Intranasal and intravenous administration of octa-arginine modified poly(lactic-co-glycolic acid) nanoparticles facilitates central nervous system delivery of loperamide

Abstract

This study demonstrates the potential of R8-PLGA NPs as carriers of therapeutic agents to the CNS.

Novel functionalization strategies of polymeric nanoparticles as carriers for brain medications

“…The present results on the penetration of functionalized NPs in the cortical parenchyma are supported by previous reports on the presence of apoE‐functionalized albumin NPs (250 nm in size) in cortical neurons 30 min after iv injection in mice and rats . Uptake of PLGA NPs functionalized with peptides (glycopeptide, leptin‐derived peptide, and phage‐displayed peptide), but not non‐functionalized ones, by cortical neurons was also shown in rats at 2 h after systemic injection …”

“…Concerning the size of the custom‐made, non‐functionalized PLGA NPs, previous studies indicated that NPs in a similar dimensional range can provide tools for drug delivery to the brain . However, NP size is a critical parameter for BBB traversal, and in the present study non‐functionalized PLGA NPs were not found to enter the brain parenchyma.…”

“…The brain penetration of fluorescent tagged PLGA NPs engineered with two different moieties (pep‐apoE or l ‐PGDS) was here investigated in vivo with different techniques. Other functionalization ligands have been previously tested in in vitro models of BBB to assess the passage across the endhotelial cells, or in vivo for brain targeting of PLGA NPs. A sequence derived from leptin or a similar opioid glycopeptide (NPs around 200 nm in size) have been used to functionalize fluorescent PLGA NPs and functional (anorectic and nociceptive) effects were assessed in rats up to 2 h after iv injection.…”

Mixed cationic liposomes for brain delivery of drugs by the intranasal route: The acetylcholinesterase reactivator 2-PAM as encapsulated drug model

“…The main strategy to improve drug delivery to the brain by intranasal administration is the modification of nanoparticles by absorption and permeation enhancers. For that purpose, surfactants, bile salts, cyclodextrins, derivatives of chitosan, arginine, lactoferrin, have already been proposed [11][12][13][14][15][16]. Liposomes are well-known universal nano-carriers.…”

Polysorbate 80-coated PLGA nanoparticles improve the permeability of acetylpuerarin and enhance its brain-protective effects in rats

“…Therefore, PLGA is approved by the US Food and Drug Administration and the European Medicine Agency in various drug delivery systems, including polymeric NPs in human [19]. Furthermore, studies[20,21] have shown the potential of PLGA‐NPs as carriers of therapeutic agents to the brain.…”