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叶酸插层的镁/铝层状双氢氧化物——一种用于局部应用的多功能纳米杂化递送系统。

Folic Acid-Intercalated Mg/Al Layered Double Hydroxides-A Multifunctional Nanohybrid Delivery System for Topical Applications.

作者信息

Kleyi Phumelele, Mandiwana Vusani, de Beer Marinda, Kesavan Pillai Sreejarani, Ray Suprakas Sinha

机构信息

Centre for Nanostructured and Advanced Materials, DSI-CSIR Nanotechnology Innovation Centre, Council for Scientific and Industrial Research, Pretoria 0001, South Africa.

Department of Chemical Sciences, University of Johannesburg, Doornfontein, Johannesburg 2028, South Africa.

出版信息

ACS Omega. 2024 Nov 26;9(49):48185-48195. doi: 10.1021/acsomega.4c05374. eCollection 2024 Dec 10.

Abstract

The delivery of active functional molecules across the skin is laborious due to its structural intricacy and exceptional barrier characteristics. Developments in nanotechnology yielded innovative transport vehicles derived from nanomaterials to reinforce the skin's ability to interact with active ingredient molecules and increase its bioavailability. The current study employed crystalline inorganic two-dimensional double hydroxides (LDHs) as an efficient carrier and delivery vehicle for folic acid (FA) in a topical skincare formulation. FA was incorporated into the interlayer region of Mg/Al LDHs utilizing a coprecipitation procedure to produce a nanohybrid. The nanohybrid was characterized by XRD and FTIR. FA intercalation into the interlayer galleries of the nanohybrid was confirmed by an XRD diffractogram, which established a shift of the basal reflection of LDHs to lower 2θ angles. FTIR of the nanohybrids revealed the characteristic absorption frequencies of FA, indicating the existence of FA within the LDH matrix. The FA-intercalated nanohybrid showed antioxidant activity similar to that of free FA. A topical formulation was prepared by dispersing FA-intercalated LDH nanohybrid in an oil-in-water (o/w) emulsion, and it was used to evaluate its properties further. Rheological property evaluation showed that the presence of the nanohybrid resulted in better flow behavior and higher yield stress of the formulation, implying improved stability and quality. The nanohybrid also enhanced the storage modulus and, thus, the dynamic rigidity of the formulation. The test compounds expressed no cytotoxicity in HaCaT cells, as cell viability significantly increased in monolayer cultures after a 24-h incubation period. Release studies conducted using the nanohybrid showed a pH-dependent controlled release of FA. Transdermal permeation experiments using Franz diffusion cells demonstrated a direct correlation between the concentration of penetrated FA with time, which signified a gradual and effective transfer of FA from the LDH matrix into the oil/water emulsion, demonstrating its efficacy. Thus, the study revealed excellent prospects for the nanohybrid as a multifunctional active ingredient in topical applications.

摘要

由于皮肤结构复杂且具有特殊的屏障特性,将活性功能分子透过皮肤进行递送十分困难。纳米技术的发展产生了源自纳米材料的创新型转运载体,以增强皮肤与活性成分分子相互作用的能力并提高其生物利用度。当前的研究采用结晶无机二维双氢氧化物(LDHs)作为局部护肤配方中叶酸(FA)的有效载体和递送媒介。利用共沉淀法将FA掺入Mg/Al LDHs的层间区域以制备纳米杂化物。通过XRD和FTIR对该纳米杂化物进行了表征。XRD衍射图证实了FA插入到纳米杂化物的层间通道中,这使得LDHs的基面反射向较低的2θ角发生了偏移。纳米杂化物的FTIR显示了FA的特征吸收频率,表明LDH基质中存在FA。FA插层的纳米杂化物表现出与游离FA相似的抗氧化活性。通过将FA插层的LDH纳米杂化物分散在水包油(o/w)乳液中来制备局部配方,并用于进一步评估其性能。流变学性能评估表明,纳米杂化物的存在使配方具有更好的流动行为和更高的屈服应力,这意味着稳定性和质量得到了改善。纳米杂化物还提高了储能模量,从而提高了配方的动态刚性水平。测试化合物在HaCaT细胞中未表现出细胞毒性,因为在24小时孵育期后单层培养中的细胞活力显著增加。使用纳米杂化物进行的释放研究表明FA具有pH依赖性控释特性。使用Franz扩散池进行的透皮渗透实验表明,渗透的FA浓度与时间呈直接相关性,这表明FA从LDH基质逐渐有效地转移到油/水乳液中,证明了其有效性。因此,该研究揭示了纳米杂化物作为局部应用中的多功能活性成分具有极好的前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d10/11635470/9e374226477d/ao4c05374_0001.jpg

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