Drug delivery challenges and formulation aspects of proteolysis targeting chimera (PROTACs)

被引：38

作者：

Saraswat, Aishwarya L. ^{[1
]}

Vartak, Richa ^{[1
]}

Hegazy, Rehab ^{[1
,2
]}

Patel, Akanksha ^{[1
]}

Patel, Ketan ^{[1
]}

机构：

[1] St Johns Univ, Coll Pharm & Hlth Sci, Queens, NY 11439 USA

[2] Natl Res Ctr, Pharmacol Dept, Med Div, Giza, Egypt

来源：

DRUG DISCOVERY TODAY | 2023年 / 28卷 / 01期

基金：

美国国家卫生研究院;

关键词：

PROTAC; Nanoformulation; Protein degradation; Targeted therapy; Solubility enhancement; Drug permeation; PROTEIN-DEGRADATION; ABSORPTION; UBIQUITINATION; MOLECULES; CANCER;

D O I：

10.1016/j.drudis.2022.103387

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Proteolysis targeting chimeras (PROTACs) have been extensively explored for targeted proteasomal degradation of disease-related proteins with enormous potential in the treatment of intractable diseases. However, PROTACs are poorly soluble and permeable bulky molecules facing several bioavailability challenges irrespective of the route of administration. Our review lays out crucial challenges in the delivery of target protein degraders and nanoformulation approaches to overcome physicochemical and biological hurdles that can aid in transporting these target-protein degraders to the disease site. We have elaborated on the current formulation approaches and further highlighted the prospective delivery strategies that could be probed for disease-specific targeted delivery of PROTACs.

引用

页码：1 / 9

页数：9

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