title: Using drug-excipient interactions for siRNA delivery.
abstract: SiRNA is the trigger of RNA interference, a mechanism discovered in the late 1990s. To release the therapeutic potential of this versatile but large and fragile molecule, excipients are used which either interact by electrostatic interaction, passively encapsulate siRNA or are covalently attached to enable specific and safe delivery of the drug substance. Controlling the delicate balance between protective complexation and release of siRNA at the right point and time is done by understanding excipients-siRNA interactions. These can be lipids, polymers such as PEI, PLGA, Chitosans, Cyclodextrins, as well as aptamers and peptides. This review describes the mechanisms of interaction of the most commonly used siRNA delivery vehicles, and looks at the results of their clinical and preclinical studies.
authors.affiliation: Novartis Pharma AG, Technical Research & Development (TRD), Pharmaceutical and Analytical Development (PHAD), CH-4057 Basel, Switzerland. katharina.bruno@novartis.com
authors.forename: Katharina
authors.initials: K
authors.lastname: Bruno
mesh_terms: D000818:Animals; D002986:Clinical Trials as Topic; D016503:Drug Delivery Systems; D004353:Drug Evaluation, Preclinical; D005079:Excipients / Q000737:chemistry*; D006801:Humans; D034622:RNA Interference; D034741:RNA, Small Interfering / Q000008:administration & dosage*; D055672:Static Electricity; D013997:Time Factors
chemical_list: D005079:Excipients; D034741:RNA, Small Interfering