Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate
Nifedipine (NIF) is a 1,4-dihydropyridine-based calcium channel blocker with poor solubility, whose bioavailability is highly dependent on the type of formulation. Dry powder mixtures of 20% w/w NIF with microcrystalline cellulose (MCC) and its high surface area nanocellulose analogue, which is name...
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| Format: | Article |
| Language: | English |
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MDPI AG
2019-01-01
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| Series: | Pharmaceutics |
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| Online Access: | http://www.mdpi.com/1999-4923/11/1/37 |
| _version_ | 1811300070912425984 |
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| author | Athanasios Mantas Albert Mihranyan |
| author_facet | Athanasios Mantas Albert Mihranyan |
| author_sort | Athanasios Mantas |
| collection | DOAJ |
| description | Nifedipine (NIF) is a 1,4-dihydropyridine-based calcium channel blocker with poor solubility, whose bioavailability is highly dependent on the type of formulation. Dry powder mixtures of 20% w/w NIF with microcrystalline cellulose (MCC) and its high surface area nanocellulose analogue, which is namely Cladophora (CLAD) cellulose, were produced by heating at the melting temperature of the drug for 1 h. Non-heated samples were used as a reference. The solid-state properties of the mixtures were characterized by scanning electron microscopy, differential scanning calorimetry and X-ray diffraction. The drug release was studied in biorelevant media, including simulated gastric fluid (SGF), fasted-state simulated intestinal fluid (FaSIF) and fed-state simulated intestinal fluid (FeSIF). An enhanced apparent solubility and faster dissolution rate of NIF were observed in the heated mixture of NIF with CLAD-H in all tested biorelevant media (i.e., SGF, FaSIF and FeSIF), which was due to NIF amorphization in the high surface area nanocellulose powder. Ordinary MCC, which is essentially non-porous, did not produce an enhancement of a similar magnitude. The results of the study suggest that dry powder formulation using high surface area nanocellulose is a facile new strategy for formulating calcium channel blocker drugs, which could potentially be a viable alternative to currently used soft gel liquid capsules. |
| first_indexed | 2024-04-13T06:45:52Z |
| format | Article |
| id | doaj.art-a621a7f586014303964b38949515f3e0 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-13T06:45:52Z |
| publishDate | 2019-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-a621a7f586014303964b38949515f3e02022-12-22T02:57:35ZengMDPI AGPharmaceutics1999-49232019-01-011113710.3390/pharmaceutics11010037pharmaceutics11010037Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution RateAthanasios Mantas0Albert Mihranyan1Nanotechnology and Functional Materials, Department of Engineering Sciences, Uppsala University, 75121 Uppsala, SwedenNanotechnology and Functional Materials, Department of Engineering Sciences, Uppsala University, 75121 Uppsala, SwedenNifedipine (NIF) is a 1,4-dihydropyridine-based calcium channel blocker with poor solubility, whose bioavailability is highly dependent on the type of formulation. Dry powder mixtures of 20% w/w NIF with microcrystalline cellulose (MCC) and its high surface area nanocellulose analogue, which is namely Cladophora (CLAD) cellulose, were produced by heating at the melting temperature of the drug for 1 h. Non-heated samples were used as a reference. The solid-state properties of the mixtures were characterized by scanning electron microscopy, differential scanning calorimetry and X-ray diffraction. The drug release was studied in biorelevant media, including simulated gastric fluid (SGF), fasted-state simulated intestinal fluid (FaSIF) and fed-state simulated intestinal fluid (FeSIF). An enhanced apparent solubility and faster dissolution rate of NIF were observed in the heated mixture of NIF with CLAD-H in all tested biorelevant media (i.e., SGF, FaSIF and FeSIF), which was due to NIF amorphization in the high surface area nanocellulose powder. Ordinary MCC, which is essentially non-porous, did not produce an enhancement of a similar magnitude. The results of the study suggest that dry powder formulation using high surface area nanocellulose is a facile new strategy for formulating calcium channel blocker drugs, which could potentially be a viable alternative to currently used soft gel liquid capsules.http://www.mdpi.com/1999-4923/11/1/37amorphous solid dispersionscalcium channel blockersbiorelevant mediaCladophora cellulose |
| spellingShingle | Athanasios Mantas Albert Mihranyan Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate Pharmaceutics amorphous solid dispersions calcium channel blockers biorelevant media Cladophora cellulose |
| title | Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate |
| title_full | Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate |
| title_fullStr | Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate |
| title_full_unstemmed | Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate |
| title_short | Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate |
| title_sort | immediate release nifedipine binary dry powder mixtures with nanocellulose featuring enhanced solubility and dissolution rate |
| topic | amorphous solid dispersions calcium channel blockers biorelevant media Cladophora cellulose |
| url | http://www.mdpi.com/1999-4923/11/1/37 |
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