Overview
Nanomedicine encompasses a wide variety of formulations including polymeric nanoparticles, liposomes, lipid nanoparticles, micelles, polymersomes, nano-emulsions, nanotubes, and nanofibers. These nano-sized constructs can be used to overcome drug delivery challenges such as drug solubilization, API targeting, protection of sensitive APIs from degradation and/or immune responses, and API transport across biological barriers. This webinar will focus on biodegradable polymeric nanoparticle formulations and the products and processes required for achieving sub-micron particle sizes.
Many traditional microparticle applications rely on copolymers of lactide and glycolide (LG polymers) for controlled and/or sustained release. Nanoparticles of LG polymers, while also potentially imparting some level of controlled drug release, are intended to effect targeted delivery of an API to a desired location rather than sustained systemic delivery. The amount of applied energy required to generate particles in the nanometer range can be reduced by incorporating a poly(ethyleneglycol) (PEG) block into the LG polymer chain. While traditional LG polymers can be used, the amphiphilicity imparted by PLA-PEG di-block copolymers, makes them especially suited for nanoparticle formation. By adjusting the relative molecular weight of the mPEG and poly(DL-lactide) blocks, the excipient properties and formulation properties can be carefully tuned.
While excipient quality and security of supply is paramount, the process by which nanoparticles are made is also critical to the end drug product. Current processes include high-pressure homogenization, high-shear mixing, probe sonication, and microfluidics, among others, which often result in temperature and pressure elevations that are detrimental to sensitive APIs and high-shear forces that can cause nanoparticle deformation and aggregation. The process scale limitations also inherent to these batch processes severely limit their applicability to commercial-scale and peptide/protein-based nanoparticle formulations. As a result, regulatory agencies continue to push for continuous nanoparticle processes with robust scale-up potential.
Learning Objectives
- The current limitations of nanoparticle manufacturing and how to overcome them
- The benefits of PLA-PEG block copolymers for nanoparticle formation
