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用于皮肤年轻化的聚乙二醇化聚D,L-乳酸纳米颗粒的研制与表征

Development and Characterization of PEGylated Poly D,L-Lactic Acid Nanoparticles for Skin Rejuvenation.

作者信息

Lee Seunghwa, Moon Hyoung-Wook, Lee Seong-Jin, Cho Jin-Cheol

机构信息

R&D Center, CHA Meditech Co., Ltd., 119 Techno 2-ro (#206, Migun Techno World, Yongsan-Dong), Yuseong-gu, Daejeon 34116, Republic of Korea.

出版信息

Nanomaterials (Basel). 2025 Mar 20;15(6):470. doi: 10.3390/nano15060470.

Abstract

Recently, various biocompatible and biodegradable materials have garnered significant attention as cosmetic fillers for skin rejuvenation. Among these, poly ε-caprolactone (PCL), poly L-lactic acid (PLLA), poly D,L-lactic acid (PDLLA), and polydioxanone (PDO) microspheres have been developed and commercialized as a dermal filler. However, its irregularly hydrophobic microspheres pose hydration challenges, often causing syringe needle blockages and side effects such as delayed onset nodules and papules after the procedure. In this study, we synthesized a polyethylene glycol-poly D,L-lactic acid (mPEG-PDLLA) copolymer to address the limitations of conventional polymer fillers. Comprehensive characterization of the copolymer was performed using nuclear magnetic resonance spectroscopy, Fourier transform infrared spectroscopy, and differential scanning calorimetry. The mPEG-PDLLA copolymers demonstrated a unimodal size distribution of approximately 121 ± 20 nm in an aqueous solution. The in vitro cytotoxicity and collagen genesis of mPEG-PDLLA copolymers were evaluated using human dermal fibroblast cells. In this study, angiogenesis was observed over time in hairless mice injected with mPEG-PDLLA copolymers, confirming its potential role in enhancing collagen synthesis. To assess the inflammatory response, the expression levels of the genes MMP1 and IL-1β were analyzed. Additionally, gene expression levels such as transforming growth factor-β and collagen types I and III were compared with Rejuran in animal studies. The newly developed collagen-stimulating PEGylated PDLLA may be a safe and effective option for skin rejuvenation.

摘要

最近,各种生物相容性和可生物降解材料作为用于皮肤年轻化的美容填充剂受到了广泛关注。其中,聚ε-己内酯(PCL)、聚L-乳酸(PLLA)、聚D,L-乳酸(PDLLA)和聚二氧杂环己酮(PDO)微球已被开发并商业化作为真皮填充剂。然而,其不规则的疏水性微球带来了水合方面的挑战,常常导致注射器针头堵塞以及术后出现延迟性结节和丘疹等副作用。在本研究中,我们合成了聚乙二醇-聚D,L-乳酸(mPEG-PDLLA)共聚物以解决传统聚合物填充剂的局限性。使用核磁共振光谱、傅里叶变换红外光谱和差示扫描量热法对该共聚物进行了全面表征。mPEG-PDLLA共聚物在水溶液中显示出约121±20 nm的单峰尺寸分布。使用人真皮成纤维细胞评估了mPEG-PDLLA共聚物的体外细胞毒性和胶原蛋白生成。在本研究中,观察到在注射了mPEG-PDLLA共聚物的无毛小鼠中随时间出现血管生成,证实了其在增强胶原蛋白合成中的潜在作用。为了评估炎症反应,分析了MMP1和IL-1β基因的表达水平。此外,在动物研究中,将转化生长因子-β以及I型和III型胶原蛋白等基因表达水平与瑞蓝进行了比较。新开发的具有胶原蛋白刺激作用的聚乙二醇化PDLLA可能是皮肤年轻化的一种安全有效的选择。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0517/11944346/7632c2ceaae3/nanomaterials-15-00470-g001.jpg

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