High-Throughput Microfluidic Production of Ultrasmall Lecithin Nanoliposomes for High-Efficacy Transdermal Delivery and Skin-Aging Treatment

利用高通量微流控技术制备超小型卵磷脂纳米脂质体,用于高效透皮给药和皮肤老化治疗

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Abstract

BACKGROUND: Liposome particles with smaller sizes could increase transdermal drug delivery efficacy for enhanced skin penetration. While microfluidic methods have enabled controlled liposome synthesis, achieving efficient production of ultrasmall nanoliposomes (NLP(US)) with a size smaller than 40 nm yet remains an unmet challenge. METHODS: In this study, we employed a helical-blade-strengthened co-flow focusing (HBSCF) device to efficiently synthesize NLP(US), which demonstrated superior skin permeation and retention. RESULTS: Liposome formulation primarily contains unsaturated lecithin, which endows an unprecedented capacity to NLP(US) to scavenge reactive oxygen species (ROS). Moreover, NLP(US) can effectively encapsulate a broad spectrum of anti-aging agents, including coenzyme Q10 (CoQ10), while preserving its physical properties. In a photoaged skin model, topical application of CoQ10-loaded NLP(US) (CoQ10@NLP(US)) inhibited ultraviolet B (UVB)-induced matrix metalloproteinase-1 (MMP-1) production, and promoted collagen type I (Col-I) synthesis in skin cells, thereby effectively rejuvenating the photoaged skin. CONCLUSIONS: This study presents a straightforward and efficient method for the production of NLP(US), thereby offering a promising platform for transdermal delivery of diverse therapeutic agents.

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