Solvent-Free Fabrication of Biphasic Lipid-Based Microparticles with Tunable Structure
Lipid-based biphasic microparticles are generally produced by long and complex techniques based on double emulsions. In this study, spray congealing was used as a solvent-free fabrication method with improved processability to transform water-in-oil non-aqueous emulsions into spherical solid lipid-b...
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| Format: | Article |
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MDPI AG
2021-12-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/1/54 |
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| author | Serena Bertoni Beatrice Albertini Joanna Ronowicz-Pilarczyk Natalia Calonghi Nadia Passerini |
| author_facet | Serena Bertoni Beatrice Albertini Joanna Ronowicz-Pilarczyk Natalia Calonghi Nadia Passerini |
| author_sort | Serena Bertoni |
| collection | DOAJ |
| description | Lipid-based biphasic microparticles are generally produced by long and complex techniques based on double emulsions. In this study, spray congealing was used as a solvent-free fabrication method with improved processability to transform water-in-oil non-aqueous emulsions into spherical solid lipid-based particles with a biphasic structure (b-MPs). Emulsions were prepared by melt emulsification using different compositions of lipids (Dynasan<sup>®</sup>118 and Compritol<sup>®</sup>888 ATO), surfactants (Cetylstearyl alcohol and Span<sup>®</sup>60) and hydrophilic carriers (PEGs, Gelucire<sup>®</sup>48/16 and Poloxamer 188). First, pseudo-ternary phase diagrams were constructed to identify the area corresponding to each emulsion type (coarse emulsion or microemulsion). The hydrophobicity of the lipid mostly affected the interfacial tension, and thus the microstructure of the emulsion. Emulsions were then processed by spray congealing and the obtained b-MPs were characterized in terms of thermal and chemical properties (by DSC and FT-IR), external and internal morphology (by SEM, CLSM and Raman mapping). Solid free-flowing spherical particles (main size range 200–355 µm) with different architectures were successfully produced: microemulsions led to the formation of particles with a homogeneous internal structure, while coarse emulsions generated “multicores-shell” particles consisting of variable size hydrophilic cores evenly distributed within the crystalline lipid phase. Depending on their composition and structure, b-MPs could achieve various release profiles, representing a more versatile system than microparticles based on a single lipid phase. The formulation and technological strategy proposed, provides a feasible and cost-effective way of fabricating b-MPs with tunable internal structure and release behavior. |
| first_indexed | 2024-03-10T00:44:01Z |
| format | Article |
| id | doaj.art-4436047fc2d34ff5892e9c5ecfc14460 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T00:44:01Z |
| publishDate | 2021-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-4436047fc2d34ff5892e9c5ecfc144602023-11-23T15:03:10ZengMDPI AGPharmaceutics1999-49232021-12-011415410.3390/pharmaceutics14010054Solvent-Free Fabrication of Biphasic Lipid-Based Microparticles with Tunable StructureSerena Bertoni0Beatrice Albertini1Joanna Ronowicz-Pilarczyk2Natalia Calonghi3Nadia Passerini4Department of Pharmacy and BioTechnology, Pharm Tech Lab, University of Bologna, Via S. Donato 19/2, 40127 Bologna, ItalyDepartment of Pharmacy and BioTechnology, Pharm Tech Lab, University of Bologna, Via S. Donato 19/2, 40127 Bologna, ItalyDepartment of Inorganic and Analytical Chemistry, Faculty of Pharmacy, Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, Jurasza 2, 85-089 Bydgoszcz, PolandDepartment of Pharmacy and BioTechnology, Cancer Metabolism Lab, University of Bologna, Via Irnerio 48, 40126 Bologna, ItalyDepartment of Pharmacy and BioTechnology, Pharm Tech Lab, University of Bologna, Via S. Donato 19/2, 40127 Bologna, ItalyLipid-based biphasic microparticles are generally produced by long and complex techniques based on double emulsions. In this study, spray congealing was used as a solvent-free fabrication method with improved processability to transform water-in-oil non-aqueous emulsions into spherical solid lipid-based particles with a biphasic structure (b-MPs). Emulsions were prepared by melt emulsification using different compositions of lipids (Dynasan<sup>®</sup>118 and Compritol<sup>®</sup>888 ATO), surfactants (Cetylstearyl alcohol and Span<sup>®</sup>60) and hydrophilic carriers (PEGs, Gelucire<sup>®</sup>48/16 and Poloxamer 188). First, pseudo-ternary phase diagrams were constructed to identify the area corresponding to each emulsion type (coarse emulsion or microemulsion). The hydrophobicity of the lipid mostly affected the interfacial tension, and thus the microstructure of the emulsion. Emulsions were then processed by spray congealing and the obtained b-MPs were characterized in terms of thermal and chemical properties (by DSC and FT-IR), external and internal morphology (by SEM, CLSM and Raman mapping). Solid free-flowing spherical particles (main size range 200–355 µm) with different architectures were successfully produced: microemulsions led to the formation of particles with a homogeneous internal structure, while coarse emulsions generated “multicores-shell” particles consisting of variable size hydrophilic cores evenly distributed within the crystalline lipid phase. Depending on their composition and structure, b-MPs could achieve various release profiles, representing a more versatile system than microparticles based on a single lipid phase. The formulation and technological strategy proposed, provides a feasible and cost-effective way of fabricating b-MPs with tunable internal structure and release behavior.https://www.mdpi.com/1999-4923/14/1/54spray chillingspray coolingmelt emulsificationcore-shellmicroemulsioninterfacial tension |
| spellingShingle | Serena Bertoni Beatrice Albertini Joanna Ronowicz-Pilarczyk Natalia Calonghi Nadia Passerini Solvent-Free Fabrication of Biphasic Lipid-Based Microparticles with Tunable Structure Pharmaceutics spray chilling spray cooling melt emulsification core-shell microemulsion interfacial tension |
| title | Solvent-Free Fabrication of Biphasic Lipid-Based Microparticles with Tunable Structure |
| title_full | Solvent-Free Fabrication of Biphasic Lipid-Based Microparticles with Tunable Structure |
| title_fullStr | Solvent-Free Fabrication of Biphasic Lipid-Based Microparticles with Tunable Structure |
| title_full_unstemmed | Solvent-Free Fabrication of Biphasic Lipid-Based Microparticles with Tunable Structure |
| title_short | Solvent-Free Fabrication of Biphasic Lipid-Based Microparticles with Tunable Structure |
| title_sort | solvent free fabrication of biphasic lipid based microparticles with tunable structure |
| topic | spray chilling spray cooling melt emulsification core-shell microemulsion interfacial tension |
| url | https://www.mdpi.com/1999-4923/14/1/54 |
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