Rapamycin is an anti-inflammatory and autophagy-inducing molecule, and has been reported to inhibit the progression of both kidney32 and lung33 fibrosis via increased expression of TGF-α and epidermal growth factor receptor (EGFR) signaling. Rapamycin also reduces collagen deposition in UUO-induced kidney fibrosis34 and bleomycin-induced lung fibrosis35. However, the therapeutic use of intravenously infused rapamycin is hindered by its low solubility in water and the difficulty of its delivery, resulting in unwanted systemic side effects31.
… we stably encapsulate the potential anti-fibrotic water-insoluble drug, rapamycin, in CBP-micelles. We show that these novel formulations of therapeutics bind to collagen in vitro and that their efficacy in mouse models of lung and kidney fibrosis is improved, compared to free, untargeted drugs. Our results demonstrate that collagen-targeted anti-fibrotic drugs may be next generation therapies of high clinical potential.
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