The use of medicinal drugs represented a great evolution for humanity regarding disease combat. As a consequence, human life expectancy in the last century has increased considerably. However, there are still several issues to be addressed in this area, mostly related to the physicochemical properties of bioactive agents and their side effects. For instance, despite the high amount of money and time spent yearly by the pharmaceutical industry in drug research, several active pharmaceutical ingredients are launched in the market still presenting low aqueous solubility, low thermal stability, low tabletability, frequent incidence of annoying side effects, among others. Therefore, approaches that could contribute to overpass such issues are of great importance. Following these lines, this talk will present two approaches that might be helpful in this regard: encapsulation of drug molecules within the interlamellar space of clay minerals and the cocrystallization of active pharmaceutical ingredients with generally recognized as safe materials. Through some examples from recent studies, it will be shown that, in fact, cocrystallization and encapsulation in clay minerals stand as promising alternatives to enhance the effectiveness of active pharmaceutical ingredients end minimize their side effects.