A large amount of citrus waste is generated annually. This waste is of great economic worth, since it contains high levels of polyphenols, which have attracted scientific interest due to their potent antimicrobial and antiradical activities. Pretreatment is a crucial step that precedes the extraction process and influences the yields and quality of polyphenols. This review emphasizes the effect of different drying processes, such as freeze drying, hot-air drying, vacuum drying, microwave drying, infrared drying, and high-speed drying, on the polyphenol retention in citrus by-products. Further treatments of the dried citrus by-products for assisting the liberation of bound polyphenols are also provided and comprehensively discussed.