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Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Curr+Pharm+Des 2020 ; 26 (31): 3840-3846 Nephropedia Template TP
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Alpha-MSH Targeted Liposomal Nanoparticle for Imaging in Inflammatory Bowel Disease (IBD) #MMPMID32718282
Penate-Medina T; Damoah C; Benezra M; Will O; Kairemo K; Humbert J; Sebens S; Penate-Medina O
Curr Pharm Des 2020[]; 26 (31): 3840-3846 PMID32718282show ga
BACKGROUND: The purpose of our study was to find a novel targeted imaging and drug delivery vehicle for inflammatory bowel disease (IBD). IBD is a common and troublesome disease that still lacks effective therapy and imaging options. As an attempt to improve the disease treatment, we tested alphaMSH for the targeting of nanoliposomes to IBD sites. alphaMSH, an endogenous tridecapeptide, binds to the melanocortin-1 receptor (MC1-R) and has anti-inflammatory and immunomodulating effects. MC1-R is found on macrophages, neutrophils and the renal tubule system. We formulated and tested a liposomal nanoparticle involving alphaMSH in order to achieve a specific targeting to the inflamed intestines. METHODS: NDP-alphaMSH peptide conjugated to Alexa Fluor 680 was linked to the liposomal membrane via NSuccinyl PE and additionally loaded into the lumen of the liposomes. Liposomes without the alphaMSH-conjugate and free NDP-alphaMSH were used as a control. The liposomes were also loaded with ICG to track them. The liposomes were tested in DSS treated mice, which had received DSS via drinking water order to develop a model IBD. Inflammation severity was assessed by the Disease Activity Index (DAI) score and ex vivo histological CD68 staining of samples taken from different parts of the intestine. The liposome targeting was analyzed by analyzing the ICG and ALEXA 680 fluorescence in the intestine compared to the biodistribution. RESULTS: NPD-alphaMSH was successfully labeled with Alexa and retained its biological activity. Liposomes were identified in expected regions in the inflamed bowel regions and in the kidneys, where MC1-R is abundant. In vivo liposome targeting correlated with the macrophage concentration at the site of the inflammation supporting the active targeting of the liposomes through alphaMSH. The liposomal alphaMSH was well tolerated by animals. CONCLUSION: This study opens up the possibility to further develop an alphaMSH targeted theranostic delivery to different clinically relevant applications in IBD inflammation but also opens possibilities for use in other inflammations like lung inflammation in Covid 19.
Curr+Pharm+Des 2020 ; 26 (31): 3840-3846
