Ciprofibrate-Loaded Nanoparticles Prepared by Nanoprecipitation: Synthesis, Characterization, and Drug Release
Ciprofibrate (CIP) is a highly lipophilic and poorly water-soluble drug, typically used for dyslipidemia treatment. Although it is already commercialized in capsules, no previous studies report its solid-state structure; thus, information about the correlation with its physicochemical properties is...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-09-01
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| Series: | Polymers |
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| Online Access: | https://www.mdpi.com/2073-4360/13/18/3158 |
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| author | Raissa Lohanna Gomes Quintino Corrêa Renan dos Santos Lindomar José Calumby Albuquerque Gabriel Lima Barros de Araujo Charlotte Jennifer Chante Edwards-Gayle Fabio Furlan Ferreira Fanny Nascimento Costa |
| author_facet | Raissa Lohanna Gomes Quintino Corrêa Renan dos Santos Lindomar José Calumby Albuquerque Gabriel Lima Barros de Araujo Charlotte Jennifer Chante Edwards-Gayle Fabio Furlan Ferreira Fanny Nascimento Costa |
| author_sort | Raissa Lohanna Gomes Quintino Corrêa |
| collection | DOAJ |
| description | Ciprofibrate (CIP) is a highly lipophilic and poorly water-soluble drug, typically used for dyslipidemia treatment. Although it is already commercialized in capsules, no previous studies report its solid-state structure; thus, information about the correlation with its physicochemical properties is lacking. In parallel, recent studies have led to the improvement of drug administration, including encapsulation in polymeric nanoparticles (NPs). Here, we present CIP’s crystal structure determined by PXRD data. We also propose an encapsulation method for CIP in micelles produced from Pluronic P123/F127 and PEO-<i>b</i>-PCL, aiming to improve its solubility, hydrophilicity, and delivery. We determined the NPs’ physicochemical properties by DLS, SLS, ELS, SAXS and the loaded drug amount by UV-Vis spectroscopy. Micelles showed sizes around 10–20 nm for Pluronic and 35–45 nm for the PEO-<i>b</i>-PCL NPs with slightly negative surface charge and successful CIP loading, especially for the latter; a substantial reduction in ζ-potential may be evidenced. For Pluronic nanoparticles, we scanned different conditions for the CIP loading, and its encapsulation efficiency was reduced while the drug content increased in the nanoprecipitation protocol. We also performed in vitro release experiments; results demonstrate that probe release is driven by Fickian diffusion for the Pluronic NPs and a zero-order model for PEO-<i>b</i>-PCL NPs. |
| first_indexed | 2024-03-10T07:16:29Z |
| format | Article |
| id | doaj.art-78d81f15e3f24e529f5ac5db438d9efe |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-10T07:16:29Z |
| publishDate | 2021-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-78d81f15e3f24e529f5ac5db438d9efe2023-11-22T14:57:15ZengMDPI AGPolymers2073-43602021-09-011318315810.3390/polym13183158Ciprofibrate-Loaded Nanoparticles Prepared by Nanoprecipitation: Synthesis, Characterization, and Drug ReleaseRaissa Lohanna Gomes Quintino Corrêa0Renan dos Santos1Lindomar José Calumby Albuquerque2Gabriel Lima Barros de Araujo3Charlotte Jennifer Chante Edwards-Gayle4Fabio Furlan Ferreira5Fanny Nascimento Costa6Center for Natural and Human Sciences (CCNH), Federal University of ABC (UFABC), Santo André 09210-580, BrazilCenter for Natural and Human Sciences (CCNH), Federal University of ABC (UFABC), Santo André 09210-580, BrazilCenter for Natural and Human Sciences (CCNH), Federal University of ABC (UFABC), Santo André 09210-580, BrazilDepartment of Pharmacy, Faculty of Pharmaceutical Sciences, University of Sao Paulo, Sao Paulo 05508-900, BrazilDiamond Light Source, Harwell Science & Innovation Campus, Didcot, Oxfordshire OX11 0DE, UKCenter for Natural and Human Sciences (CCNH), Federal University of ABC (UFABC), Santo André 09210-580, BrazilCenter for Natural and Human Sciences (CCNH), Federal University of ABC (UFABC), Santo André 09210-580, BrazilCiprofibrate (CIP) is a highly lipophilic and poorly water-soluble drug, typically used for dyslipidemia treatment. Although it is already commercialized in capsules, no previous studies report its solid-state structure; thus, information about the correlation with its physicochemical properties is lacking. In parallel, recent studies have led to the improvement of drug administration, including encapsulation in polymeric nanoparticles (NPs). Here, we present CIP’s crystal structure determined by PXRD data. We also propose an encapsulation method for CIP in micelles produced from Pluronic P123/F127 and PEO-<i>b</i>-PCL, aiming to improve its solubility, hydrophilicity, and delivery. We determined the NPs’ physicochemical properties by DLS, SLS, ELS, SAXS and the loaded drug amount by UV-Vis spectroscopy. Micelles showed sizes around 10–20 nm for Pluronic and 35–45 nm for the PEO-<i>b</i>-PCL NPs with slightly negative surface charge and successful CIP loading, especially for the latter; a substantial reduction in ζ-potential may be evidenced. For Pluronic nanoparticles, we scanned different conditions for the CIP loading, and its encapsulation efficiency was reduced while the drug content increased in the nanoprecipitation protocol. We also performed in vitro release experiments; results demonstrate that probe release is driven by Fickian diffusion for the Pluronic NPs and a zero-order model for PEO-<i>b</i>-PCL NPs.https://www.mdpi.com/2073-4360/13/18/3158ciprofibratedrug deliveryRietveld methodcrystallographynanotechnology |
| spellingShingle | Raissa Lohanna Gomes Quintino Corrêa Renan dos Santos Lindomar José Calumby Albuquerque Gabriel Lima Barros de Araujo Charlotte Jennifer Chante Edwards-Gayle Fabio Furlan Ferreira Fanny Nascimento Costa Ciprofibrate-Loaded Nanoparticles Prepared by Nanoprecipitation: Synthesis, Characterization, and Drug Release Polymers ciprofibrate drug delivery Rietveld method crystallography nanotechnology |
| title | Ciprofibrate-Loaded Nanoparticles Prepared by Nanoprecipitation: Synthesis, Characterization, and Drug Release |
| title_full | Ciprofibrate-Loaded Nanoparticles Prepared by Nanoprecipitation: Synthesis, Characterization, and Drug Release |
| title_fullStr | Ciprofibrate-Loaded Nanoparticles Prepared by Nanoprecipitation: Synthesis, Characterization, and Drug Release |
| title_full_unstemmed | Ciprofibrate-Loaded Nanoparticles Prepared by Nanoprecipitation: Synthesis, Characterization, and Drug Release |
| title_short | Ciprofibrate-Loaded Nanoparticles Prepared by Nanoprecipitation: Synthesis, Characterization, and Drug Release |
| title_sort | ciprofibrate loaded nanoparticles prepared by nanoprecipitation synthesis characterization and drug release |
| topic | ciprofibrate drug delivery Rietveld method crystallography nanotechnology |
| url | https://www.mdpi.com/2073-4360/13/18/3158 |
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