LAUSR

ABSTRACT Introduction Oral absorption of BCS IV drug benefits little from improved dissolution. Therefore, the absorption of BCS IV drug nanocrystals ‘as a whole’ strategy is preferred, and structural modification of nanocrystals is required. Surface modification helps the nanocrystals maintain particle structure before drug dissolution is needed, thus enhancing the oral absorption of BCS IV drugs and promoting therapeutic effect. Here, the main challenges and solutions of oral BCS IV drug nanocrystals delivery are discussed. Moreover, strategies for nanocrystal surface modification that facilitates oral bioavailability of BCS IV drugs are highlighted, and provide insights for the innovation in oral drug delivery. Areas covered Promising size, shape, and surface modification of nanocrystals have gained interests for application in oral BCS IV drugs. Expert opinion Nanocrystal surface modification is a feasible method to maintain the structural integrity of nanocrystals, and the introduced materials can also be modified to integrate additional functions to further facilitate the absorption of nanocrystals. It is expected that the absorption ‘as a whole’ strategy of nanocrystals will provide different choices for the oral BCS IV drugs.