE-PEG3400 without affecting the affinity to its receptor. The synthesized conjugate was inserted into preformed sterically stabilized liposomes to obtain dermorphin-grafted SSL. DSPE-PEG34Qo-dermorphin and dermorphin-SSL retained their affinity and selectivity for MOR. Moreover, dermorphin-SSL and encapsulated probes were taken up by CHO-hMOR cells, but not by naive CHO cells or very closely related CHO-hDOR cells. Dermorphin-SSL can be used to deliver drugs to the intracellular component of intended cells with high fidelity. Therefore, dermorphin-SSL is useful to carry pharmaceutical agents to achieve region-specific delivery of analgesics and/or to attenuate side effects associated with opioids.
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