The Evaluation of Meloxicam Nanocrystals by Oral Administration with Different Particle Sizes
Meloxicam (MLX) is a non-steroidal anti-inflammatory drug used to treat rheumatoid arthritis and osteoarthritis. However, its poor water solubility limits the dissolution process and influences absorption. In order to solve this problem and improve its bioavailability, we prepared it in nanocrystals...
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| Format: | Article |
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MDPI AG
2022-01-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/2/421 |
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| author | Yao Yu Yang Tian Hui Zhang Qingxian Jia Xuejun Chen Dongzhou Kang Yimeng Du Shenghan Song Aiping Zheng |
| author_facet | Yao Yu Yang Tian Hui Zhang Qingxian Jia Xuejun Chen Dongzhou Kang Yimeng Du Shenghan Song Aiping Zheng |
| author_sort | Yao Yu |
| collection | DOAJ |
| description | Meloxicam (MLX) is a non-steroidal anti-inflammatory drug used to treat rheumatoid arthritis and osteoarthritis. However, its poor water solubility limits the dissolution process and influences absorption. In order to solve this problem and improve its bioavailability, we prepared it in nanocrystals with three different particle sizes to improve solubility and compare the differences between various particle sizes. The nanocrystal particle sizes were studied through dynamic light scattering (DLS) and laser scattering (LS). Transmission electron microscopy (TEM) was used to characterize the morphology of nanocrystals. The sizes of meloxicam-nanocrystals-A (MLX-NCs-A), meloxicam-nanocrystals-B (MLX-NCs-B), and meloxicam-nanocrystals-C (MLX-NCs-C) were 3.262 ± 0.016 μm, 460.2 ± 9.5 nm, and 204.9 ± 2.8 nm, respectively. Molecular simulation was used to explore the distribution and interaction energy of MLX molecules and stabilizer molecules in water. The results of differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) proved that the crystalline state did not change in the preparation process. Transport studies of the Caco-2 cell model indicated that the cumulative degree of transport would increase as the particle size decreased. Additionally, plasma concentration–time curves showed that the AUC<sub>0–∞</sub> of MLX-NCs-C were 3.58- and 2.92-fold greater than those of MLX-NCs-A and MLX-NCs-B, respectively. These results indicate that preparing MLX in nanocrystals can effectively improve the bioavailability, and the particle size of nanocrystals is an important factor in transmission and absorption. |
| first_indexed | 2024-03-10T00:50:37Z |
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| id | doaj.art-173dc3da471a4fe0af1e6710e0a954fb |
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| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T00:50:37Z |
| publishDate | 2022-01-01 |
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| series | Molecules |
| spelling | doaj.art-173dc3da471a4fe0af1e6710e0a954fb2023-11-23T14:51:41ZengMDPI AGMolecules1420-30492022-01-0127242110.3390/molecules27020421The Evaluation of Meloxicam Nanocrystals by Oral Administration with Different Particle SizesYao Yu0Yang Tian1Hui Zhang2Qingxian Jia3Xuejun Chen4Dongzhou Kang5Yimeng Du6Shenghan Song7Aiping Zheng8Pharmaceutical Experiment Center, College of Pharmacy, Yanbian University, Yanji 133002, ChinaState Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, 27th Taiping Road, Haidian District, Beijing 100850, ChinaState Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, 27th Taiping Road, Haidian District, Beijing 100850, ChinaPharmaceutical Experiment Center, College of Pharmacy, Yanbian University, Yanji 133002, ChinaPharmaceutical Experiment Center, College of Pharmacy, Yanbian University, Yanji 133002, ChinaPharmaceutical Experiment Center, College of Pharmacy, Yanbian University, Yanji 133002, ChinaState Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, 27th Taiping Road, Haidian District, Beijing 100850, ChinaDepartment of Vascular Surgery, Beijing Chaoyang Hospital, Capital Medical University, Beijing 100020, ChinaState Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, 27th Taiping Road, Haidian District, Beijing 100850, ChinaMeloxicam (MLX) is a non-steroidal anti-inflammatory drug used to treat rheumatoid arthritis and osteoarthritis. However, its poor water solubility limits the dissolution process and influences absorption. In order to solve this problem and improve its bioavailability, we prepared it in nanocrystals with three different particle sizes to improve solubility and compare the differences between various particle sizes. The nanocrystal particle sizes were studied through dynamic light scattering (DLS) and laser scattering (LS). Transmission electron microscopy (TEM) was used to characterize the morphology of nanocrystals. The sizes of meloxicam-nanocrystals-A (MLX-NCs-A), meloxicam-nanocrystals-B (MLX-NCs-B), and meloxicam-nanocrystals-C (MLX-NCs-C) were 3.262 ± 0.016 μm, 460.2 ± 9.5 nm, and 204.9 ± 2.8 nm, respectively. Molecular simulation was used to explore the distribution and interaction energy of MLX molecules and stabilizer molecules in water. The results of differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) proved that the crystalline state did not change in the preparation process. Transport studies of the Caco-2 cell model indicated that the cumulative degree of transport would increase as the particle size decreased. Additionally, plasma concentration–time curves showed that the AUC<sub>0–∞</sub> of MLX-NCs-C were 3.58- and 2.92-fold greater than those of MLX-NCs-A and MLX-NCs-B, respectively. These results indicate that preparing MLX in nanocrystals can effectively improve the bioavailability, and the particle size of nanocrystals is an important factor in transmission and absorption.https://www.mdpi.com/1420-3049/27/2/421meloxicamnanocrystalparticle sizesmolecular simulationpharmacokinetic |
| spellingShingle | Yao Yu Yang Tian Hui Zhang Qingxian Jia Xuejun Chen Dongzhou Kang Yimeng Du Shenghan Song Aiping Zheng The Evaluation of Meloxicam Nanocrystals by Oral Administration with Different Particle Sizes Molecules meloxicam nanocrystal particle sizes molecular simulation pharmacokinetic |
| title | The Evaluation of Meloxicam Nanocrystals by Oral Administration with Different Particle Sizes |
| title_full | The Evaluation of Meloxicam Nanocrystals by Oral Administration with Different Particle Sizes |
| title_fullStr | The Evaluation of Meloxicam Nanocrystals by Oral Administration with Different Particle Sizes |
| title_full_unstemmed | The Evaluation of Meloxicam Nanocrystals by Oral Administration with Different Particle Sizes |
| title_short | The Evaluation of Meloxicam Nanocrystals by Oral Administration with Different Particle Sizes |
| title_sort | evaluation of meloxicam nanocrystals by oral administration with different particle sizes |
| topic | meloxicam nanocrystal particle sizes molecular simulation pharmacokinetic |
| url | https://www.mdpi.com/1420-3049/27/2/421 |
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