Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, China.
Department of Pharmaceutics, School of Pharmacy, Jilin University, Changchun, China.
Expert Opin Drug Deliv. 2021 Sep;18(9):1211-1228. doi: 10.1080/17425247.2021.1903428. Epub 2021 Mar 29.
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.
Promising size, shape, and surface modification of nanocrystals have gained interests for application in oral BCS IV drugs.
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.
BCS 四类药物的口服吸收几乎不能通过改善溶解来获益。因此，更倾向于采用 BCS 四类药物纳米晶体的“整体”吸收策略，并需要对纳米晶体进行结构修饰。表面修饰有助于纳米晶体在需要药物溶解之前保持颗粒结构，从而增强 BCS 四类药物的口服吸收，促进治疗效果。本文讨论了口服 BCS 四类药物纳米晶体传递的主要挑战和解决方案。此外，还突出了促进 BCS 四类药物口服生物利用度的纳米晶体表面修饰策略，并为口服药物传递的创新提供了思路。
有前途的纳米晶体的大小、形状和表面修饰引起了人们对应用于口服 BCS 四类药物的兴趣。
纳米晶体表面修饰是维持纳米晶体结构完整性的一种可行方法，引入的材料也可以进行修饰，以集成其他功能，进一步促进纳米晶体的吸收。预计纳米晶体的“整体”吸收策略将为口服 BCS 四类药物提供不同的选择。
