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Article: Converting Nanosuspension into Inhalable and Redispersible Nanoparticles by Combined In-situ Thermal Gelation and Spray Drying

TitleConverting Nanosuspension into Inhalable and Redispersible Nanoparticles by Combined In-situ Thermal Gelation and Spray Drying
Authors
KeywordsItraconazole
Nanoparticles
Gelation
Spray drying
Inhalable and redispersible nano-agglomerates
Issue Date2020
PublisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ejpb
Citation
European Journal of Pharmaceutics and Biopharmaceutics, 2020, v. 149, p. 238-247 How to Cite?
AbstractWhile nanoparticulate drugs for deep lung delivery hold promise for particular disease treatments, their size-related physical instability and tendency of being exhaled during breathing remain major challenges to their inhaled formulation development. Here we report a viable method for converting drug nanosuspensions into inhalable, stable and redispersible nano-agglomerates through combined in-situ thermal gelation and spray drying. Itraconazole (ITZ) nanosuspensions were prepared by flash nanoprecipitation, and co-spray dried with two different grades of the gel-forming polymer, methylcellulose (MC M20 and MC M450) as protectants. MC M20 was found superior in protecting ITZ nanoparticles against thermal stress (through nanoparticle entrapment within its gel network structure) during spray drying. In terms of redispersibility, an Sf/Si ratio (i.e., ratio of nanoparticle sizes after and before spray drying) of unity (1.02 ± 0.03), reflecting full particle size preservation, was achieved by optimizing the suspending medium content and spray drying parameters. Formulation components, nanosuspension concentration and spray drying parameters all showed a significant impact on the aerosol performance of the resulting agglomerates, but an absence of defined trends or correlations. Overall, the MC-protected nano-agglomerates displayed excellent in-vitro aerosol performance with fine particle fractions higher than 50% and mass median aerodynamic diameters within the 2–3 µm range, which are ideal for deep lung delivery.
Persistent Identifierhttp://hdl.handle.net/10722/281235
ISSN
2019 Impact Factor: 4.604
2015 SCImago Journal Rankings: 1.423

 

DC FieldValueLanguage
dc.contributor.authorWan, KY-
dc.contributor.authorWENG, J-
dc.contributor.authorWONG, SN-
dc.contributor.authorKwok, PCL-
dc.contributor.authorChow, SF-
dc.contributor.authorChow, AHL-
dc.date.accessioned2020-03-09T09:51:56Z-
dc.date.available2020-03-09T09:51:56Z-
dc.date.issued2020-
dc.identifier.citationEuropean Journal of Pharmaceutics and Biopharmaceutics, 2020, v. 149, p. 238-247-
dc.identifier.issn0939-6411-
dc.identifier.urihttp://hdl.handle.net/10722/281235-
dc.description.abstractWhile nanoparticulate drugs for deep lung delivery hold promise for particular disease treatments, their size-related physical instability and tendency of being exhaled during breathing remain major challenges to their inhaled formulation development. Here we report a viable method for converting drug nanosuspensions into inhalable, stable and redispersible nano-agglomerates through combined in-situ thermal gelation and spray drying. Itraconazole (ITZ) nanosuspensions were prepared by flash nanoprecipitation, and co-spray dried with two different grades of the gel-forming polymer, methylcellulose (MC M20 and MC M450) as protectants. MC M20 was found superior in protecting ITZ nanoparticles against thermal stress (through nanoparticle entrapment within its gel network structure) during spray drying. In terms of redispersibility, an Sf/Si ratio (i.e., ratio of nanoparticle sizes after and before spray drying) of unity (1.02 ± 0.03), reflecting full particle size preservation, was achieved by optimizing the suspending medium content and spray drying parameters. Formulation components, nanosuspension concentration and spray drying parameters all showed a significant impact on the aerosol performance of the resulting agglomerates, but an absence of defined trends or correlations. Overall, the MC-protected nano-agglomerates displayed excellent in-vitro aerosol performance with fine particle fractions higher than 50% and mass median aerodynamic diameters within the 2–3 µm range, which are ideal for deep lung delivery.-
dc.languageeng-
dc.publisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ejpb-
dc.relation.ispartofEuropean Journal of Pharmaceutics and Biopharmaceutics-
dc.subjectItraconazole-
dc.subjectNanoparticles-
dc.subjectGelation-
dc.subjectSpray drying-
dc.subjectInhalable and redispersible nano-agglomerates-
dc.titleConverting Nanosuspension into Inhalable and Redispersible Nanoparticles by Combined In-situ Thermal Gelation and Spray Drying-
dc.typeArticle-
dc.identifier.emailChow, SF: asfchow@hku.hk-
dc.identifier.authorityChow, SF=rp02296-
dc.description.naturelink_to_subscribed_fulltext-
dc.identifier.doi10.1016/j.ejpb.2020.02.010-
dc.identifier.scopuseid_2-s2.0-85080107303-
dc.identifier.hkuros309336-
dc.identifier.volume149-
dc.identifier.spage238-
dc.identifier.epage247-
dc.publisher.placeNetherlands-

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