Nowadays, many drugs are available on the market which is not easily soluble in water that becomes a hurdle to achieve requisite bioavailability of the drug in the blood plasma. The poorly water-soluble drugs cannot become a part of our body, so they may be excreted or remain in the body, thus causing side effects. In order to improve their bioavailability in blood plasma, their solubility must be enhanced. There are various methods to improve the soluble of poorly water-soluble drugs. Gemini surfactants are a group of novel amphiphiles with more than one hydrophilic head group and hydrophobic tail group linked by a spacer at or near the head groups were explored for encapsulation of poorly water-soluble drugs. The Gemini surfactants have more tendencies to aggregate, which means have more tendencies to encapsulate drugs molecules as compared to conventional surfactants. Moreover, Gemini surfactants have low Critical Micellization Concentration (CMC) values, thus aggregate easily and form a micellar system at extremely low concentrations. The carbohydrate-derived Gemini surfactants are a special type of surfactants that have no toxic effect and are easily biodegradable in nature. It was found that these Gemini surfactants enhance the solubility of poorly water-soluble drugs many folds. The review highlights the current research activities on the biomedical application of gemini surfactants.