Huang Yanping, Yu Qin, Chen Zhongjian, Wu Wei, Zhu Quangang, Lu Yi
Shanghai Skin Disease Hospital, Tongji University School of Medicine, Shanghai 200443, China.
Key Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, China.
Acta Pharm Sin B. 2021 Aug;11(8):2469-2487. doi: 10.1016/j.apsb.2021.03.025. Epub 2021 Mar 21.
Lipid-based formulations (LBFs) have demonstrated a great potential in enhancing the oral absorption of poorly water-soluble drugs. However, construction of and correlations (IVIVCs) for LBFs is quite challenging, owing to a complex processing of these formulations. In this paper, we start with a brief introduction on the gastrointestinal digestion of lipid/LBFs and its relation to enhanced oral drug absorption; based on the concept of IVIVCs, the current status of models to establish IVIVCs for LBFs is reviewed, while future perspectives in this field are discussed. tests, which facilitate the understanding and prediction of the performance of solid dosage forms, frequently fail to mimic the processing of LBFs, leading to inconsistent results. digestion models, which more closely simulate gastrointestinal physiology, are a more promising option. Despite some successes in IVIVC modeling, the accuracy and consistency of these models are yet to be validated, particularly for human data. A reliable IVIVC model can not only reduce the risk, time, and cost of formulation development but can also contribute to the formulation design and optimization, thus promoting the clinical translation of LBFs.
基于脂质的制剂(LBFs)在提高难溶性药物的口服吸收方面已显示出巨大潜力。然而,由于这些制剂的加工过程复杂,构建LBFs的体内-体外相关性(IVIVCs)颇具挑战性。在本文中,我们首先简要介绍脂质/LBFs的胃肠道消化及其与增强口服药物吸收的关系;基于IVIVCs的概念,综述了建立LBFs的IVIVCs的模型现状,同时讨论了该领域的未来前景。有助于理解和预测固体剂型性能的体外试验,常常无法模拟LBFs的体内加工过程,导致结果不一致。更能紧密模拟胃肠道生理学的体外消化模型是更有前景的选择。尽管在IVIVC建模方面取得了一些成功,但这些模型的准确性和一致性仍有待验证,尤其是针对人体数据。一个可靠的IVIVC模型不仅可以降低制剂开发的风险、时间和成本,还可以有助于制剂的设计和优化,从而促进LBFs的临床转化。