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. 2014 Mar 26;9:1617–1626. doi: 10.2147/IJN.S53886

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© 2014 Shi et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License

The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.

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Rapa encapsulated by FKBP-decorated nanoparticles has both anticancer and immunosuppressive efficacy.

Notes: (A) ELP nanoparticles fused genetically to the cognate receptor of Rapamycin-FKBP can specifically carry the drug with high avidity. (B) FSI significantly prolongs drug release compared with plain ELP (SI). (C) FSI-Rapa has lower cytotoxicity and greater antitumor efficacy than free Rapa in an MDA-MB-468 breast tumor xenograft mouse model. Compared with free Rapa group, which showed severe cytotoxicity (15% bodyweight loss by day 23), no obvious systemic cytotoxicity was observed in the FSI-Rapa group. (A), (B), (C) Reproduced from J Control Release,171(3), Shi P, Aluri S, Lin YA, et al. Elastin-based protein polymer nanoparticles carrying drug at both corona and core suppress tumor growth in vivo, 330–338,⁴² Copyright 2013, with permission from Elsevier. (D) FSI-Rapa suppresses transcription and expression of the protease cathepsin-S (CATS), a biomarker of lacrimal gland autoimmune dacryoadenitis, better than free Rapa in a mouse model of Sjögren’s syndrome. Reproduced from J Control Release, 171(3), Shah M, Edman MC, Janga SR, et al, A rapamycin-binding protein polymer nanoparticle shows potent therapeutic activity in suppressing autoimmune dacryoadenitis in a mouse model of Sjogren’s syndrome, 269–279,⁴³ Copyright 2013 with permission from Elsevier. (E) The blood half-lives of four ELPs estimated by pharmacokinetic modeling in mice based on micro-PET imaging. ***indicates a P-value of <0.001; **indicates a P-value of <0.01 by one-way ANOVA with Tukey’s multiple comparison test. From Janib SM, Liu S, Park R, et al. Kinetic quantification of protein polymer nanoparticles using non-invasive imaging. Integr Biol (Camb). 2013;5(1):183–194.²³ Reproduced by permission of The Royal Society of Chemistry.

Abbreviations: CMT, critical micelle temperature; ELP, elastin-like polypeptide; FKBP, FK506-binding protein; FSI, FKBP-ELP; PBS, phosphate buffered saline; PET, positron emission tomography; Rapa, rapamycin; SI, ELP S48I48.