Polymeric Nanoparticles for Targeted Delivery

Polymeric nanoparticles (PNPs) are a game-changing solution for delivering diagnostic and therapeutic agents, including small molecules, peptides, proteins, and nucleic acids. By incorporating these active pharmaceutical agents (APIs) into biodegradable polymer nanoparticles, we unlock a multitude of benefits that enhance their therapeutic effects.

The following are some advantages of PNPs:

• Protects API from degradation
• Extends drug release and circulation time
• Improves solubility and bioavailability
• Enables conversion of oral formulations
• Enhances cell uptake and intracellular delivery
• Facilitates targeted delivery for optimal outcomes

At Phosphorex, our team of experts have experience in two types of Targeting for PNPs:

Passive Targeting: Unlocking the Power of Enhanced Permeability and Retention (EPR) Effect
Passive targeting offers a remarkable strategy to deliver therapeutic agents precisely to tumor sites. By leveraging the enhanced permeability and retention (EPR) effect, we can capitalize on the compromised vasculatures of tumor tissues, effectively trapping particles in the size range of 10 – 500 nm.

The success of passive targeting hinges on circulation time, which is heavily influenced by the surface characteristics of drug-loaded nanoparticles. That's where PEGylation comes into play. PEGylation has proven to be a highly effective method for extending the circulation time of nanoparticles, enhancing their overall performance.

Active Targeting: Unleashing the Potential of Nanoparticle-Mediated Drug Delivery
By physically coating or chemically conjugating targeting agents onto the surface of drug-loaded nanoparticles, we achieve remarkable active targeting. This approach ensures that the drug reaches its intended destination while shielding it from degradation until release.

Our expertise lies in utilizing biodegradable polymers such as polylactide (PLA), poly(lactide-co-glycolide) (PLGA), polycaprolactone (PCL), and their copolymers with polyethylene glycol (PEG) to encapsulate APIs for delivery. These materials enable optimal drug release and therapeutic efficacy.

At Phosphorex, we offer a comprehensive range of services to support active targeting:

• Creative formulations and robust processes to load drug molecules into nanoparticles of various sizes, including particles smaller than 100 nm
• Solutions for modifying the physical characteristics of nanoparticle surfaces to enhance targeting effectiveness
• Multiple conjugation routes to covalently bind targeting antibodies to nanoparticle surfaces using either conventional EDC chemistry or click chemistry approaches
• Fluorescent labeling options for in vivo imaging, where a fluorescent dye is encapsulated inside the nanoparticle matrix or conjugated to the nanoparticle surface

Analytical Capabilities:

Formulation, process development, and analytics are interconnected. Advancing analytical method development in a stage appropriate manner is critical to ensure success of program from feasibility to clinical manufacture. Phosphorex’s analytical services for sustained release drug delivery systems include API characterization, physical characterization, and development stability studies.

Contact us at bd@phosphorex.com and let’s explore your potential delivery method together for PNPs.