Self-Assembling Drug-Amphiphiles: A New Platform for the Delivery of Anticancer Chemotherapeutics

UNMET NEED
Many anticancer drug delivery systems suffer from lack of target specificity and drug-loading limitations. Additionally, many drug delivery systems require the use of a nanocarrier, which have certain disadvantages including limitations on the amount of loaded drug and batch to batch variability. This invention is a self-assembled drug-amphiphile that releases anticancer drugs under tumor-relevant conditions.

PROBLEM SOLVED
Johns Hopkins researchers have developed a novel, self-assembled amphiphiles for drug delivery. This method does not require the addition of nanocarriers, as the anticancer drug itself self-assembles into a nanostructure. Proof of concept was done wiht the amphiphile consisting of an anti-cancer drug conjugated to a peptide via degradable hydrophilic linker. In water, these amphiphiles form well-defined, drug-loaded nanostructures. These drugs are shown to be cytotoxic to many cancer cell lines in vitro (breast cancer, ovarian cancer, brain cancer, etc.). The modified drug molecules self assemble into discrete nanostructures, which release the payload drug in the presence of a tumor. This method of drug delivery allows for high and finely controlled drug loading. Additional advantages of this technology include:

• Modified drug molecule may contain one or more types
• Drug-amphiphile nanostructures self-deliver
• High drug loading (>20%)
• Potentially prevent premature degradation, increase absorption, modify clearance pharmacokinetics, increase tissue selectivity and allow intravenous or oral delivery of poorly soluble hydrophobic agents or water0soluble prodrugs.
• Importantly, this invention may offer the opportunity to reformulate discontinued drugs because of their poor bioavailability, lack of selectivity to a desired target tissue or extreme toxicity.

STAGE OF DEVELOPMENT
The technology is at the preclinical stage of development. The inventors characterized the cytotoxic effect of the Drug-Amphiphiles containing 1,2,4 molecules/per complex in several cancer cell lines. nanostructures show effective in vitro cytotoxicity against numerous cancer cell lines, including breast cancer, brain cancer, ovarian cancer, etc.

ASSOCIATED PUBLICATIONS
■ J Am Chem Soc. 2013 Feb 27;135(8):2907-10 ■

TECHNOLOGY CLASSIFICATION
Primary Category: Drug Delivery

Category(s):