Improved pDMI Inhaler Formulations

Case ID:

Novel biodegradable, non-toxic nanoparticles that act as stabilizing excipients with a wide variety of suspension drug candidates including polar & non-polar drug particles, bio-macromolecules (proteins/peptides), gene therapies (DNA/siRNA) as well as amorphous and crystalline therapeutics have been developed which provide a platform for improving insoluble drug delivery. A large variety of approaches have been developed at WSU aimed at increasing the effectiveness of pressurized meter-dose inhalers (pMDIs) through improved aerosol characteristics, drug stability and reduced biotoxicity. Dr. Sandro da Rocha has been researching novel oral inhalation formulations and methods relevant in numerous pulmonary drug delivery markets including asthma, COPD, and lung cancer. Novel nanoparticle-based drug compositions have been shown to greatly improve and expand therapeutic drug delivery to the lungs through pressurized meter-dose inhalers (pMDIs).  Some of these technologies can also be applied to dry powder inhaler.

  Stage of Development:  Pre-Clinical

• in vivo animal studies (mice) confirm lung deposition characteristics and low inflammation potential
• in vitro studies on Calu-3 cells (cultured human airway epithelial cells) &  A549 cells (human lung adenocarcinoma cell line, model of Type II alveolar epithelium)
• complete aerosol characterization using Anderson Casade Impactor (ACI) and other methods

Benefit Analysis:
While patient compliance is a big issue, pMDIs are still the most frequently prescribed inhaler device in the world. The technologies developed at WSU directly address the challenge of reformulation pMDI drugs from traditional CFC propellants to more environmentally friendly Hydrofluorakane (HFA) propellants.  Especially for new and insoluble active pharmaceutical ingredients there is a limited selection of excipients compatible with HFA and safe for human use.

Patent Status: Multiple Patents Pending
• 13/129,804 “Nanoparticles and Porous Particles and Methods of Making the Same”
• 13/129,803 “Method for Engineering Porous Particles for Aerosol Formulations for Pulmonary Drug Delivery”
• 12/741,021 “Method for Engineering Polar Drug Particles with Surface-Trapped Hydrofluroalkane-Philes”
• 12/738,826 “Co-polymer Stabilizers For Hydryfluoroalkane Dispersions”

Licensing Opportunity:  WSU is looking for a commercial partner for the portfolio of inhaler technologies to develop optimal pMDI formulations that would enhance effectiveness of delivery, reduce cost (lower drug dose) and could be developed in coordination with clinical trials for new drugs that are not compatible with existing formulations.

“Propellant-based inhalers for the non-invasive delivery of genes via oral inhalation” DS Conti et. al. JOURNAL OF CONTROLLED RELEASE, 157 (3), pp 406-417
2011 "Nanoparticle Stabilized Compressible Hydrofluoroalkanes" L. Wu & S.R.P. da Rocha, LANGMUIR , 27, pp 10501-10506.
2010 "The potential for the noninvasive delivery of polymeric nanocarriers using propellant-based inhalers in the treatment of Chlamydial respiratory infections", B. Bharatwaj et. al. BIOMATERIALS, 31, pp 7376-7385.
2008 "Core-shell Particles for the Dispersions of Small Polar Drugs and Biomolecules in Hydrofluoroalkane Propellants" L. Wu et. al. PHARMACEUTICAL RESEARCH, 25, pp 289-301.
2008 "Novel Propellant-driven Inhalation Formulations: Engineering Polar Drug Particles with Surface-trapped Hydrofluoroalkanephiles", L. Wu et. al.  EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 33(2), pp 146-158.
2008 "Biocompatible and Biodegradable Copolymer Stabilizers for Hydrofluoroalkane Dispersions: A Colloidal Probe Microscopy Investigation" L. Wu & S.R.P. da Rocha, LANGMUIR, 23(24), pp 12104-12110.


Patent Information:
For Information, Contact:
Nicole Grynaviski
Commercialization Principal
Wayne State University
Sandro Da Rocha
Libo Wu
Drug Delivery