Targeted drug products have been a key objective of pharmaceutical development, especially since the advent of monoclonal antibodies. These targeted pharmaceuticals are typically composed of monoclonal antibody-drug conjugates (ADC). ADC technologies, however, do have several challenges that have limited and slowed their development and commercial use. These challenges include: 1) inflexibility in altering the ratio of targeting biopharmaceutical (i.e., antibody) to the drug component, 2) inefficiency in linking soluble biopharmaceuticals to hydrophobic pharmaceuticals, 3) limited compatible conjugation chemistries that can deliver and then release pharmaceuticals to tissue targets, and 4) a business model that often revolves around propriety linkers and its related business terms. New formulation technologies that use nanoparticles can circumvent these limitations. Nanoparticles with hydrophobic interiors and charged surfaces can formulate and “link” both hydrophobic and hydrophilic pharmaceuticals and biopharmaceuticals. These hydrophobic nanoparticles are composed of mixtures of solid and liquid lipids, resulting in particles that efficiently encapsulate lipophilic pharmaceutical agents and/or useful research markers: for example paclitaxel and hydrophobic fluorochromes, respectively. It has been demonstrated by the authors and other researchers that more than one hundred different APIs can be encapsulated by these kinds of solid lipid nanoparticles (SLNP). Physicochemical attributes, like surface charge or zeta potential, of SLNP can be tailored by inclusion of surfactants into the formations. The resulting particle surfaces can interact with either the hydrophobic or electrostatically-charged domains of amphipathic and hydrophilic molecules. These particles have been demonstrated to efficiently bind to and be coated by pharmaceuticals and biopharmaceutical molecules like vaccine antigens, adjuvants, microbial TLR-agonists, and are being developed for monoclonal antibodies that target tumor cells and other tissues. These nanoparticle formulations effectively link biopharmaceutical and pharmaceutical molecules, like that of ADC, but without the need for and limitations of conjugation chemistries. This can result in final products with unique and useful physicochemical and biological attributes including, improved vaccine potency and safety, and targeted pharmaceutical and biopharmaceutical drugs directed against specific disease targets.

Nanoparticle formulations linking pharmaceutical components by electrostatic and hydrophobic binding: A faster and more flexible alternative to ADC

249th National Meeting (2015)

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