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富含吐温80和甘油的提取物负载透明质体的制剂及其体外功效评估

Formulation and In Vitro Efficacy Assessment of Extract Loading Hyalurosomes Enriched with Tween 80 and Glycerol.

作者信息

Firoznezhad Mohammad, Castangia Ines, Tuberoso Carlo Ignazio Giovanni, Cottiglia Filippo, Marongiu Francesca, Porceddu Marco, Usach Iris, Escribano-Ferrer Elvira, Manca Maria Letizia, Manconi Maria

机构信息

Department of Pharmacy, University of Salerno, 84084 Fisciano, Italy.

Department of Scienze della Vita e dell'Ambiente, University of Cagliari, 09124 Cagliari, Italy.

出版信息

Nanomaterials (Basel). 2022 Mar 26;12(7):1096. doi: 10.3390/nano12071096.

Abstract

The extract of L. (Lamiaceae) was obtained using the aerial parts of the plant, by means of a maceration process. Verbascoside, caffeic acids derivatives and flavonols were the main components contained in the extract as detected using high-performance liquid chromatography coupled with diode array detector (HPLC-DAD) as an analytical method. The extract was successfully incorporated into hyalurosomes, which were further enriched by adding a water cosolvent (glycerol) and a surfactant (Tween 80), thus obtaining glycerohyalurosomes. Liposomes, transfersomes and glycerosomes were prepared as well and used as comparisons. All vesicles were small, as the mean diameter was never higher than 115 nm, thus ideal for topical application and stable on storage, probably thanks to the highly negative surface charge of the vesicles (-33 mV). The cryo-TEM images confirmed the formation of close-packed, oligolamellar and multicompartment hyalurosomes and glycerohyalurosomes in which around 95% of the used extract was retained, confirming their ability to simultaneously load a wide range of molecules having different chemical natures. Moreover, the extract, when loaded in hyalurosomes and glycerohyalurosomes was able to counteract the damages induced in the fibroblasts by hydrogen peroxide to a better extent (viability110%) than that loaded in the other vesicles (viability100%), and effectively promoted their proliferation and migration ensuring the healing of the wound performed in a cell monolayer (scratch assay) during 48 h of experiment. Overall in vitro results confirmed the potential of glycerohyalurosomes as delivery systems for extract for the treatment of skin lesions connected with oxidative stress.

摘要

通过浸渍法,利用唇形科植物的地上部分获得该植物提取物。采用高效液相色谱-二极管阵列检测器(HPLC-DAD)作为分析方法检测发现,提取物中的主要成分是毛蕊花糖苷、咖啡酸衍生物和黄酮醇。提取物成功地被包封进透明质体中,通过添加水助溶剂(甘油)和表面活性剂(吐温80)进一步富集,从而得到甘油透明质体。同时制备了脂质体、传递体和甘油体作为对照。所有囊泡都很小,平均直径从未超过约115nm,因此非常适合局部应用且储存稳定,这可能得益于囊泡的高负表面电荷(约-33mV)。冷冻透射电子显微镜图像证实形成了紧密堆积、寡层和多室的透明质体和甘油透明质体,其中约95%的所用提取物被保留,证实了它们同时负载多种具有不同化学性质分子的能力。此外,当提取物负载在透明质体和甘油透明质体中时,与负载在其他囊泡中的提取物相比,能更好地抵消过氧化氢对成纤维细胞造成的损伤(存活率约110%),而负载在其他囊泡中的提取物存活率约为100%,并且在48小时的实验过程中,能有效促进成纤维细胞的增殖和迁移,确保细胞单层(划痕试验)中伤口的愈合。总体体外实验结果证实了甘油透明质体作为该植物提取物递送系统用于治疗与氧化应激相关皮肤损伤的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59ac/9000414/bcfa2d354698/nanomaterials-12-01096-g001.jpg

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