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维生素A固体脂质纳米粒外用凝胶:作为一种皮肤给药系统的美好前景。

Topical Gel of Vitamin A Solid Lipid Nanoparticles: A Hopeful Promise as a Dermal Delivery System.

作者信息

Boskabadi Mahshid, Saeedi Majid, Akbari Jafar, Morteza-Semnani Katayoun, Hashemi Seyyed Mohammad Hassan, Babaei Amirhossein

机构信息

Student Research Committee, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.

Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.

出版信息

Adv Pharm Bull. 2021 Sep;11(4):663-674. doi: 10.34172/apb.2021.075. Epub 2020 Oct 3.

Abstract

The Objective of the present investigation was to enhance the skin delivery of vitamin A (Vit A) via producing solid lipid nanoparticles (SLNs) through ultrasonication technique. For achieving optimal skin delivery, impacts of two surfactants ratio of Tween80:Span80 on nanoparticles (NPs) features and the respective functions were examined. Powder X-ray diffractometer (PXRD), photon correlation spectroscopy, attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), transmission electron microscopy (TEM), and differential scanning calorimetry (DSC) were applied for characterizing the solid state of Vit A in the SLN. Results showed that size of the NPs is usually enhanced by adding co-emulsifier (Span80). Notably, minimum NPs size (64.85±4.259 nm) was achieved while the hydrophilic-lipophilic balance (HLB) of the binary surfactants was 12.08, close to HLB of beeswax (HLB=12) as lipid matrix. Also, maximum entrapment efficiency (66.01±8.670%) was observed in the formulation. DSC thermogram indicated an amorphous form of Vit A in SLN. ATR-FTIR spectra of Vit A-SLN illustrated that prominent functional groups are found in the formulations that might be a sign of acceptable entrapment of Vit A in a lipid matrix. Moreover, ATR-FTIR studies showed no chemical interactions between Vit A and excipients. Skin irritation test proved the non-irritancy of Vit A-SLN2, when applied to the dorsal region of Wistar rats. Finally, any cellular toxicity was not seen for NPs. It was found that the procured Vit A-SLNs could be utilized as potent carriers for the dermal delivery of Vit A.

摘要

本研究的目的是通过超声技术制备固体脂质纳米粒(SLNs)来提高维生素A(Vit A)的皮肤递送能力。为了实现最佳的皮肤递送效果,研究了吐温80:司盘80两种表面活性剂比例对纳米粒(NPs)特性及其各自功能的影响。采用粉末X射线衍射仪(PXRD)、光子相关光谱、衰减全反射傅里叶变换红外光谱(ATR-FTIR)、透射电子显微镜(TEM)和差示扫描量热法(DSC)对SLN中Vit A的固态进行表征。结果表明,添加助乳化剂(司盘80)通常会使NPs的尺寸增大。值得注意的是,当二元表面活性剂的亲水亲油平衡(HLB)为12.08时,NPs尺寸最小(64.85±4.259 nm),接近作为脂质基质的蜂蜡的HLB(HLB = 12)。此外,该制剂的包封率最高(66.01±8.670%)。DSC热谱图表明SLN中Vit A为无定形形式。Vit A-SLN的ATR-FTIR光谱表明,制剂中存在显著的官能团,这可能是Vit A在脂质基质中包封良好的迹象。此外,ATR-FTIR研究表明Vit A与辅料之间没有化学相互作用。皮肤刺激性试验证明,将Vit A-SLN2应用于Wistar大鼠背部时无刺激性。最后,未观察到NPs有任何细胞毒性。研究发现,所制备的Vit A-SLNs可作为Vit A皮肤递送的有效载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f93a/8642790/0d916b39fc31/apb-11-663-g001.jpg

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