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Abstract
Among the different techniques proposed for preparing cyclodextrin inclusion complex in the solid state, mechanochemical activation by grinding appears as a fast, highly efficient, convenient, versatile, sustainable, and eco-friendly solvent-free method. This review is intended to give a systematic overview of the currently available data in this field, highlighting both the advantages as well as the shortcomings of such an approach. The possible mechanisms involved in the inclusion complex formation in the solid state, by grinding, have been illustrated. For each type of applied milling device, the respective process variables have been examined and discussed, together with the characteristics of the obtained products, also in relation with the physicochemical characteristics of both the drug and cyclodextrin subjected to grinding. The critical process parameters were evidenced in order to provide a useful guide for a rational selection of the most suitable conditions for an efficient inclusion complex preparation by grinding, with the final purpose of promoting a wider use of this effective solvent-free cyclodextrin inclusion complex preparation method in the solid state.
Highlights
Cyclodextrins (CDs) are well recognized multifunctional excipients able to increase solubility, dissolution rate, chemical stability, and bioavailability of different drugs through the inclusion complex formation [1,2]
The aim of this review is to provide a systematic overview of the most commonly used grinding devices and conditions applied, in order to provide a useful guideline for a rational selection of the most suitable conditions for an efficient inclusion complex preparation by grinding
Co-grinding with crystalline CD derivatives leads to only partial drug complexation [32,77] or requires longer grinding time until complete product amorphization [31], which is generally accepted as an indication of inclusion complex formation in the solid state
Summary
Cyclodextrins (CDs) are well recognized multifunctional excipients able to increase solubility, dissolution rate, chemical stability, and bioavailability of different drugs through the inclusion complex formation [1,2]. In the case of Bs -type complexes, mainly occurring with natural CDs, the product is isolated by crystallization [14], whereas in the case of A-type complexes, the solvent is removed by an adequate drying technique, such as coevaporation under reduced pressure (COE) [22,23], spray-drying (SPD) [24,25], or freeze-drying (FD) [26,27] The drawbacks of such methods are in high consumption of time, energy and organic solvents (such as ethanol and methanol) whose complete removal from the final solid product could be quite costly and challenging, due to the ability of such solvents for the inclusion complex formation [28], that could lead to toxic effects. On the other hand, offers the advantages to be a simple, fast and highly effective method for the preparation of drug/CD inclusion complexes in the solid state, generally not requiring the use of organic solvents [39] This provides additional advantages, avoiding problems and limitations of solution-based techniques, such as solubility issues, solvent complexation, or solvolysis. Grinding represents an economically and environmentally desirable technology and it will be the focus of this review
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