BROADLY APPLICABLE

Our approach and technologies can be applied to potent small molecules, peptides, or even proteins.

Importantly, only a few families of carrier molecule designs are needed to bind and satisfy most drug candidate requirements. Also, carrier design and binding chemistries can be manipulated to create new therapeutic approaches .

UNIQUE, AFFINITY-BASED DRUG RELEASE:

Our approach focuses on releasing a drug payload from our carrier molecules appropriately, not just "slow-release" over time. See Affinity-based drug delivery page for details.

NEW DRUG FORMULATIONS CREATED QUICKLY:

Our drug delivery carrier molecules, are designed to imbue optimal, desired drug characteristics. For example,optimize drug pharmacokinetics may need improvement, or drug solubility and bioavailability may be the objective.

Our platform is flexible and can formulate new therapies in months, not years that are often needed. Many drug payloads may be loaded and reformulated in a matter of a few months. Other drugs needing carrier or binding chemistry manipulation can be formulated in four to six months, typically. After a formulation has been created and characterized, the new drug formulation is ready for validation in the appropriate in vitro and/or in vivo model system prior to IND preparation and filing.

Using our reversible binding approach to drug loading (to a carrier) may also minimize the amount of toxicity and clinical testing required when approved drugs are formulated with PGC carriers - potentially reducing laboratory and regulatory costs and accelerating time to market.

BIOCOMPATIBLE, BIODEGRADABLE, NON-TOXIC, NON-IMMUNOGENIC:

Our carrier molecules - due to their chemical design and composition - are expected to be non-toxic, non-immunogenic, and have broad capability. Additionally, the fundamental platform has been tested in phase I human studies and shown to be safe (Callahan et al., AJR, July 1998).

COMPARISON TO PEGYLATION, "STEALTH" LIPOSOMES

PharmaIn's patented drug delivery technologies advance upon delivery systems and technologies currently used to improve drug characteristics, including PEGylation, "Stealth" liposomes, or direct chemical modification of a given drug.

Versus PEGylation:

PEGylation is the chemical attachment of polyethylene glycol chains or "PEGs" to drug molecules that shield therapeutic molecules. This often leads to decreased biological activity of the active agent (protein) being PEGylated - to the point where some proteins just are not amenable to PEGylation.

Also, unlike direct PEGylation, appropriate small molecules, peptides, or proteins can be attached to PGC carrier through reversible binding (our PRB technology), avoiding alteration of the therapeutic molecule and potentially reducing active agent activity.

In addition, scientific concern has been expressed about the apparent accumulation of conventional PEG molecules in the body. Large PEG molecules used to PEGylated proteins are not readily cleared and may accumulate in vital organs such as the kidneys, with uncertain and potentially troublesome effects. Scientific concerns regarding PEG accumulation are greatest in treatment regimens where relatively high doses or frequent administrations of therapeutics are necessary, such as in cancer cases, potentially limiting drug dose to less than optimal.

Our platforms do not use large PEG molecules and thus alleviate the safety concern over the use of large PEG molecules.

Versus "Stealth" Liposomes:

Stealth liposomes primarily involve the encapsulation of therapeutic molecules in lipids shielded by PEG molecules, also serving to enhance and deliver the medicines. This alternative drug delivery technology is typically useful for small molecules. Our platform has broader application and often requires less harsh conditions to formulate a drug - further preserving drug activity.

TARGETED TISSUE ACCUMULATION

PGC carrier molecules can be designed to preferentially accumulate in areas of enhanced vascular permeability, e.g. certain inflammation and tumor sites. PGC carrier molecules have a larger size (~10nm) than PEGylated molecules (few nanometers) and smaller than Stealth liposomes (~100nm), and PGC can carry hundreds molecules (vs. PEGylation with usually just one molecule) of drug payload.

Comparison of Size