Phosphorex accelerates development of nanomedicines by fabricating nanoparticles, modifying their surface for different targeting needs, scaling up to support preclinical and IND-enabling studies and developing GMP processes.
Without effective targeting, many drugs such as chemo agents, immune-modulators and nucleic acids, cannot fully realize their therapeutic potential and may cause adverse effects. Nanoparticles, whether polymeric or lipid-based, have the potential to address these challenges via either passive or active targeting.
Passive Targeting
The enhanced permeability and retention effect (EPR-effect) can be leveraged for passive targeting of therapeutic agents to tumor sites. This effect results from the compromised vasculatures of tumor tissues which can trap particles in the size range of 10 – 500 nm.
The success of passive targeting is directly related to circulation time, which is influenced by the surface characteristics of drug-loaded nanoparticles. For example, the surface of drug-loaded nanoparticles may be treated with a hydrophilic entity so they can circulate in the blood for an extended period of time and have a better chance to reach the intended target.
One such approach is PEGylation, in which polyethylene glycol is added to the surface of nanoparticles. PEGylation can be accomplished by either including a PEG copolymer into the starting formula of the nanoparticle preparation or by coating or conjugation of PEG units following the production of the nanoparticles.
Active Targeting
Nanoparticle-mediated targeted drug delivery can be achieved by physically coating or chemically conjugating a targeting agent onto the surface of drug-loaded nanoparticles. In addition to targeting, nanoparticles shield the drug from degradation by enzymes and other factors until they are released by the particles at the destination site.
Polymeric nanoparticles used to encapsulate APIs for delivery include biodegradable polymers such as polylactide (PLA), poly(lactide-co-glycolide) (PLGA), polycaprolactone (PCL) and polyethylene glycol (PEG).
Phosphorex offers innovative approaches for active targeting including:
- Creative formulations and robust processes to load drug molecules into nanoparticles of various particle sizes, including particles in the 10-100 nm range to extend circulation time
- A range of conjugating routes to covalently bind targeting antibodies to the surface of nanoparticles based on either conventional EDC chemistry or a click chemistry approach
- A novel, robust and more economically feasible process to anchor a targeting agent – either a peptide, protein, polymer or surfactant – on the surface of drug-loaded nanoparticles without chemical conjugation
- Fluorescent labeling for imaging in which a fluorescent dye is either encapsulated inside the nanoparticle matrix or conjugated to the surface the nanoparticles, enabling in vivo imaging of the nanoparticles
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