Preparation and in vitro evaluation of hot-melt extruded pectin-based pellets containing ketoprofen for colon targeting
This work developed high drug-load pellets for colon targeting in minimal steps by coupling hot-melt extrusion (HME) with a die-surface cutting pelletizer, offering a potential continuous pellet manufacturing process. Ketoprofen (KTP) was selected as a model drug for this study due to its thermal st...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2023-12-01
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| Series: | International Journal of Pharmaceutics: X |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2590156722000470 |
| _version_ | 1797798696631402496 |
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| author | Sagar Narala Dinesh Nyavanandi Preethi Mandati Ahmed Adel Ali Youssef Abdullah Alzahrani Praveen Kolimi Feng Zhang Michael Repka |
| author_facet | Sagar Narala Dinesh Nyavanandi Preethi Mandati Ahmed Adel Ali Youssef Abdullah Alzahrani Praveen Kolimi Feng Zhang Michael Repka |
| author_sort | Sagar Narala |
| collection | DOAJ |
| description | This work developed high drug-load pellets for colon targeting in minimal steps by coupling hot-melt extrusion (HME) with a die-surface cutting pelletizer, offering a potential continuous pellet manufacturing process. Ketoprofen (KTP) was selected as a model drug for this study due to its thermal stability and severe upper gastrointestinal side effects. Low and high methoxyl grade pectins were the enzyme-triggered release matrix, and hydroxypropyl methylcellulose (HME 4 M/HME 100LV) was used as a premature release-retarding agent. The powder X-ray diffraction technique and the differential scanning calorimetry results revealed that KTP exists in the solid-solution state within the polymeric matrix after the HME step. The scanning electron micrographs of the fabricated pellets showed a smooth surface without any cracks. The lead formulation showed the lowest premature drug release (∼13%) with an extended KTP release profile over a 24 h period in the presence and absence of the release-triggering enzyme. The lead formulation was stable for 3 months at accelerated stability conditions (40 °C/75 ± 5% RH) concerning drug content, in vitro release, and thermal characteristics. In summary, coupling HME and pelletization processes could be a promising technology for developing colon-targeted drug delivery systems. |
| first_indexed | 2024-03-13T04:07:44Z |
| format | Article |
| id | doaj.art-cba887c0e9554274982da1e0682ec6d7 |
| institution | Directory Open Access Journal |
| issn | 2590-1567 |
| language | English |
| last_indexed | 2024-03-13T04:07:44Z |
| publishDate | 2023-12-01 |
| publisher | Elsevier |
| record_format | Article |
| series | International Journal of Pharmaceutics: X |
| spelling | doaj.art-cba887c0e9554274982da1e0682ec6d72023-06-21T06:59:10ZengElsevierInternational Journal of Pharmaceutics: X2590-15672023-12-015100156Preparation and in vitro evaluation of hot-melt extruded pectin-based pellets containing ketoprofen for colon targetingSagar Narala0Dinesh Nyavanandi1Preethi Mandati2Ahmed Adel Ali Youssef3Abdullah Alzahrani4Praveen Kolimi5Feng Zhang6Michael Repka7Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USADepartment of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USADepartment of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USADepartment of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USA; Department of Pharmaceutical Technology, Faculty of Pharmacy, Kafrelsheikh University, Kafrelsheikh 33516, EgyptDepartment of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USADepartment of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USACollege of Pharmacy, The University of Texas at Austin, Austin, TX 78712, USADepartment of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USA; Pii Center for Pharmaceutical Technology, The University of Mississippi, University, MS 38677, USA; Corresponding author at: Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.This work developed high drug-load pellets for colon targeting in minimal steps by coupling hot-melt extrusion (HME) with a die-surface cutting pelletizer, offering a potential continuous pellet manufacturing process. Ketoprofen (KTP) was selected as a model drug for this study due to its thermal stability and severe upper gastrointestinal side effects. Low and high methoxyl grade pectins were the enzyme-triggered release matrix, and hydroxypropyl methylcellulose (HME 4 M/HME 100LV) was used as a premature release-retarding agent. The powder X-ray diffraction technique and the differential scanning calorimetry results revealed that KTP exists in the solid-solution state within the polymeric matrix after the HME step. The scanning electron micrographs of the fabricated pellets showed a smooth surface without any cracks. The lead formulation showed the lowest premature drug release (∼13%) with an extended KTP release profile over a 24 h period in the presence and absence of the release-triggering enzyme. The lead formulation was stable for 3 months at accelerated stability conditions (40 °C/75 ± 5% RH) concerning drug content, in vitro release, and thermal characteristics. In summary, coupling HME and pelletization processes could be a promising technology for developing colon-targeted drug delivery systems.http://www.sciencedirect.com/science/article/pii/S2590156722000470KetoprofenPectinHot-melt extrusionColon targetingHydroxypropyl methylcellulose |
| spellingShingle | Sagar Narala Dinesh Nyavanandi Preethi Mandati Ahmed Adel Ali Youssef Abdullah Alzahrani Praveen Kolimi Feng Zhang Michael Repka Preparation and in vitro evaluation of hot-melt extruded pectin-based pellets containing ketoprofen for colon targeting International Journal of Pharmaceutics: X Ketoprofen Pectin Hot-melt extrusion Colon targeting Hydroxypropyl methylcellulose |
| title | Preparation and in vitro evaluation of hot-melt extruded pectin-based pellets containing ketoprofen for colon targeting |
| title_full | Preparation and in vitro evaluation of hot-melt extruded pectin-based pellets containing ketoprofen for colon targeting |
| title_fullStr | Preparation and in vitro evaluation of hot-melt extruded pectin-based pellets containing ketoprofen for colon targeting |
| title_full_unstemmed | Preparation and in vitro evaluation of hot-melt extruded pectin-based pellets containing ketoprofen for colon targeting |
| title_short | Preparation and in vitro evaluation of hot-melt extruded pectin-based pellets containing ketoprofen for colon targeting |
| title_sort | preparation and in vitro evaluation of hot melt extruded pectin based pellets containing ketoprofen for colon targeting |
| topic | Ketoprofen Pectin Hot-melt extrusion Colon targeting Hydroxypropyl methylcellulose |
| url | http://www.sciencedirect.com/science/article/pii/S2590156722000470 |
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