Abstract
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.
Highlights
Oral administration is the most commonly used route of administration, offering various advantages including convenience of administration, compliance of medication, safety and economy
This review only provides a very brief introduction to Amorphous solid dispersions (ASDs), which leads to the main focus of the review, i.e., microwave induced in situ amorphization, as an upcoming approach to solving the physical stability concerns of ASDs
The aim of this review is to provide a systemic overview of the state-of-the-art of microwave-induced in situ amorphization as a novel ASD preparation strategy as well as highlighting current challenges of this technology
Summary
Oral administration is the most commonly used route of administration, offering various advantages including convenience of administration, compliance of medication, safety and economy. This review only provides a very brief introduction to ASDs, which leads to the main focus of the review, i.e., microwave induced in situ amorphization, as an upcoming approach to solving the physical stability concerns of ASDs. As predicted by Hancock et al, amorphous APIs exhibited 10 to 1600 times higher solubility than their most stable crystalline counterparts due to their higher Gibbs free energy [12]. In 2017, microwave-induced in situ amorphization was firstly proposed by Doreth et al as a promising approach to tackling these problems [22] This technique can be utilized to circumvent the physical stability issue and simplify the problematic downstream processing of ASDs by preparing a final dosage form containing the crystalline drug and subsequently “activating”, i.e., amorphizing, the drug on demand within its final dosage form prior to administration using household microwave ovens under an optimized and well defined operation setting, including microwave power and time. The aim of this review is to provide a systemic overview of the state-of-the-art of microwave-induced in situ amorphization as a novel ASD preparation strategy as well as highlighting current challenges of this technology
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