Nanoparticles of thiolated chitosan for controlled delivery of moxifloxacin: In-vitro and in-vivo evaluation
Controlled release drug delivery system of moxifloxacin produces better therapeutic effects and maintain the plasma concentration for prolong period of time. The objective of this work was to formulate nanoparticles of thiolated chitosan (TC) having enhanced mucoadhesion and controlled release behav...
| Main Authors: | , , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2022-10-01
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| Series: | Journal of King Saud University: Science |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S1018364722003998 |
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| author | Ghulam Abbas Akhtar Rasul M. Fakhar-e-Alam Malik Saadullah Saima Muzammil Omeira Iqbal M. Atif Muhammad Hanif Shahid Shah Shafiq Ahmad Sulman Shafeeq Muhammad Afzal |
| author_facet | Ghulam Abbas Akhtar Rasul M. Fakhar-e-Alam Malik Saadullah Saima Muzammil Omeira Iqbal M. Atif Muhammad Hanif Shahid Shah Shafiq Ahmad Sulman Shafeeq Muhammad Afzal |
| author_sort | Ghulam Abbas |
| collection | DOAJ |
| description | Controlled release drug delivery system of moxifloxacin produces better therapeutic effects and maintain the plasma concentration for prolong period of time. The objective of this work was to formulate nanoparticles of thiolated chitosan (TC) having enhanced mucoadhesion and controlled release behaviour of drug. The chitosan (CS) was thiolated by conjugation with thiourea. Ionic gelation method using TC was used for the preparation of the nanoparticles. FTIR, DSC, TGA and 1H NMR were used to characterize the CS and TC. The measurement of particle size and zeta potential of the developed nanoparticles confirmed that the formulation was stable. The CS, TC and nanoparticles were evaluated for mucoadhesion and swelling. The toxicity of developed nanoparticles was evaluated by Caco-2 cell line. The release of drug from nanoparticles of non-thiolated (NT) and TC was studied using simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and phosphate buffer pH 7.4. The albino rats were used to investigate the moxifloxacin pharmacokinetics from nanoparticles of TC. The thiol group showed peak at 2122 cm−1 which was confirmed by FTIR. The thermal stability of NT and TC was confirmed by DSC and TGA. The thiolation of CS was confirmed by 1H NMR. The nanoparticle of TCN3 showed 105 nm average particle size and zeta potential of TCN1 to TCN5 was range from −18 to + 29. The TC show better mucoadhesion as compare to the CS. The drug, CS, TC and nanoparticles of TCN3 did not exhibit any effect on the viability of Caco-2 cells. In SGF, the drug release from nanoparticles was 5 to 10 %. TCN3 formulation showed 97.84% and 99.43% release of moxifloxacin in SIF and phosphate buffer pH 7.4 within 24 h. The nanoparticles of TCN3 showed 97.13% release of moxifloxacin within 8 h. The TCN3 formulation showed greater bioavailability and improved pharmacokinetic parameters of moxifloxacin as compare to the marketed formulation. Our findings proved that the thiolation of CS with thiourea is an easy and reproducible method to improve the mucoadhesion and the controlled release pattern of the drug over an extended period of time. |
| first_indexed | 2024-04-14T08:24:52Z |
| format | Article |
| id | doaj.art-13051926c2c94f8d88f5fb29f0f80b75 |
| institution | Directory Open Access Journal |
| issn | 1018-3647 |
| language | English |
| last_indexed | 2024-04-14T08:24:52Z |
| publishDate | 2022-10-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Journal of King Saud University: Science |
| spelling | doaj.art-13051926c2c94f8d88f5fb29f0f80b752022-12-22T02:04:05ZengElsevierJournal of King Saud University: Science1018-36472022-10-01347102218Nanoparticles of thiolated chitosan for controlled delivery of moxifloxacin: In-vitro and in-vivo evaluationGhulam Abbas0Akhtar Rasul1M. Fakhar-e-Alam2Malik Saadullah3Saima Muzammil4Omeira Iqbal5M. Atif6Muhammad Hanif7Shahid Shah8Shafiq Ahmad9Sulman Shafeeq10Muhammad Afzal11Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, PakistanDepartment of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, PakistanDepartment of Physics, Government College University Faisalabad, PakistanDepartment of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, PakistanDepartmant of Microbiology, Government College University Faisalabad, Allama Iqbal Road, Faisalabad, PakistanDepartment of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, PakistanDepartment of Physics and Astronomy, College of Science, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University Multan, PakistanDepartment of Pharmacy Practice, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Pakistan; Corresponding authors.Industrial Engineering Department, College of Engineering, King Saud University, P.O. Box 800, Riyadh 11421, Saudi ArabiaDepartment of Microbiology, Tumor and Cell Biology, Karolinska Institute, Stockholm, Sweden; Corresponding authors.Departmant of Bioinformatics and Biotechnology, Government College University Faisalabad, Allama Iqbal Road, Faisalabad, PakistanControlled release drug delivery system of moxifloxacin produces better therapeutic effects and maintain the plasma concentration for prolong period of time. The objective of this work was to formulate nanoparticles of thiolated chitosan (TC) having enhanced mucoadhesion and controlled release behaviour of drug. The chitosan (CS) was thiolated by conjugation with thiourea. Ionic gelation method using TC was used for the preparation of the nanoparticles. FTIR, DSC, TGA and 1H NMR were used to characterize the CS and TC. The measurement of particle size and zeta potential of the developed nanoparticles confirmed that the formulation was stable. The CS, TC and nanoparticles were evaluated for mucoadhesion and swelling. The toxicity of developed nanoparticles was evaluated by Caco-2 cell line. The release of drug from nanoparticles of non-thiolated (NT) and TC was studied using simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and phosphate buffer pH 7.4. The albino rats were used to investigate the moxifloxacin pharmacokinetics from nanoparticles of TC. The thiol group showed peak at 2122 cm−1 which was confirmed by FTIR. The thermal stability of NT and TC was confirmed by DSC and TGA. The thiolation of CS was confirmed by 1H NMR. The nanoparticle of TCN3 showed 105 nm average particle size and zeta potential of TCN1 to TCN5 was range from −18 to + 29. The TC show better mucoadhesion as compare to the CS. The drug, CS, TC and nanoparticles of TCN3 did not exhibit any effect on the viability of Caco-2 cells. In SGF, the drug release from nanoparticles was 5 to 10 %. TCN3 formulation showed 97.84% and 99.43% release of moxifloxacin in SIF and phosphate buffer pH 7.4 within 24 h. The nanoparticles of TCN3 showed 97.13% release of moxifloxacin within 8 h. The TCN3 formulation showed greater bioavailability and improved pharmacokinetic parameters of moxifloxacin as compare to the marketed formulation. Our findings proved that the thiolation of CS with thiourea is an easy and reproducible method to improve the mucoadhesion and the controlled release pattern of the drug over an extended period of time.http://www.sciencedirect.com/science/article/pii/S1018364722003998NanoparticlesChitosanThiolationIn-vitro releasePharmacokinetics |
| spellingShingle | Ghulam Abbas Akhtar Rasul M. Fakhar-e-Alam Malik Saadullah Saima Muzammil Omeira Iqbal M. Atif Muhammad Hanif Shahid Shah Shafiq Ahmad Sulman Shafeeq Muhammad Afzal Nanoparticles of thiolated chitosan for controlled delivery of moxifloxacin: In-vitro and in-vivo evaluation Journal of King Saud University: Science Nanoparticles Chitosan Thiolation In-vitro release Pharmacokinetics |
| title | Nanoparticles of thiolated chitosan for controlled delivery of moxifloxacin: In-vitro and in-vivo evaluation |
| title_full | Nanoparticles of thiolated chitosan for controlled delivery of moxifloxacin: In-vitro and in-vivo evaluation |
| title_fullStr | Nanoparticles of thiolated chitosan for controlled delivery of moxifloxacin: In-vitro and in-vivo evaluation |
| title_full_unstemmed | Nanoparticles of thiolated chitosan for controlled delivery of moxifloxacin: In-vitro and in-vivo evaluation |
| title_short | Nanoparticles of thiolated chitosan for controlled delivery of moxifloxacin: In-vitro and in-vivo evaluation |
| title_sort | nanoparticles of thiolated chitosan for controlled delivery of moxifloxacin in vitro and in vivo evaluation |
| topic | Nanoparticles Chitosan Thiolation In-vitro release Pharmacokinetics |
| url | http://www.sciencedirect.com/science/article/pii/S1018364722003998 |
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