It is a great challenge to develop new and innovative medicines for the treatment of a variety of diseases, which are effective and safe to administer. The use of combinatorial chemistry and molecular modelling in the development of new drugs has resulted in molecules with pronounced lipophilicity and high molecular weight, and consequently poor solubility in water. The poor solubility of new drug entities has been recognized as one of the most important factors that lead to rejections of such new structures, as they show low bioavailability and suboptimal therapeutic effect. Cyclodextrins are cyclic oligosaccharides used in pharmaceutical technology as multifunctional excipients able to mask the unpleasant taste and odor of a drug and to improve their solubility and consequently bioavailability. Cyclodextrin-based drug formulations currently available on the market are intended for various routes of administration, including parenteral administration. Parenteral administration provides certain advantages over other routes of administration, so the development and clinical trials of parenteral formulations containing cyclodextrins are in the pipeline of numerous pharmaceutical companies. The favorable efficiency and the safety of currently available formulations may lead to a significant increase in the number of such formulations in daily clinical practice in the near future. This paper outlines the advantages and disadvantages of cyclodextrin used in the development of parenteral preparations. To this end, the results of clinical studies of formulations that have recently been registered or are in advanced stages of clinical trials have been considered. Looking at superior therapeutic outcomes, including the faster onset of action accompanied by reduced number and intensity of side effects, a significant increase in the number of parenteral formulations in clinical practice can be expected in the near future.