Article (Scientific journals)
Innovative lipoplexes formulations with enhanced siRNA efficacy for cancer treatment: Where are we now?
Berger, Manon; Lechanteur, Anna; Evrard, Brigitte et al.
2021In International Journal of Pharmaceutics
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Keywords :
Cancer; Gene delivery; Lipid nanoparticle; pH-sensitive lipid; Cell-penetrating peptide
Abstract :
[en] Over the past two decades, RNA interference has become an extensively studied mechanism to silence gene and treat diseases including cancer. siRNA appears as a promising strategy that could avoid some side effects related to traditional chemotherapy. Considering the weak stability of naked siRNA in blood, vectors like cationic liposomes or Lipid Nanoparticles (LNPs) are widely used to carry and protect siRNA until it reaches the tumor targeted. Despite extensive research, only three RNAi drugs are currently approved by the Food and Drug Administration, including only one LNP formulation of siRNA to treat hereditary ATTR amyloidosis. This shows the difficulty of lipoplexes clinical translation, in particular in cancer therapy. To overcome the lipoplexes limitations, searches are made on innovative lipoplexes formulations with enhanced siRNA efficacy. The present review is focusing on the recent use of pH-sensitive lipids, peptides and cell-penetrating peptides or polymers. The incorporation of some of these components in the lipoplex formulation induces a fusogenic property or an enhanced endosomal escape, an enhanced cellular uptake, an enhanced tumor targeting, an improved stability in the blood stream …These innovations appear critical to obtain an efficient siRNA accumulation in tumor cells with effective antitumor effect considering the complex tumor environment.
Research center :
Center for Interdisciplinary Research on Medicines (CIRM)
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Berger, Manon  ;  Université de Liège - ULiège > Département de pharmacie > Développement de nanomédicaments
Lechanteur, Anna  ;  Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Evrard, Brigitte  ;  Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Piel, Géraldine ;  Université de Liège - ULiège > Département de pharmacie > Développement de nanomédicaments
Language :
English
Title :
Innovative lipoplexes formulations with enhanced siRNA efficacy for cancer treatment: Where are we now?
Publication date :
July 2021
Journal title :
International Journal of Pharmaceutics
ISSN :
0378-5173
eISSN :
1873-3476
Publisher :
Elsevier, Netherlands
Peer reviewed :
Peer Reviewed verified by ORBi
Funders :
ARC for Lipegalt project
Available on ORBi :
since 12 July 2021

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