Synthesis, Characterization and In Vitro Evaluation of Chitosan Nanoparticles Physically Admixed with Lactose Microspheres for Pulmonary Delivery of Montelukast
This study aimed to synthesise montelukast-loaded polymeric nanoparticles via the ionic gelation method using chitosan as a natural polymer and tripolyphosphate as a crosslinking agent. Tween 80, hyaluronic acid and leucine were added to modify the physicochemical properties of nanoparticles, reduce...
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MDPI AG
2022-08-01
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| Series: | Polymers |
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| Online Access: | https://www.mdpi.com/2073-4360/14/17/3564 |
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| author | Faqir Ullah Kifayat Ullah Shah Shefaat Ullah Shah Asif Nawaz Touseef Nawaz Kamran Ahmad Khan Raed F. Alserihi Hossam H. Tayeb Shams Tabrez Mulham Alfatama |
| author_facet | Faqir Ullah Kifayat Ullah Shah Shefaat Ullah Shah Asif Nawaz Touseef Nawaz Kamran Ahmad Khan Raed F. Alserihi Hossam H. Tayeb Shams Tabrez Mulham Alfatama |
| author_sort | Faqir Ullah |
| collection | DOAJ |
| description | This study aimed to synthesise montelukast-loaded polymeric nanoparticles via the ionic gelation method using chitosan as a natural polymer and tripolyphosphate as a crosslinking agent. Tween 80, hyaluronic acid and leucine were added to modify the physicochemical properties of nanoparticles, reduce the nanoparticles’ uptake by alveolar macrophages and improve powder aerosolisation, respectively. The nanoparticles ranged from 220 nm to 383 nm with a polydispersity index of ≤0.50. The zeta potential of nanoparticles ranged from 11 mV to 22 mV, with a drug association efficiency of 46–86%. The simple chitosan nanoparticles (F2) were more spherical in comparison to other formulations (F4–F6), while the roughness of hyaluronic acid (F5) and leucine (F6) added formulations was significantly high er than F2 and Tween 80 added formulation (F4). The DSC and FTIR analysis depict that the physical and chemical properties of the drug were preserved. The release of the drugs from nanoparticles was more sustained in the case of F5 and F6 when compared to F2 and F4 due to the additional coating of hyaluronic acid and leucine. The nanoparticles were amorphous and cohesive and prone to exhalation due to their small size. Therefore, nanoparticles were admixed with lactose microspheres to reduce particle agglomeration and improve powder dispersion from a dry powder inhaler (DPI). The DPI formulations achieved a dispersed fraction of 75 to 90%, a mass median aerodynamic diameter (MMAD) of 1–2 µm and a fine particle fraction (FPF) of 28–83% when evaluated using the Anderson cascade impactor from Handihaler<sup>®</sup>. Overall, the montelukast-loaded nanoparticles physically admixed with lactose microspheres achieved optimum deposition in the deep lung for potential application in asthmatic patients. |
| first_indexed | 2024-03-10T01:21:02Z |
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| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-10T01:21:02Z |
| publishDate | 2022-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-7ecfec7ce04a49a3a808553f0ba9c9a22023-11-23T13:58:58ZengMDPI AGPolymers2073-43602022-08-011417356410.3390/polym14173564Synthesis, Characterization and In Vitro Evaluation of Chitosan Nanoparticles Physically Admixed with Lactose Microspheres for Pulmonary Delivery of MontelukastFaqir Ullah0Kifayat Ullah Shah1Shefaat Ullah Shah2Asif Nawaz3Touseef Nawaz4Kamran Ahmad Khan5Raed F. Alserihi6Hossam H. Tayeb7Shams Tabrez8Mulham Alfatama9Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanFaculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanFaculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanFaculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanFaculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanFaculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanDepartment of Medical Laboratory Sciences, Faculty of Applied Medical Sciences, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Medical Laboratory Sciences, Faculty of Applied Medical Sciences, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Medical Laboratory Sciences, Faculty of Applied Medical Sciences, King Abdulaziz University, Jeddah 21589, Saudi ArabiaFaculty of Pharmacy, Universiti Sultan Zainal Abidin, Besut Campus, Besut 22200, Terengganu, MalaysiaThis study aimed to synthesise montelukast-loaded polymeric nanoparticles via the ionic gelation method using chitosan as a natural polymer and tripolyphosphate as a crosslinking agent. Tween 80, hyaluronic acid and leucine were added to modify the physicochemical properties of nanoparticles, reduce the nanoparticles’ uptake by alveolar macrophages and improve powder aerosolisation, respectively. The nanoparticles ranged from 220 nm to 383 nm with a polydispersity index of ≤0.50. The zeta potential of nanoparticles ranged from 11 mV to 22 mV, with a drug association efficiency of 46–86%. The simple chitosan nanoparticles (F2) were more spherical in comparison to other formulations (F4–F6), while the roughness of hyaluronic acid (F5) and leucine (F6) added formulations was significantly high er than F2 and Tween 80 added formulation (F4). The DSC and FTIR analysis depict that the physical and chemical properties of the drug were preserved. The release of the drugs from nanoparticles was more sustained in the case of F5 and F6 when compared to F2 and F4 due to the additional coating of hyaluronic acid and leucine. The nanoparticles were amorphous and cohesive and prone to exhalation due to their small size. Therefore, nanoparticles were admixed with lactose microspheres to reduce particle agglomeration and improve powder dispersion from a dry powder inhaler (DPI). The DPI formulations achieved a dispersed fraction of 75 to 90%, a mass median aerodynamic diameter (MMAD) of 1–2 µm and a fine particle fraction (FPF) of 28–83% when evaluated using the Anderson cascade impactor from Handihaler<sup>®</sup>. Overall, the montelukast-loaded nanoparticles physically admixed with lactose microspheres achieved optimum deposition in the deep lung for potential application in asthmatic patients.https://www.mdpi.com/2073-4360/14/17/3564montelukastchitosanlactosenanoparticlesmicrospheresinhalation drug delivery |
| spellingShingle | Faqir Ullah Kifayat Ullah Shah Shefaat Ullah Shah Asif Nawaz Touseef Nawaz Kamran Ahmad Khan Raed F. Alserihi Hossam H. Tayeb Shams Tabrez Mulham Alfatama Synthesis, Characterization and In Vitro Evaluation of Chitosan Nanoparticles Physically Admixed with Lactose Microspheres for Pulmonary Delivery of Montelukast Polymers montelukast chitosan lactose nanoparticles microspheres inhalation drug delivery |
| title | Synthesis, Characterization and In Vitro Evaluation of Chitosan Nanoparticles Physically Admixed with Lactose Microspheres for Pulmonary Delivery of Montelukast |
| title_full | Synthesis, Characterization and In Vitro Evaluation of Chitosan Nanoparticles Physically Admixed with Lactose Microspheres for Pulmonary Delivery of Montelukast |
| title_fullStr | Synthesis, Characterization and In Vitro Evaluation of Chitosan Nanoparticles Physically Admixed with Lactose Microspheres for Pulmonary Delivery of Montelukast |
| title_full_unstemmed | Synthesis, Characterization and In Vitro Evaluation of Chitosan Nanoparticles Physically Admixed with Lactose Microspheres for Pulmonary Delivery of Montelukast |
| title_short | Synthesis, Characterization and In Vitro Evaluation of Chitosan Nanoparticles Physically Admixed with Lactose Microspheres for Pulmonary Delivery of Montelukast |
| title_sort | synthesis characterization and in vitro evaluation of chitosan nanoparticles physically admixed with lactose microspheres for pulmonary delivery of montelukast |
| topic | montelukast chitosan lactose nanoparticles microspheres inhalation drug delivery |
| url | https://www.mdpi.com/2073-4360/14/17/3564 |
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