Multifunctional peptide carrier-modified polymer micelle accelerates oral siRNA-delivery to the colon and improves gene silencing-mediated therapeutic effects in ulcerative colitis

Ibaraki, Hisako; Hatakeyama, Naruhiro; Arima, Naoki; Kanazawa, Takanori

doi:10.1016/j.jddst.2022.103481

Cited by 8 publications

(1 citation statement)

References 40 publications

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“…They found improved delivery of MPEG-PCL-CH2R4H2C/siRNA to mice colon compared to naked siRNA. siRNA loaded with micelle had better cell internalization, did not degrade the harsh pH, and was not toxic to the healthy cell [ 105 ]. Micelles have a great potential to be used as carriers for oral delivery in other GI cancer or any other cancers.…”

Section: Carriers For Oral Delivery Of Sirnamentioning

confidence: 99%

Oral delivery of RNAi for cancer therapy

Afrin

Bai

Kumar

et al. 2023

Cancer Metastasis Rev

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Cancer is a major health concern worldwide and is still in a continuous surge of seeking for effective treatments. Since the discovery of RNAi and their mechanism of action, it has shown promises in targeted therapy for various diseases including cancer. The ability of RNAi to selectively silence the carcinogenic gene makes them ideal as cancer therapeutics. Oral delivery is the ideal route of administration of drug administration because of its patients’ compliance and convenience. However, orally administered RNAi, for instance, siRNA, must cross various extracellular and intracellular biological barriers before it reaches the site of action. It is very challenging and important to keep the siRNA stable until they reach to the targeted site. Harsh pH, thick mucus layer, and nuclease enzyme prevent siRNA to diffuse through the intestinal wall and thereby induce a therapeutic effect. After entering the cell, siRNA is subjected to lysosomal degradation. Over the years, various approaches have been taken into consideration to overcome these challenges for oral RNAi delivery. Therefore, understanding the challenges and recent development is crucial to offer a novel and advanced approach for oral RNAi delivery. Herein, we have summarized the delivery strategies for oral delivery RNAi and recent advancement towards the preclinical stages.

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Section: Carriers For Oral Delivery Of Sirnamentioning

confidence: 99%