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Proceeding Paper

Application of the Quality-by-Design (QbD) Approach to Improve the Nose-to-Brain Delivery of Diazepam-Loaded Nanostructured Lipid Carriers (NLCs) †

by
Cláudia Pina Costa
1,*,
Sara Cunha
1,
Andreia F. Peixoto
2,
João Nuno Moreira
3,4,
José Manuel Sousa Lobo
1 and
Ana Catarina Silva
1,5
1
UCIBIO/REQUIMTE, MEDTECH, Laboratory of Pharmaceutical Technology, Department of Drug Sciences, Faculty of Pharmacy, University of Porto, 4099-002 Porto, Portugal
2
LAQV/REQUIMTE, Department of Chemistry and Biochemistry, Faculty of Sciences, University of Porto, 4169-007 Porto, Portugal
3
CNC—Center for Neuroscience and Cell Biology, Center for Innovative Biomedicine and Biotechnology (CIBB), Faculty of Medicine (Pólo I), University of Coimbra, 3004-531 Coimbra, Portugal
4
UC—University of Coimbra, CIBB, Faculty of Pharmacy, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal
5
FP-ENAS (UFP Energy, Environment and Health Research Unit), CEBIMED (Biomedical Research Centre), Faculty of Health Sciences, University Fernando Pessoa, 4249-004, Porto, Portugal
*
Author to whom correspondence should be addressed.
†
Presented at the 1st International Electronic Conference on Pharmaceutics, 1–15 December 2020; Available online: https://iecp2020.sciforum.net/.
Proceedings 2021, 78(1), 40; https://doi.org/10.3390/IECP2020-08658
Published: 1 December 2020
(This article belongs to the Proceedings of The 1st International Electronic Conference on Pharmaceutics)
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Abstract

The intranasal administration of nanostructured lipid carriers (NLCs) has been suggested as a promising strategy to improve the fast treatment of epilepsy. This route allows for drug passage directly from the nose to the brain, avoiding the need of bypassing the blood–brain barrier. In addition, the quality-by-design (QbD) approach is a useful tool for the optimization of manufacturing variables, resulting in effective and safe pharmaceutical formulations. The aim of this work was to use the QbD approach to optimize a NLCs formulation for the nose-to-brain delivery of diazepam. The studies began with the screening of excipients and the assessment of the lipid-drug compatibility. The central composite design was used to evaluate the effects of critical material attributes (CMAs) (ratio of solid and liquid lipids and the amount of drug and emulsifiers) on the CQAs of the diazepam-loaded NLCs formulation (particle size, polydispersity index (PDI), zeta potential (ZP) and encapsulation efficiency (EE)). The results showed that the most adequate ratios of lipids and emulsifiers were 6.65:2.85 and 4.2:0.3 (%, w/w), with values of 84.92 nm, 0.18, −18.20 mV and 95.48% for particle size, PDI, ZP and EE, respectively. This formulation was selected for further studies related to the optimization of critical process parameters (CPPs).
Keywords: epilepsy; nose-to-brain delivery; intranasal delivery; nanostructured lipid carriers; quality-by-design epilepsy; nose-to-brain delivery; intranasal delivery; nanostructured lipid carriers; quality-by-design

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MDPI and ACS Style

Costa, C.P.; Cunha, S.; Peixoto, A.F.; Moreira, J.N.; Lobo, J.M.S.; Silva, A.C. Application of the Quality-by-Design (QbD) Approach to Improve the Nose-to-Brain Delivery of Diazepam-Loaded Nanostructured Lipid Carriers (NLCs). Proceedings 2021, 78, 40. https://doi.org/10.3390/IECP2020-08658

AMA Style

Costa CP, Cunha S, Peixoto AF, Moreira JN, Lobo JMS, Silva AC. Application of the Quality-by-Design (QbD) Approach to Improve the Nose-to-Brain Delivery of Diazepam-Loaded Nanostructured Lipid Carriers (NLCs). Proceedings. 2021; 78(1):40. https://doi.org/10.3390/IECP2020-08658

Chicago/Turabian Style

Costa, Cláudia Pina, Sara Cunha, Andreia F. Peixoto, João Nuno Moreira, José Manuel Sousa Lobo, and Ana Catarina Silva. 2021. "Application of the Quality-by-Design (QbD) Approach to Improve the Nose-to-Brain Delivery of Diazepam-Loaded Nanostructured Lipid Carriers (NLCs)" Proceedings 78, no. 1: 40. https://doi.org/10.3390/IECP2020-08658

APA Style

Costa, C. P., Cunha, S., Peixoto, A. F., Moreira, J. N., Lobo, J. M. S., & Silva, A. C. (2021). Application of the Quality-by-Design (QbD) Approach to Improve the Nose-to-Brain Delivery of Diazepam-Loaded Nanostructured Lipid Carriers (NLCs). Proceedings, 78(1), 40. https://doi.org/10.3390/IECP2020-08658

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