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Title: Innovative Aqueous Nanoemulsion Prepared by Phase Inversion Emulsification with Exceptional Homogeneity
Authors: Pires, Patrícia C. 
Fernandes, Mariana
Nina, Francisca
Gama, Francisco
Gomes, Maria F
Rodrigues, Lina E
Meirinho, Sara
Silvestre, Samuel 
Alves, Gilberto 
Santos, Adriana O.
Keywords: nanoemulsion; intranasal; low energy; homogenous; phase inversion; propylene glycol monocaprylate type II
Issue Date: 4-Jul-2023
Publisher: MDPI
Project: This research was funded by Fundação para a Ciência e a Tecnologia (FCT), through funds from the Portuguese State Budget (grant numbers UIDB/00709/2020, UIDP/00709/2020), and by the European Regional Development Fund, under the Portugal 2020 Program, through the Regional Operational Program of the Center (Centro2020), (CENTRO-01-0145-FEDER-000013 and CENTRO- 01-0145-FEDER-181231). SM was funded by FCT (PhD fellowship number SFRH/BD/136028/2018). FG was funded by FCT (BII fellowship from the program “Verão com Ciência”, MERCI project). 
Serial title, monograph or event: Pharmaceutics
Volume: 15
Issue: 7
Abstract: Formulating low-solubility or low-permeability drugs is a challenge, particularly with the low administration volumes required in intranasal drug delivery. Nanoemulsions (NE) can solve both issues, but their production and physical stability can be challenging, particularly when a high proportion of lipids is necessary. Hence, the aim of the present work was to develop a NE with good solubilization capacity for lipophilic drugs like simvastatin and able to promote the absorption of drugs with low permeability like fosphenytoin. Compositions with high proportion of two lipids were screened and characterized. Surprisingly, one of the compositions did not require high energy methods for high droplet size homogeneity. To better understand formulation factors important for this feature, several related compositions were evaluated, and their relative cytotoxicity was screened. Optimized compositions contained a high proportion of propylene glycol monocaprylate NF, formed very homogenous NE using a low-energy phase inversion method, solubilized simvastatin at high drug strength, and promoted a faster intranasal absorption of the hydrophilic prodrug fosphenytoin. Hence, a new highly homogeneous NE obtained by a simple low-energy method was successfully developed, which is a potential alternative for industrial application for the solubilization and protection of lipophilic actives, as well as (co-)administration of hydrophilic molecules.
ISSN: 1999-4923
DOI: 10.3390/pharmaceutics15071878
Rights: openAccess
Appears in Collections:FFUC- Artigos em Revistas Internacionais

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