APR Nov/Dec 2022 - 63

« DRUG DELIVERY
It should be noted that the three mentioned excipients would typically
not be used in isolation; amino acids, and specifically leucine types, are
commonly utilized in academic research to enhance the aerosolization
properties of spray dried particles
3.
Shur J., Price R., Lewis D., Young P. M., Woollam G., Singh D., Edge S., From single excipients
to dual excipient platforms in dry powder inhaler products, International Journal of
Pharmaceutics, Volume 514, Issue 2,2016, https://www.sciencedirect.com/science/
article/pii/S037851731630446X
for pulmonary drug delivery.
During the spray drying process, leucine molecules accumulate at
the surface of droplets with their hydrophobic part facing the gas
phase. When the concentration of leucine increases at the surface and
supersaturation is achieved, leucine crystallizes at the outer surface,
forming a shell. This benefits the aerosolization performance, as it
results in lower cohesion forces within the particles. Figure 2 shows a
graphical representation of the spray drying process of a biologic with
a disaccharide and leucine. Disaccharide molecules shield the biologic,
while leucine accumulates at the surface and has more impact on the
physical surface properties of the spray dried powder.
Embracing the Potential of NextGeneration
Inhaled Medications
10.
Drug developers are expanding the use of inhaled medications in a bid
to tackle unmet medical needs. However, with high-dose medications
and biologics being unsuited to the carrier-based DPI model, this new
dawn requires new formulation processing techniques.
Spray drying is emerging as one of the most promising carrier-free
technologies and has already yielded important
results. Careful
consideration of excipient use within this emerging area of interest
can help developers create bespoke formulations that meet the
characteristics of the API and the needs of the patient alike.
As discussed in this article, the field of pulmonary delivery is expanding
from small molecule delivery to biologics and from low dose to high
dose formulations. The authors believe that this is just the start in
targeting the delivery of new and existing medicine to the lungs.
This shift is occurring now, for example, inhaled cannabinoids can
deliver higher efficacy at lower doses than orally delivered products.
This approach has shown some promise in therapy areas, such as
cancer treatment-associated nausea, depression, anxiety, migraine,
and pain, among others.9
Researchers in lung cancer,10
hypertension,11 and Alzheimer's disease12
pulmonary
are also investigating the
benefits of pulmonary delivery. All in all, it's an exciting and promising
moment in this field.
References
1.
2.
11.
4.
5.
6.
7.
Air Physio. How Does Mucociliary Clearance Work - Mucus Clearance and Removal. (2018).
Available at: https://www.airphysio.com/mucociliary-clearance-and-removal/
GlobalData, Future of Pharma - Looking Ahead to 2022: https://store.globaldata.com/
report/future-of-pharma-insight-analysis/
Liang, W., Pan, H. W., Vllasaliu, D., & Lam, J. K. (2020). Pulmonary delivery of biological
drugs. Pharmaceutics, 12(11), 1025. https://www.mdpi.com/1999-4923/12/11/1025
Thomas, F. (2021). Taking a Breath: Advances in Inhaled Biologics The inhaled route
of administration for biologics is experiencing renewed interest, particularly in light
of the COVID-19 pandemic. BIOPHARM INTERNATIONAL, 34(4), 18-+.https://www.
biopharminternational.com/view/taking-a-breath-advances-in-inhaled-biologics
8.
9.
Healy A. M., Amaro M. I., Paluch K. J., Tajber L., Dry powders for oral inhalation free of
lactose carrier particles, Advanced Drug Delivery Reviews, Volume 75, 2014, https://www.
sciencedirect.com/science/article/pii/S0169409X14000702
National Academies of Sciences, Engineering, and Medicine. (2017). Therapeutic effects
of cannabis and cannabinoids. In The health effects of cannabis and cannabinoids: The
current state of evidence and recommendations for research. National Academies Press
(US). https://www.ncbi.nlm.nih.gov/books/NBK425767/
Rosière, R., Berghmans, T., De Vuyst, P., Amighi, K., & Wauthoz, N. (2019). The position of
inhaled chemotherapy in the care of patients with lung tumors: clinical feasibility and
indications according to recent pharmaceutical progresses. Cancers, 11(3), 329. https://
www.ncbi.nlm.nih.gov/pmc/articles/PMC6468657/#:~:text=associated%20with%20
chemotherapy.-,Inhaled%20chemotherapy%20has%20been%20proved%20to%20be%20
feasible%20and%20safe,systemic%20toxicities%20are%20consequently%20reduced.
Hill, N. S., Preston, I. R., & Roberts, K. E. (2015). Inhaled therapies for pulmonary
hypertension. Respiratory Care, 60(6), 794-805. https://pubmed.ncbi.nlm.nih.gov/26
070575/#:~:text=Accordingly%2C%20a%20number%20of%20inhaled,as%20a%20
continuously%20nebulized%20medication.
12. Alzheimer's Society. New research shows promise for Phase 2/3 trial of inhaled insulin
in people with MCI or mid Alzheimer's disease - Alzheimer's Society comment. (2019).
Available at: https://www.alzheimers.org.uk/news/2019-07-17/new-research-showspromise-phase-23-trial-inhaled-insulin-people-mci-or-mid
Author
Biographies
Pauline van der Wijst-Janssen is a Product Application
Specialist at DFE Pharma. She has been working on
application development of excipients based upon
fundamental knowledge of excipients and powder physics.
She joined DFE Pharma in 2017 and worked as a product developer and
application specialist on multiple OSD and DPI projects. Pauline holds
a Master's Degree (cum laude) in Physical Chemistry from the Radboud
University in Nijmegen, with an additional specialization in Science,
Management and Innovation. Since April 2022, she is also affiliated with
the University of Groningen with a PhD student position.
Jardim, J. R., & Nascimento, O. A. (2019). The importance of inhaler adherence to
prevent COPD exacerbations. Medical Sciences, 7(4), 54. https://www.mdpi.com/20763271/7/4/54
Peng,
T., Lin, S., Niu, B., Wang, X., Huang, Y., Zhang, X., ... & Wu, C. (2016). Influence
of physical properties of carrier on the performance of dry powder inhalers. Acta
pharmaceutica sinica B, 6(4), 308-318. https://www.ncbi.nlm.nih.gov/pmc/articles/
PMC4951591/
Ross Blezard is a Product Application Specialist for
Biopharmaceuticals. He brings extensive experience in the
development of inhalation drug products and material
characterization, and has previously held positions
including Head of formulation development for a UK based CDMO and
Senior Scientist (Physical sciences) for a global leader in the food and
pharmaceutical industries.
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