In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes
Mefenamic acid (MFA) is a hydrophobic drug with low dissolution rate. This study aimed to develop stable and reproducible aqueous formulations of MFA using liposomes as drug carriers. The drug entrapment, particles size and drug release profiles, and stability and reproducibility of the liposomes we...
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| Format: | Article |
| Language: | English |
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Universidade de Sao Paulo
2019
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| Online Access: | http://psasir.upm.edu.my/id/eprint/80220/1/In%20vitro%20characterization%20and%20in%20vivo%20performance%20of%20mefenamic%20acid-sodium%20diethyldithiocarbamate%20based%20liposomes.pdf |
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| author | Jarrar, Qais Bashir Mahmoud Abdullah, Muhammad Nazrul Hakim Cheema, Manraj Singh Zakaria, Zainul Amiruddin |
| author_facet | Jarrar, Qais Bashir Mahmoud Abdullah, Muhammad Nazrul Hakim Cheema, Manraj Singh Zakaria, Zainul Amiruddin |
| author_sort | Jarrar, Qais Bashir Mahmoud |
| collection | UPM |
| description | Mefenamic acid (MFA) is a hydrophobic drug with low dissolution rate. This study aimed to develop stable and reproducible aqueous formulations of MFA using liposomes as drug carriers. The drug entrapment, particles size and drug release profiles, and stability and reproducibility of the liposomes were determined. In addition, the maximum tolerated dose (MTD) was determined in rats via the oral
and intraperitoneal routes of administration. Also, the anti-inflammatory efficacy of these liposomes was evaluated using carrageenan-induced paw edema model in rats. MFA-DDC based liposomes demonstrated a drug entrapment efficacy of 93.6%, particles size of 170.9 nm, and polydispersity index of 0.24 which were not statistically affected when stored in room and refrigerated temperatures for at least 4 weeks. The MTD of the intraperitoneally administrated MFA-loaded liposomes was 20 mg MFA/kg, whereas for those of oral administrations, it was up to 80 mg MFA/kg. Intraperitoneal dose (80 mg MFA/kg) of MFA-DDC liposomes induced extrapyramidal symptoms associated with significant elevation in serum potassium and muscle enzymes. Moreover, significant inhibition of paw edema was demonstrated by the oral and intraperitoneal routes. These findings suggest that MFA-DDC based liposomes are an effective formulation of MFA and recommend the use of bioequivalence assessments with commercial formulations. |
| first_indexed | 2024-03-06T10:27:35Z |
| format | Article |
| id | upm.eprints-80220 |
| institution | Universiti Putra Malaysia |
| language | English |
| last_indexed | 2024-03-06T10:27:35Z |
| publishDate | 2019 |
| publisher | Universidade de Sao Paulo |
| record_format | dspace |
| spelling | upm.eprints-802202020-10-02T08:29:59Z http://psasir.upm.edu.my/id/eprint/80220/ In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes Jarrar, Qais Bashir Mahmoud Abdullah, Muhammad Nazrul Hakim Cheema, Manraj Singh Zakaria, Zainul Amiruddin Mefenamic acid (MFA) is a hydrophobic drug with low dissolution rate. This study aimed to develop stable and reproducible aqueous formulations of MFA using liposomes as drug carriers. The drug entrapment, particles size and drug release profiles, and stability and reproducibility of the liposomes were determined. In addition, the maximum tolerated dose (MTD) was determined in rats via the oral and intraperitoneal routes of administration. Also, the anti-inflammatory efficacy of these liposomes was evaluated using carrageenan-induced paw edema model in rats. MFA-DDC based liposomes demonstrated a drug entrapment efficacy of 93.6%, particles size of 170.9 nm, and polydispersity index of 0.24 which were not statistically affected when stored in room and refrigerated temperatures for at least 4 weeks. The MTD of the intraperitoneally administrated MFA-loaded liposomes was 20 mg MFA/kg, whereas for those of oral administrations, it was up to 80 mg MFA/kg. Intraperitoneal dose (80 mg MFA/kg) of MFA-DDC liposomes induced extrapyramidal symptoms associated with significant elevation in serum potassium and muscle enzymes. Moreover, significant inhibition of paw edema was demonstrated by the oral and intraperitoneal routes. These findings suggest that MFA-DDC based liposomes are an effective formulation of MFA and recommend the use of bioequivalence assessments with commercial formulations. Universidade de Sao Paulo 2019 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/80220/1/In%20vitro%20characterization%20and%20in%20vivo%20performance%20of%20mefenamic%20acid-sodium%20diethyldithiocarbamate%20based%20liposomes.pdf Jarrar, Qais Bashir Mahmoud and Abdullah, Muhammad Nazrul Hakim and Cheema, Manraj Singh and Zakaria, Zainul Amiruddin (2019) In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes. Brazilian Journal of Pharmaceutical Sciences, 55 (1). pp. 1-13. ISSN 1984-8250; ESSN: 2175-9790 https://www.researchgate.net/publication/336887556_In_vitro_characterization_and_in_vivo_performance_of_mefenamic_acid-sodium_diethyldithiocarbamate_based_liposomes 10.1590/s2175-97902019000117870 |
| spellingShingle | Jarrar, Qais Bashir Mahmoud Abdullah, Muhammad Nazrul Hakim Cheema, Manraj Singh Zakaria, Zainul Amiruddin In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes |
| title | In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes |
| title_full | In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes |
| title_fullStr | In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes |
| title_full_unstemmed | In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes |
| title_short | In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes |
| title_sort | in vitro characterization and in vivo performance of mefenamic acid sodium diethyldithiocarbamate based liposomes |
| url | http://psasir.upm.edu.my/id/eprint/80220/1/In%20vitro%20characterization%20and%20in%20vivo%20performance%20of%20mefenamic%20acid-sodium%20diethyldithiocarbamate%20based%20liposomes.pdf |
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