Formulation of HDACi Loaded ß-Cyclodextrin-poly (ß-amino ester) Nanoparticles

Description:

Researchers have developed a novel formulation strategy to encapsulate molecules, including but not limited to histone deacetylase inhibitor (HDACi) drugs in nanoparticle networks composed of beta-cyclodextrin-poly(beta-amino esters). Advantages of this system include high loading capacity, increased in vivo tolerability, sustained release, and improved drug distribution and activity in the treatment of solid tumors.

Technology Overview

A beta-cyclodextrin-based, cross-linked polymer is employed in the formulation as a novel excipient instead of conventional diblock copolymers like PLGA and PLA-PEG. This pre-synthesized polymeric network forms particles in aqueous medium that are in the range of 100-500nm with defined polydispersity. Simply doping the drug at a desired concentration, followed by mechanical agitation, leads to the formulation of drug bound nanoparticles through self-assembly. The particles can then be retrieved and concentrated with subsequent lyophilization.

Benefits/Technology Advantages

- Simpler loading strategy compared to previously studied techniques that does not require physical manipulation to optimize (i.e. no temperature or pH changes needed)

- Higher drug loading capability per nanoparticle (8 wt% or more in terms of drug to excipient ratio)

- Novel mechanisms of drug loading and release are a particular benefit to drugs with ionizable moieties

- Unique surface chemistry improves modularity of the system for further engineering, including attachment of surface targeting ligands or imaging agents

Potential Applications

- Sustained drug release

- Oncology, Neuro-oncology, Trauma, Inflammation, Neuro-Immunology, Neurodegeneration, HIV/AIDs, Cardioprotection

Lead Inventor

Rachael Sirianni, Ph.D.: Her research is focused on the development and translation of novel therapeutics for the treatment of pediatric brain tumors.

Intellectual Property Status