Preparation and characterization of naproxen solid dispersion using different hydrophilic carriers and in-vivo evaluation of its analgesic activity in mice
Background: Solid dispersion (SD) has been used conventionally as a successful technique for improving the dissolution profile and bioavailability of poorly water-soluble drugs. The aim of this study was to progress the dissolution rate and bioavailability of naproxen (BCS class II) by SD technique....
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| Format: | Article |
| Language: | English |
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Elsevier
2023-05-01
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| Series: | Heliyon |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2405844023026397 |
| _version_ | 1797815702380347392 |
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| author | Monia Akter Nupur Mst Mahfuza Rahman Khurshida Akter Khadiza Binte Hanif Jinat Fatema Sharna Md Shahin Sarker Mir Imam Ibne Wahed |
| author_facet | Monia Akter Nupur Mst Mahfuza Rahman Khurshida Akter Khadiza Binte Hanif Jinat Fatema Sharna Md Shahin Sarker Mir Imam Ibne Wahed |
| author_sort | Monia Akter Nupur |
| collection | DOAJ |
| description | Background: Solid dispersion (SD) has been used conventionally as a successful technique for improving the dissolution profile and bioavailability of poorly water-soluble drugs. The aim of this study was to progress the dissolution rate and bioavailability of naproxen (BCS class II) by SD technique. Materials & methods: In this study, hydrophilic carriers are used for preparing solid dispersion of naproxen by evaporation method. The prepared optimized SDNs were evaluated by in-vitro drug dissolution test, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The in-vivo analgesic effects tests of the optimized SDNs (SDN-2 and SDN-5) were performed by tail immersion method and writhing method. Results: All the prepared SDNs exhibited a significant increase in the dissolution of naproxen compared to that of the pure drug. Among them, SDN-2 (the dispersion with sodium starch glycolate at 1:2 ratio of naproxen and sodium starch glycolate) and SDN-5 (using the combination of PEG-8000 and sodium starch glycolate with naproxen at 1:1:1 ratio) showed faster dissolution rate as compared to other solid dispersions (SDNs) and pure naproxen. SDN-2 showed 5.4 times better dissolution rate and SDN-5 depicted 6.5-fold increment of dissolution rate compared to pure naproxen drug. DSC, PXRD and SEM microscopy showed that the drugs crystallinity was decreased during the preparation process. FTIR study revealed that naproxen was stable in polymeric dispersions and there was no interaction among the drug and polymers. In writhing method, the percentage inhibition of the number of writhes showed significantly greater (p < 0.01), (p < 0.0001) analgesic activity for the higher dose treatment groups SDN-2(H), and SDN-5(H), respectively, when contrasted to the pure drug naproxen. For tail immersion test, there is increase in latency time at 90 min which is significantly greater (P < 0.01), (P < 0.05), (P < 0.01) for treatment groups SDN-2(H), SDN-5(L), and SDN-5(H), respectively that ultimately authenticates that the optimized SDNs (SDN-2, SDN-5) showed better analgesic activity in mice in comparison with the pure drug. Conclusion: It can be concluded that dissolution of the naproxen could be improved by the making solid dispersion using sodium starch glycolate and/or combination of sodium starch glycolate and PEG 8000 due to the complete transformation of drug into amorphous form with the entire loss of crystallinity, as evidenced by DSC, PXRD, and SEM and also consequences the enhanced analgesic activity in mice. |
| first_indexed | 2024-03-13T08:26:40Z |
| format | Article |
| id | doaj.art-4d841424d9d24bdfbe939bfa529ac4c4 |
| institution | Directory Open Access Journal |
| issn | 2405-8440 |
| language | English |
| last_indexed | 2024-03-13T08:26:40Z |
| publishDate | 2023-05-01 |
| publisher | Elsevier |
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| series | Heliyon |
| spelling | doaj.art-4d841424d9d24bdfbe939bfa529ac4c42023-05-31T04:44:35ZengElsevierHeliyon2405-84402023-05-0195e15432Preparation and characterization of naproxen solid dispersion using different hydrophilic carriers and in-vivo evaluation of its analgesic activity in miceMonia Akter Nupur0Mst Mahfuza Rahman1Khurshida Akter2Khadiza Binte Hanif3Jinat Fatema Sharna4Md Shahin Sarker5Mir Imam Ibne Wahed6Department of Pharmacy, Comilla University, Cumilla, 3506, BangladeshDepartment of Pharmacy, Comilla University, Cumilla, 3506, Bangladesh; Corresponding author.Department of Pharmacy, Comilla University, Cumilla, 3506, BangladeshDepartment of Pharmacy, Comilla University, Cumilla, 3506, BangladeshDepartment of Pharmacy, Comilla University, Cumilla, 3506, BangladeshDepartment of Pharmacy, Jashore University of Science &Technology, Jashore, 7408, BangladeshDepartment of Pharmacy, Faculty of Science, University of Rajshahi, Rajshahi, 6205, BangladeshBackground: Solid dispersion (SD) has been used conventionally as a successful technique for improving the dissolution profile and bioavailability of poorly water-soluble drugs. The aim of this study was to progress the dissolution rate and bioavailability of naproxen (BCS class II) by SD technique. Materials & methods: In this study, hydrophilic carriers are used for preparing solid dispersion of naproxen by evaporation method. The prepared optimized SDNs were evaluated by in-vitro drug dissolution test, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The in-vivo analgesic effects tests of the optimized SDNs (SDN-2 and SDN-5) were performed by tail immersion method and writhing method. Results: All the prepared SDNs exhibited a significant increase in the dissolution of naproxen compared to that of the pure drug. Among them, SDN-2 (the dispersion with sodium starch glycolate at 1:2 ratio of naproxen and sodium starch glycolate) and SDN-5 (using the combination of PEG-8000 and sodium starch glycolate with naproxen at 1:1:1 ratio) showed faster dissolution rate as compared to other solid dispersions (SDNs) and pure naproxen. SDN-2 showed 5.4 times better dissolution rate and SDN-5 depicted 6.5-fold increment of dissolution rate compared to pure naproxen drug. DSC, PXRD and SEM microscopy showed that the drugs crystallinity was decreased during the preparation process. FTIR study revealed that naproxen was stable in polymeric dispersions and there was no interaction among the drug and polymers. In writhing method, the percentage inhibition of the number of writhes showed significantly greater (p < 0.01), (p < 0.0001) analgesic activity for the higher dose treatment groups SDN-2(H), and SDN-5(H), respectively, when contrasted to the pure drug naproxen. For tail immersion test, there is increase in latency time at 90 min which is significantly greater (P < 0.01), (P < 0.05), (P < 0.01) for treatment groups SDN-2(H), SDN-5(L), and SDN-5(H), respectively that ultimately authenticates that the optimized SDNs (SDN-2, SDN-5) showed better analgesic activity in mice in comparison with the pure drug. Conclusion: It can be concluded that dissolution of the naproxen could be improved by the making solid dispersion using sodium starch glycolate and/or combination of sodium starch glycolate and PEG 8000 due to the complete transformation of drug into amorphous form with the entire loss of crystallinity, as evidenced by DSC, PXRD, and SEM and also consequences the enhanced analgesic activity in mice.http://www.sciencedirect.com/science/article/pii/S2405844023026397NaproxenSolid dispersionPEG 8000Sodium starch glycolateAnalgesic activitysolvent evaporation method |
| spellingShingle | Monia Akter Nupur Mst Mahfuza Rahman Khurshida Akter Khadiza Binte Hanif Jinat Fatema Sharna Md Shahin Sarker Mir Imam Ibne Wahed Preparation and characterization of naproxen solid dispersion using different hydrophilic carriers and in-vivo evaluation of its analgesic activity in mice Heliyon Naproxen Solid dispersion PEG 8000 Sodium starch glycolate Analgesic activity solvent evaporation method |
| title | Preparation and characterization of naproxen solid dispersion using different hydrophilic carriers and in-vivo evaluation of its analgesic activity in mice |
| title_full | Preparation and characterization of naproxen solid dispersion using different hydrophilic carriers and in-vivo evaluation of its analgesic activity in mice |
| title_fullStr | Preparation and characterization of naproxen solid dispersion using different hydrophilic carriers and in-vivo evaluation of its analgesic activity in mice |
| title_full_unstemmed | Preparation and characterization of naproxen solid dispersion using different hydrophilic carriers and in-vivo evaluation of its analgesic activity in mice |
| title_short | Preparation and characterization of naproxen solid dispersion using different hydrophilic carriers and in-vivo evaluation of its analgesic activity in mice |
| title_sort | preparation and characterization of naproxen solid dispersion using different hydrophilic carriers and in vivo evaluation of its analgesic activity in mice |
| topic | Naproxen Solid dispersion PEG 8000 Sodium starch glycolate Analgesic activity solvent evaporation method |
| url | http://www.sciencedirect.com/science/article/pii/S2405844023026397 |
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