The characteristics and biological activity enhancements of melatonin encapsulations for skin care product applications

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Phongsapak Phanphothong , Nattawadee Kanpipit , Suthasinee Thapphasaraphong
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Abstract

Melatonin (MLT) exhibits antioxidant, ultraviolet protection, anti-inflammatory, and anti-aging properties. However, its effectiveness is limited by instability, a short half-life, and incompatible absorption. In this research, we encapsulated melatonin (MLT) in transfersomes (MT) and niosomes (MN) to enhance their properties and investigate their effects through in vitro cell assays using murine macrophages cells and human foreskin fibroblasts cells. The vesicle morphology, vesicle size, polydispersity index, zeta potential, entrapment efficiency (EE%), attenuated total reflectance-Fourier transform spectroscopy (ATR-FTIR) spectra, along with in vitro release, permeation profiles, and stability study were also evaluated. The results showed that both encapsulations displayed spherical morphology at the nanometric scale, their great physical stability and provided an EE% range of 58–78%. The MLT incorporation into the vesicle was confirmed by the ATR-FTIR spectra. Additionally, the encapsulation’ release profiles fitted with the Higuchi model, indicating controlled release of melatonin. Furthermore, MT showed greater permeability than MN and MS including melatonin deposition. In cell assays, MT exhibited significantly higher nitric oxide inhibition and stimulation of collagen compared to MN and MS. Therefore, MT demonstrated the highest possibility for anti-inflammatory and collagen-stimulating activities that could be applied in pharmaceutical or anti-aging cosmetic products.

Abstract Image

用于皮肤护理产品应用的褪黑激素包封物的特性和生物活性增强。
褪黑激素(MLT)具有抗氧化、紫外线防护、抗炎和抗衰老的特性。然而,它的有效性受到不稳定性、半衰期短和不相容吸收的限制。在这项研究中,我们将褪黑激素(MLT)封装在转移体(MT)和泌酸体(MN)中,以增强其特性,并通过使用小鼠巨噬细胞和人包皮成纤维细胞的体外细胞测定来研究其作用。还评估了囊泡形态、囊泡大小、多分散指数、ζ电位、包封率(EE%)、衰减全反射傅立叶变换光谱(ATR-FTIR)以及体外释放、渗透特性和稳定性研究。结果表明,两种封装在纳米尺度上都显示出球形形态,它们具有良好的物理稳定性,并且提供了58-78%的EE%范围。通过ATR-FTIR光谱证实了MLT掺入囊泡中。此外,胶囊的释放曲线符合Higuchi模型,表明褪黑素的释放受到控制。此外,MT表现出比MN和MS更大的渗透性,包括褪黑素沉积。在细胞测定中,与MN和MS相比,MT表现出显著更高的一氧化氮对胶原的抑制和刺激作用。因此,MT显示出抗炎和胶原刺激活性的最高可能性,可应用于药物或抗衰老化妆品。
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来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
期刊介绍: International Journal of Pharmaceutics: X offers authors with high-quality research who want to publish in a gold open access journal the opportunity to make their work immediately, permanently, and freely accessible. International Journal of Pharmaceutics: X authors will pay an article publishing charge (APC), have a choice of license options, and retain copyright. Please check the APC here. The journal is indexed in SCOPUS, PUBMED, PMC and DOAJ. The International Journal of Pharmaceutics is the second most cited journal in the "Pharmacy & Pharmacology" category out of 358 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.
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