Synthesis and evaluation of chitosan based controlled release nanoparticles for the delivery of ticagrelor
The aim of this contemporary work was to formulate a controlled release mucoadhesive nanoparticle formulation for enhancing the oral bioavailability of Ticagrelor (TG), a BCS class IV drug, having low oral bioavailability of about 36%. The nanoparticles can act as efficient carriers for hydrophobic...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2022-12-01
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| Series: | Designed Monomers and Polymers |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/15685551.2022.2054117 |
| _version_ | 1797983860022050816 |
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| author | Nariman Shahid Alia Erum Muhammad Zaman Ume Ruqia Tulain Qurat-ul-ain Shoaib Nadia Shamshad Malik Rizwana Kausar Ayesha Rashid Umaira Rehman |
| author_facet | Nariman Shahid Alia Erum Muhammad Zaman Ume Ruqia Tulain Qurat-ul-ain Shoaib Nadia Shamshad Malik Rizwana Kausar Ayesha Rashid Umaira Rehman |
| author_sort | Nariman Shahid |
| collection | DOAJ |
| description | The aim of this contemporary work was to formulate a controlled release mucoadhesive nanoparticle formulation for enhancing the oral bioavailability of Ticagrelor (TG), a BCS class IV drug, having low oral bioavailability of about 36%. The nanoparticles can act as efficient carriers for hydrophobic drugs, due to having high surface area and hence can improve their aqueous solubility due to their hydrophilic nature. The nanoparticles (NPs) of TG were formulated using chitosan (CH) as polymer and sodium tripolyphosphate (TPP) as cross-linker, by ionic gelation technique with varying concentrations of polymer with respect to TG and TPP. Characterization of prepared nanoparticles was carried out to assess zeta potential, size, shape, entrapment efficiency (EE) and loading capacity (LC), using zeta sizer, surface morphology and chemical compatibility analysis. Drug release was observed using UV-Spectrophotometer. By increasing concentration of CH the desired size of particles (106.9 nm), zeta potential (22.6 mv) and poly dispersity index (0.364) was achieved. In vitro profiles showed a controlled and prolonged release of TG in both lower pH-1.2 and neutral pH-7.4 mediums, with effective protection of entrapped TG in simulated gastric conditions. X-ray diffraction patterns (XRD) showed the crystalline nature of formed NPs. Hence, this effort showed that hydrophobic drugs can be effectively encapsulated in nanoparticulate systems to enhance their solubility and stability, ultimately improving their bioavailability and effectiveness with better patient compliance by reducing dosing frequencies as well. |
| first_indexed | 2024-04-11T06:53:46Z |
| format | Article |
| id | doaj.art-b208cd2f3c2d48a3a1a1a4bc124a11cb |
| institution | Directory Open Access Journal |
| issn | 1385-772X 1568-5551 |
| language | English |
| last_indexed | 2024-04-11T06:53:46Z |
| publishDate | 2022-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Designed Monomers and Polymers |
| spelling | doaj.art-b208cd2f3c2d48a3a1a1a4bc124a11cb2022-12-22T04:39:06ZengTaylor & Francis GroupDesigned Monomers and Polymers1385-772X1568-55512022-12-01251556310.1080/15685551.2022.20541172054117Synthesis and evaluation of chitosan based controlled release nanoparticles for the delivery of ticagrelorNariman Shahid0Alia Erum1Muhammad Zaman2Ume Ruqia Tulain3Qurat-ul-ain Shoaib4Nadia Shamshad Malik5Rizwana Kausar6Ayesha Rashid7Umaira Rehman8University of SargodhaUniversity of SargodhaUniversity of Central PunjabUniversity of SargodhaAkhtar Saeed College of Pharmaceutical SciencesCapital University of Science and TechnologyILM College of Pharmaceutical SciencesThe Women University MultanUniversity of SargodhaThe aim of this contemporary work was to formulate a controlled release mucoadhesive nanoparticle formulation for enhancing the oral bioavailability of Ticagrelor (TG), a BCS class IV drug, having low oral bioavailability of about 36%. The nanoparticles can act as efficient carriers for hydrophobic drugs, due to having high surface area and hence can improve their aqueous solubility due to their hydrophilic nature. The nanoparticles (NPs) of TG were formulated using chitosan (CH) as polymer and sodium tripolyphosphate (TPP) as cross-linker, by ionic gelation technique with varying concentrations of polymer with respect to TG and TPP. Characterization of prepared nanoparticles was carried out to assess zeta potential, size, shape, entrapment efficiency (EE) and loading capacity (LC), using zeta sizer, surface morphology and chemical compatibility analysis. Drug release was observed using UV-Spectrophotometer. By increasing concentration of CH the desired size of particles (106.9 nm), zeta potential (22.6 mv) and poly dispersity index (0.364) was achieved. In vitro profiles showed a controlled and prolonged release of TG in both lower pH-1.2 and neutral pH-7.4 mediums, with effective protection of entrapped TG in simulated gastric conditions. X-ray diffraction patterns (XRD) showed the crystalline nature of formed NPs. Hence, this effort showed that hydrophobic drugs can be effectively encapsulated in nanoparticulate systems to enhance their solubility and stability, ultimately improving their bioavailability and effectiveness with better patient compliance by reducing dosing frequencies as well.http://dx.doi.org/10.1080/15685551.2022.2054117nanoparticleschitosanticagrelorhydrophobichydrophilicionic gelationbioavailability |
| spellingShingle | Nariman Shahid Alia Erum Muhammad Zaman Ume Ruqia Tulain Qurat-ul-ain Shoaib Nadia Shamshad Malik Rizwana Kausar Ayesha Rashid Umaira Rehman Synthesis and evaluation of chitosan based controlled release nanoparticles for the delivery of ticagrelor Designed Monomers and Polymers nanoparticles chitosan ticagrelor hydrophobic hydrophilic ionic gelation bioavailability |
| title | Synthesis and evaluation of chitosan based controlled release nanoparticles for the delivery of ticagrelor |
| title_full | Synthesis and evaluation of chitosan based controlled release nanoparticles for the delivery of ticagrelor |
| title_fullStr | Synthesis and evaluation of chitosan based controlled release nanoparticles for the delivery of ticagrelor |
| title_full_unstemmed | Synthesis and evaluation of chitosan based controlled release nanoparticles for the delivery of ticagrelor |
| title_short | Synthesis and evaluation of chitosan based controlled release nanoparticles for the delivery of ticagrelor |
| title_sort | synthesis and evaluation of chitosan based controlled release nanoparticles for the delivery of ticagrelor |
| topic | nanoparticles chitosan ticagrelor hydrophobic hydrophilic ionic gelation bioavailability |
| url | http://dx.doi.org/10.1080/15685551.2022.2054117 |
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