Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility
A challenge in the pharmaceutical sector is the development of controlled release dosage forms for oral administration of poorly soluble drugs, in particular, drugs characterized by pH-dependent solubility through the gastrointestinal tract, which itself shows wide variability in terms of environmen...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-05-01
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| Series: | Polymers |
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| Online Access: | https://www.mdpi.com/2073-4360/14/10/2127 |
| _version_ | 1797496145338957824 |
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| author | Valeria Friuli Silvia Pisani Bice Conti Giovanna Bruni Lauretta Maggi |
| author_facet | Valeria Friuli Silvia Pisani Bice Conti Giovanna Bruni Lauretta Maggi |
| author_sort | Valeria Friuli |
| collection | DOAJ |
| description | A challenge in the pharmaceutical sector is the development of controlled release dosage forms for oral administration of poorly soluble drugs, in particular, drugs characterized by pH-dependent solubility through the gastrointestinal tract, which itself shows wide variability in terms of environmental pHs. The best approach is to increase the dissolution rate of the drugs at the different pHs and only then modify its release behavior from the pharmaceutical form. This work aims to demonstrate the ability of properly designed polymeric nanofibers in enhancing the release rate of model drugs with different pH-dependent solubility in the different physiological pHs of the gastrointestinal tract. Polymeric nanofibers loaded with meloxicam and carvedilol were prepared using the electrospinning technique and were then included in properly designed tablet formulations to obtain fast or sustained release dosage forms. The nanofibers and the tablets were characterized for their morphological, physico-chemical and dissolution properties. The tablets are able to deliver the dose according to the expected release behavior, and zero-order, first-order, Higuchi, Korsmeyer–Peppas and Hixon–Crowell kinetics models were used to analyze the prevailing release mechanism of the tablets. This study shows that the electrospun fibers can be advantageously included in oral dosage forms to improve their release performances. |
| first_indexed | 2024-03-10T03:00:28Z |
| format | Article |
| id | doaj.art-1271473b277c4f59befcf4982e8eac5b |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-10T03:00:28Z |
| publishDate | 2022-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-1271473b277c4f59befcf4982e8eac5b2023-11-23T12:47:56ZengMDPI AGPolymers2073-43602022-05-011410212710.3390/polym14102127Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent SolubilityValeria Friuli0Silvia Pisani1Bice Conti2Giovanna Bruni3Lauretta Maggi4Department of Drug Sciences, University of Pavia, Via Taramelli 12, 27100 Pavia, ItalyDepartment of Otolaryngology, Fondazione IRCCS Policlinico San Matteo, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, Via Taramelli 12, 27100 Pavia, ItalyDepartment of Chemistry, Physical-Chemistry Section, University of Pavia, Via Taramelli 16, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, Via Taramelli 12, 27100 Pavia, ItalyA challenge in the pharmaceutical sector is the development of controlled release dosage forms for oral administration of poorly soluble drugs, in particular, drugs characterized by pH-dependent solubility through the gastrointestinal tract, which itself shows wide variability in terms of environmental pHs. The best approach is to increase the dissolution rate of the drugs at the different pHs and only then modify its release behavior from the pharmaceutical form. This work aims to demonstrate the ability of properly designed polymeric nanofibers in enhancing the release rate of model drugs with different pH-dependent solubility in the different physiological pHs of the gastrointestinal tract. Polymeric nanofibers loaded with meloxicam and carvedilol were prepared using the electrospinning technique and were then included in properly designed tablet formulations to obtain fast or sustained release dosage forms. The nanofibers and the tablets were characterized for their morphological, physico-chemical and dissolution properties. The tablets are able to deliver the dose according to the expected release behavior, and zero-order, first-order, Higuchi, Korsmeyer–Peppas and Hixon–Crowell kinetics models were used to analyze the prevailing release mechanism of the tablets. This study shows that the electrospun fibers can be advantageously included in oral dosage forms to improve their release performances.https://www.mdpi.com/2073-4360/14/10/2127nanofiberssustained releasefast releasetabletspolymerpoorly soluble drug |
| spellingShingle | Valeria Friuli Silvia Pisani Bice Conti Giovanna Bruni Lauretta Maggi Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility Polymers nanofibers sustained release fast release tablets polymer poorly soluble drug |
| title | Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility |
| title_full | Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility |
| title_fullStr | Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility |
| title_full_unstemmed | Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility |
| title_short | Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility |
| title_sort | tablet formulations of polymeric electrospun fibers for the controlled release of drugs with ph dependent solubility |
| topic | nanofibers sustained release fast release tablets polymer poorly soluble drug |
| url | https://www.mdpi.com/2073-4360/14/10/2127 |
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