Microwave-Induced In Situ Amorphization: A New Strategy for Tackling the Stability Issue of Amorphous Solid Dispersions
The thermodynamically unstable nature of amorphous drugs has led to a persistent stability issue of amorphous solid dispersions (ASDs). Lately, microwave-induced in situ amorphization has been proposed as a promising solution to this problem, where the originally loaded crystalline drug is in situ a...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-07-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/12/7/655 |
| _version_ | 1827713247454691328 |
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| author | Wei Qiang Korbinian Löbmann Colin P. McCoy Gavin P. Andrews Min Zhao |
| author_facet | Wei Qiang Korbinian Löbmann Colin P. McCoy Gavin P. Andrews Min Zhao |
| author_sort | Wei Qiang |
| collection | DOAJ |
| description | The thermodynamically unstable nature of amorphous drugs has led to a persistent stability issue of amorphous solid dispersions (ASDs). Lately, microwave-induced in situ amorphization has been proposed as a promising solution to this problem, where the originally loaded crystalline drug is in situ amorphized within the final dosage form using a household microwave oven prior to oral administration. In addition to circumventing issues with physical stability, it can also simplify the problematic downstream processing of ASDs. In this review paper, we address the significance of exploring and developing this novel technology with an emphasis on systemically reviewing the currently available literature in this pharmaceutical arena and highlighting the underlying mechanisms involved in inducing in situ amorphization. Specifically, in order to achieve a high drug amorphicity, formulations should be composed of drugs with high solubility in polymers, as well as polymers with high hygroscopicity and good post-plasticized flexibility of chains. Furthermore, high microwave energy input is considered to be a desirable factor. Lastly, this review discusses challenges in the development of this technology including chemical stability, selection criteria for excipients and the dissolution performance of the microwave-induced ASDs. |
| first_indexed | 2024-03-10T18:32:19Z |
| format | Article |
| id | doaj.art-1e31102a61fc4a479b2a8a3084b84685 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T18:32:19Z |
| publishDate | 2020-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-1e31102a61fc4a479b2a8a3084b846852023-11-20T06:29:02ZengMDPI AGPharmaceutics1999-49232020-07-0112765510.3390/pharmaceutics12070655Microwave-Induced In Situ Amorphization: A New Strategy for Tackling the Stability Issue of Amorphous Solid DispersionsWei Qiang0Korbinian Löbmann1Colin P. McCoy2Gavin P. Andrews3Min Zhao4School of Pharmacy, Queen’s University Belfast, Belfast BT9 7BL, UKDepartment of Pharmacy, University of Copenhagen, 2100 Copenhagen, DenmarkSchool of Pharmacy, Queen’s University Belfast, Belfast BT9 7BL, UKSchool of Pharmacy, Queen’s University Belfast, Belfast BT9 7BL, UKSchool of Pharmacy, Queen’s University Belfast, Belfast BT9 7BL, UKThe thermodynamically unstable nature of amorphous drugs has led to a persistent stability issue of amorphous solid dispersions (ASDs). Lately, microwave-induced in situ amorphization has been proposed as a promising solution to this problem, where the originally loaded crystalline drug is in situ amorphized within the final dosage form using a household microwave oven prior to oral administration. In addition to circumventing issues with physical stability, it can also simplify the problematic downstream processing of ASDs. In this review paper, we address the significance of exploring and developing this novel technology with an emphasis on systemically reviewing the currently available literature in this pharmaceutical arena and highlighting the underlying mechanisms involved in inducing in situ amorphization. Specifically, in order to achieve a high drug amorphicity, formulations should be composed of drugs with high solubility in polymers, as well as polymers with high hygroscopicity and good post-plasticized flexibility of chains. Furthermore, high microwave energy input is considered to be a desirable factor. Lastly, this review discusses challenges in the development of this technology including chemical stability, selection criteria for excipients and the dissolution performance of the microwave-induced ASDs.https://www.mdpi.com/1999-4923/12/7/655microwave irradiationamorphous solid dispersionspoorly soluble drugsin situ amorphizationphysical stability |
| spellingShingle | Wei Qiang Korbinian Löbmann Colin P. McCoy Gavin P. Andrews Min Zhao Microwave-Induced In Situ Amorphization: A New Strategy for Tackling the Stability Issue of Amorphous Solid Dispersions Pharmaceutics microwave irradiation amorphous solid dispersions poorly soluble drugs in situ amorphization physical stability |
| title | Microwave-Induced In Situ Amorphization: A New Strategy for Tackling the Stability Issue of Amorphous Solid Dispersions |
| title_full | Microwave-Induced In Situ Amorphization: A New Strategy for Tackling the Stability Issue of Amorphous Solid Dispersions |
| title_fullStr | Microwave-Induced In Situ Amorphization: A New Strategy for Tackling the Stability Issue of Amorphous Solid Dispersions |
| title_full_unstemmed | Microwave-Induced In Situ Amorphization: A New Strategy for Tackling the Stability Issue of Amorphous Solid Dispersions |
| title_short | Microwave-Induced In Situ Amorphization: A New Strategy for Tackling the Stability Issue of Amorphous Solid Dispersions |
| title_sort | microwave induced in situ amorphization a new strategy for tackling the stability issue of amorphous solid dispersions |
| topic | microwave irradiation amorphous solid dispersions poorly soluble drugs in situ amorphization physical stability |
| url | https://www.mdpi.com/1999-4923/12/7/655 |
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