グレープフルーツ由来ナノ粒子をTATペプチドで修飾した経皮薬物送達の潜在的強化

背景:

• Plant-derived nanoparticles (PdNPs) show promise for nucleic acid delivery, particularly for transdermal applications.; Enhancing the skin penetration of PdNPs is crucial for effective transdermal delivery.; Cell penetration peptides (CPPs), such as the Tat-peptide, can facilitate cellular uptake and skin penetration.

研究 の 目的:

• To evaluate the feasibility of enhancing skin penetration of grapefruit-derived nanoparticles (GNPs) using surface modification with stearylated Tat-peptide (STR-Tat).; To assess the impact of STR-Tat modification on GNP properties, cellular uptake, and skin penetration.; To determine the potential of STR-Tat modified GNPs for transdermal nucleic acid delivery.

主な方法:

• GNP surface modification with synthesized STR-Tat via simple mixing.; Measurement of particle size and zeta potential of modified GNPs (STR-Tat-GNPs).; In vivo skin penetration studies on mouse models, alongside in vitro cellular uptake and toxicity assays.

主要な成果:

• STR-Tat-GNPs exhibited a positive zeta potential, contrasting with the negative zeta potential of unmodified GNPs.; Enhanced cellular uptake was observed for STR-Tat-GNPs with minimal cytotoxicity.; In vivo studies showed significant penetration of DiI-labeled STR-Tat-GNPs into hair follicles and deeper dermal layers.

結論:

• Simple STR-Tat surface modification effectively enhances the skin penetration of GNPs.; This approach improves the delivery of lipophilic substances via GNPs without inducing significant cellular toxicity.; STR-Tat modified GNPs represent a promising strategy for developing plant-derived nanoparticles with high skin penetration ability for nucleic acid delivery.