Design, Evaluation and Comparison of Nanostructured Lipid Carriers and Chitosan Nanoparticles as Carriers of Poorly Soluble Drugs to Develop Oral Liquid Formulations Suitable for Pediatric Use
There is a serious need of pediatric drug formulations, whose lack causes the frequent use of extemporaneous preparations obtained from adult dosage forms, with consequent safety and quality risks. Oral solutions are the best choice for pediatric patients, due to administration ease and dosage-adapt...
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MDPI AG
2023-04-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/4/1305 |
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| author | Giulia Nerli Lídia M. D. Gonçalves Marzia Cirri António J. Almeida Francesca Maestrelli Natascia Mennini Paola A. Mura |
| author_facet | Giulia Nerli Lídia M. D. Gonçalves Marzia Cirri António J. Almeida Francesca Maestrelli Natascia Mennini Paola A. Mura |
| author_sort | Giulia Nerli |
| collection | DOAJ |
| description | There is a serious need of pediatric drug formulations, whose lack causes the frequent use of extemporaneous preparations obtained from adult dosage forms, with consequent safety and quality risks. Oral solutions are the best choice for pediatric patients, due to administration ease and dosage-adaptability, but their development is challenging, particularly for poorly soluble drugs. In this work, chitosan nanoparticles (CSNPs) and nanostructured lipid carriers (NLCs) were developed and evaluated as potential nanocarriers for preparing oral pediatric solutions of cefixime (poorly soluble model drug). The selected CSNPs and NLCs showed a size around 390 nm, Zeta-potential > 30 mV, and comparable entrapment efficiency (31–36%), but CSNPs had higher loading efficiency (5.2 vs. 1.4%). CSNPs maintained an almost unchanged size, homogeneity, and Zeta-potential during storage, while NLCs exhibited a marked progressive Zeta-potential decrease. Drug release from CSNPs formulations (differently from NLCs) was poorly affected by gastric pH variations, and gave rise to a more reproducible and controlled profile. This was related to their behavior in simulated gastric conditions, where CSNPs were stable, while NLCs suffered a rapid size increase, up to micrometric dimensions. Cytotoxicity studies confirmed CSNPs as the best nanocarrier, proving their complete biocompatibility, while NLCs formulations needed 1:1 dilution to obtain acceptable cell viability values. |
| first_indexed | 2024-03-11T04:37:23Z |
| format | Article |
| id | doaj.art-85b3c7ca18284c59ab484ea8e044bba2 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T04:37:23Z |
| publishDate | 2023-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-85b3c7ca18284c59ab484ea8e044bba22023-11-17T20:55:38ZengMDPI AGPharmaceutics1999-49232023-04-01154130510.3390/pharmaceutics15041305Design, Evaluation and Comparison of Nanostructured Lipid Carriers and Chitosan Nanoparticles as Carriers of Poorly Soluble Drugs to Develop Oral Liquid Formulations Suitable for Pediatric UseGiulia Nerli0Lídia M. D. Gonçalves1Marzia Cirri2António J. Almeida3Francesca Maestrelli4Natascia Mennini5Paola A. Mura6Department of Chemistry, University of Florence, Via Schiff 6, Sesto Fiorentino, 50019 Florence, ItalyResearch Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003 Lisboa, PortugalDepartment of Chemistry, University of Florence, Via Schiff 6, Sesto Fiorentino, 50019 Florence, ItalyResearch Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003 Lisboa, PortugalDepartment of Chemistry, University of Florence, Via Schiff 6, Sesto Fiorentino, 50019 Florence, ItalyResearch Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003 Lisboa, PortugalDepartment of Chemistry, University of Florence, Via Schiff 6, Sesto Fiorentino, 50019 Florence, ItalyThere is a serious need of pediatric drug formulations, whose lack causes the frequent use of extemporaneous preparations obtained from adult dosage forms, with consequent safety and quality risks. Oral solutions are the best choice for pediatric patients, due to administration ease and dosage-adaptability, but their development is challenging, particularly for poorly soluble drugs. In this work, chitosan nanoparticles (CSNPs) and nanostructured lipid carriers (NLCs) were developed and evaluated as potential nanocarriers for preparing oral pediatric solutions of cefixime (poorly soluble model drug). The selected CSNPs and NLCs showed a size around 390 nm, Zeta-potential > 30 mV, and comparable entrapment efficiency (31–36%), but CSNPs had higher loading efficiency (5.2 vs. 1.4%). CSNPs maintained an almost unchanged size, homogeneity, and Zeta-potential during storage, while NLCs exhibited a marked progressive Zeta-potential decrease. Drug release from CSNPs formulations (differently from NLCs) was poorly affected by gastric pH variations, and gave rise to a more reproducible and controlled profile. This was related to their behavior in simulated gastric conditions, where CSNPs were stable, while NLCs suffered a rapid size increase, up to micrometric dimensions. Cytotoxicity studies confirmed CSNPs as the best nanocarrier, proving their complete biocompatibility, while NLCs formulations needed 1:1 dilution to obtain acceptable cell viability values.https://www.mdpi.com/1999-4923/15/4/1305chitosan nanoparticleslipid nanoparticlescefiximeoral liquid formulations for childrengastric stabilitystorage stability |
| spellingShingle | Giulia Nerli Lídia M. D. Gonçalves Marzia Cirri António J. Almeida Francesca Maestrelli Natascia Mennini Paola A. Mura Design, Evaluation and Comparison of Nanostructured Lipid Carriers and Chitosan Nanoparticles as Carriers of Poorly Soluble Drugs to Develop Oral Liquid Formulations Suitable for Pediatric Use Pharmaceutics chitosan nanoparticles lipid nanoparticles cefixime oral liquid formulations for children gastric stability storage stability |
| title | Design, Evaluation and Comparison of Nanostructured Lipid Carriers and Chitosan Nanoparticles as Carriers of Poorly Soluble Drugs to Develop Oral Liquid Formulations Suitable for Pediatric Use |
| title_full | Design, Evaluation and Comparison of Nanostructured Lipid Carriers and Chitosan Nanoparticles as Carriers of Poorly Soluble Drugs to Develop Oral Liquid Formulations Suitable for Pediatric Use |
| title_fullStr | Design, Evaluation and Comparison of Nanostructured Lipid Carriers and Chitosan Nanoparticles as Carriers of Poorly Soluble Drugs to Develop Oral Liquid Formulations Suitable for Pediatric Use |
| title_full_unstemmed | Design, Evaluation and Comparison of Nanostructured Lipid Carriers and Chitosan Nanoparticles as Carriers of Poorly Soluble Drugs to Develop Oral Liquid Formulations Suitable for Pediatric Use |
| title_short | Design, Evaluation and Comparison of Nanostructured Lipid Carriers and Chitosan Nanoparticles as Carriers of Poorly Soluble Drugs to Develop Oral Liquid Formulations Suitable for Pediatric Use |
| title_sort | design evaluation and comparison of nanostructured lipid carriers and chitosan nanoparticles as carriers of poorly soluble drugs to develop oral liquid formulations suitable for pediatric use |
| topic | chitosan nanoparticles lipid nanoparticles cefixime oral liquid formulations for children gastric stability storage stability |
| url | https://www.mdpi.com/1999-4923/15/4/1305 |
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