Smartcrystals for Efficient Dissolution of Poorly Water-Soluble Meloxicam
Nanocrystal is widely applied to improve the dissolution of poorly water-soluble drugs. We aimed to prepare meloxicam (MLX) nanocrystals using the bead mill method, followed by high-pressure homogenization (HPH). Simple drying at room temperature (RD), vacuum-drying (VD), and freeze-drying (FD) usin...
| Main Authors: | , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2022-01-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1999-4923/14/2/245 |
| _version_ | 1797477234374606848 |
|---|---|
| author | Rita Ambrus Areen Alshweiat Piroska Szabó-Révész Csilla Bartos Ildikó Csóka |
| author_facet | Rita Ambrus Areen Alshweiat Piroska Szabó-Révész Csilla Bartos Ildikó Csóka |
| author_sort | Rita Ambrus |
| collection | DOAJ |
| description | Nanocrystal is widely applied to improve the dissolution of poorly water-soluble drugs. We aimed to prepare meloxicam (MLX) nanocrystals using the bead mill method, followed by high-pressure homogenization (HPH). Simple drying at room temperature (RD), vacuum-drying (VD), and freeze-drying (FD) using mannitol or trehalose as a cryoprotectant were applied to obtain dry nanocrystals. The nanocrystals were fully characterized. The MLX nanosuspension containing 5% <i>w/v</i> MLX and 1% <i>w/v</i> of Pluronic F68 showing a mean particle size (MPS) of 242 nm and a polydispersity index (PDI) of 0.36 was prepared after 40 min of premilling and 30 min of HPH. The dried nanocrystals were spherical within the nano range. DSC and XRPD confirmed the absence of MLX amorphization. The smartcrystals showed enhanced MLX release. Approximately 100% release was achieved with phosphate buffer (PB), pH 5.6, and 80% was released with PB, pH 7.4, from the freeze-dried samples. The results revealed the effects of the drying method and cryoprotectant type on the properties of dry nanocrystals. The freeze-dried samples showed the smallest particle size, in particular trehalose-based samples. On the other hand, mannitol-based dried samples showed the highest crystallinity index among all nanocrystals (77.8%), whereas trehalose showed the lowest (59.2%). These factors explained the dissolution differences among the samples. |
| first_indexed | 2024-03-09T21:14:45Z |
| format | Article |
| id | doaj.art-2f1fc5ec0791480ea3097535bdb98bcb |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T21:14:45Z |
| publishDate | 2022-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-2f1fc5ec0791480ea3097535bdb98bcb2023-11-23T21:36:03ZengMDPI AGPharmaceutics1999-49232022-01-0114224510.3390/pharmaceutics14020245Smartcrystals for Efficient Dissolution of Poorly Water-Soluble MeloxicamRita Ambrus0Areen Alshweiat1Piroska Szabó-Révész2Csilla Bartos3Ildikó Csóka4Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, HungaryDepartment of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, The Hashemite University, Zarqa 13133, JordanInstitute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, HungaryInstitute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, HungaryInstitute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, HungaryNanocrystal is widely applied to improve the dissolution of poorly water-soluble drugs. We aimed to prepare meloxicam (MLX) nanocrystals using the bead mill method, followed by high-pressure homogenization (HPH). Simple drying at room temperature (RD), vacuum-drying (VD), and freeze-drying (FD) using mannitol or trehalose as a cryoprotectant were applied to obtain dry nanocrystals. The nanocrystals were fully characterized. The MLX nanosuspension containing 5% <i>w/v</i> MLX and 1% <i>w/v</i> of Pluronic F68 showing a mean particle size (MPS) of 242 nm and a polydispersity index (PDI) of 0.36 was prepared after 40 min of premilling and 30 min of HPH. The dried nanocrystals were spherical within the nano range. DSC and XRPD confirmed the absence of MLX amorphization. The smartcrystals showed enhanced MLX release. Approximately 100% release was achieved with phosphate buffer (PB), pH 5.6, and 80% was released with PB, pH 7.4, from the freeze-dried samples. The results revealed the effects of the drying method and cryoprotectant type on the properties of dry nanocrystals. The freeze-dried samples showed the smallest particle size, in particular trehalose-based samples. On the other hand, mannitol-based dried samples showed the highest crystallinity index among all nanocrystals (77.8%), whereas trehalose showed the lowest (59.2%). These factors explained the dissolution differences among the samples.https://www.mdpi.com/1999-4923/14/2/245dryingmeloxicamsmartcrystalsmillinghigh-pressure homogenizationnanosuspension |
| spellingShingle | Rita Ambrus Areen Alshweiat Piroska Szabó-Révész Csilla Bartos Ildikó Csóka Smartcrystals for Efficient Dissolution of Poorly Water-Soluble Meloxicam Pharmaceutics drying meloxicam smartcrystals milling high-pressure homogenization nanosuspension |
| title | Smartcrystals for Efficient Dissolution of Poorly Water-Soluble Meloxicam |
| title_full | Smartcrystals for Efficient Dissolution of Poorly Water-Soluble Meloxicam |
| title_fullStr | Smartcrystals for Efficient Dissolution of Poorly Water-Soluble Meloxicam |
| title_full_unstemmed | Smartcrystals for Efficient Dissolution of Poorly Water-Soluble Meloxicam |
| title_short | Smartcrystals for Efficient Dissolution of Poorly Water-Soluble Meloxicam |
| title_sort | smartcrystals for efficient dissolution of poorly water soluble meloxicam |
| topic | drying meloxicam smartcrystals milling high-pressure homogenization nanosuspension |
| url | https://www.mdpi.com/1999-4923/14/2/245 |
| work_keys_str_mv | AT ritaambrus smartcrystalsforefficientdissolutionofpoorlywatersolublemeloxicam AT areenalshweiat smartcrystalsforefficientdissolutionofpoorlywatersolublemeloxicam AT piroskaszaborevesz smartcrystalsforefficientdissolutionofpoorlywatersolublemeloxicam AT csillabartos smartcrystalsforefficientdissolutionofpoorlywatersolublemeloxicam AT ildikocsoka smartcrystalsforefficientdissolutionofpoorlywatersolublemeloxicam |