Arsenic Encapsulation and Triggered Release for Cancer Treatment (25053)

Novel procedures and compositions for the encapsulation and delivery of arsenic drugs.

SIGNIFICANCE: Despite its long history and excellent therapy, arsenic compounds have a variety of widely appreciated toxic side effects, which currently limit their application. The invention presented here provides a novel procedure for encapsulating arsenic compounds in liposomes allowing greater exploitation of the arsenic’s beneficial characteristics while reducing its toxicity. The encapsulated compounds can also be targeted to a particular diseased tissue by coupling the liposome with an antibody to a cell specific antigen. Additionally, the ability of these liposomes to maintain encapsulation over long periods of time make them a realistic improvement for arsenic therapy.

BACKGROUND: Liposomes have been widely used as carriers for a variety of agents from drugs to genetic material. Loading drugs into liposomes is a critical step in their delivery. Although water soluble drugs readily load into the interior of liposomes, amphipathic drugs are the most difficult to retain and can readily permeate through lipid bilayers. Arsenic trioxide (As2O3), and various other arsenic containing compounds, were used to assess loading and release of encapsulated material. The loading methodology presented by the inventors results in efficient drug incorporation, combined with the ability to control the rate of drug release. Stability experiments conducted out to six months show these compositions retain greater than 95% of the initial drug concentration.

Since targeting a drug to a specific diseased cell can enhance its therapeutic impact, drug-containing liposomes were coupled to an antibody specific for an antigen found on select B-lymphomas. Using a B-lymphoma cell line expressing this particular antigen, the antibody coupled/As2O3 encapsulated liposome targeted delivery to those cells with greater efficiency than control liposomes. This further demonstrates the value the technology provides toward improving the medicinal application of arsenic containing compounds.

STATUS: A patent application has been filed and Northwestern University is interested in licensing this technology.

Type of Offer: Licensing



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