Nanodiamond-Based Anti-HIV Drug Delivery – IP 1617

Human immunodeficiency virus type1 (HIV-1) remains one of the leading causes of death worldwide, principally indeveloping countries. Although therapeutic agents exist for the treatment ofHIV-AIDS, drug-induced toxicities and pharmacokinetic limitations commonlyresult in poor compliance and disease related complications such as, forexample, HIV-associated neurocognitive disorders (HAND). HAND is one of themost common manifestations of HIV-1 pathogenesis that causes cognitiveimpairment and other CNS-related disorders. For treating disorders such asHAND, delivery of therapeutic agents to the CNS remains a major challenge,primarily due to the ineffective transmigration of drugs through theblood-brain barrier (BBB). In recent years, the advent of nanomedicine hasstimulated the development of innovative systems for drug delivery. However,clinical success has been limited due to problems associated withbiocompatibility, sustainability, and cytotoxicity of the drugs. FIU inventors have developedpharmaceutical compositions and methods for the delivery of Efavirenz to HIVreservoir organs. The compositions comprise nanodiamond particles that aresmall enough (less than 10 nm in diameter) to penetrate the tight junctions ofthe BBB and subsequently migrate to selected treatment areas. The surface ofthe ND particles can be electrostatically charged, facilitating the adsorptionof various therapeutic and/or diagnostic agents having positive or negativecharges. Optionally, the surface of the ND particles can be chemically modifiedwith functionalities such as, for example, carboxylic acid, lactone, ketone,ether, hydroxyl, and/or amine. Furthermore, biological molecules such as, forexample, amino acids, proteins, cells, hormones, vitamins, DNAs, siRNAs,antibodies, and RNAs, can be adsorbed or covalently attached to the NDparticles’ surfaces without altering their biological activities. Finally, theincreased drug-loading capacity attributed to ND particles’ large surface areacan lead to more sustained drug release profile and improve drug dosingregimens. Anne Laure Schmitt Olivier 305-348-5948

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