Quality by design endorsed atorvastatin-loaded nanostructured lipid carriers embedded in pH-responsive gel for melanoma.

IF 3 4区医学 Q2 CHEMISTRY, APPLIED

Journal of microencapsulation Pub Date : 2024-01-01 Epub Date: 2024-01-10 DOI:10.1080/02652048.2023.2282971

Deepkumar Bagasariya, Kondasingh Charankumar, Saurabh Shah, Paras Famta, Valencia Fernandes, Syed Shahrukh, Dharmendra Kumar Khatri, Shashi Bala Singh, Saurabh Srivastava

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引用次数: 0

Abstract

Aim: Our aim was to repurpose atorvastatin for melanoma by encapsulating in a nanostructured lipid carrier matrix to promote tumour cell internalisation and skin permeation. pH-responsive chitosan gel was employed to restrict At-NLCs in upper dermal layers.

Methods: We utilised a quality by design approach for encapsulating At within the NLC matrix. Further, cellular uptake and cytotoxicity was evaluated along with pH-responsive release and ex vivo skin permeation.

Results: Cytotoxicity assay showed 3.13-fold enhanced cytotoxicity on melanoma cells compared to plain drug with nuclear staining showing apoptotic markers. In vitro, release studies showed 5.9-fold rapid release in chitosan gel matrix at pH 5.5 compared to neutral pH.

Conclusions: At-NLCs prevented precipitation, promoted skin permeation, and SK-MEL 28 cell internalisation. The localisation of NLCs on the upper dermal layer due to electrostatic interactions of skin with chitosan gel diminished the incidence of untoward systemic effects.

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设计质量认可了在ph反应凝胶中嵌入阿托伐他汀纳米结构脂质载体用于黑色素瘤。

目的:我们的目的是通过包裹在纳米结构脂质载体基质中，促进肿瘤细胞内化和皮肤渗透，将阿托伐他汀重新用于黑色素瘤。采用ph反应性壳聚糖凝胶抑制上真皮层At-NLCs。方法:采用质量设计方法将At封装在NLC矩阵中。此外，细胞摄取和细胞毒性与ph响应释放和体外皮肤渗透一起评估。结果-细胞毒性试验显示，与核染色显示凋亡标记的普通药物相比，对黑色素瘤细胞的细胞毒性增强了3.13倍。体外释放研究表明，在pH为5.5时，壳聚糖凝胶基质的快速释放量是中性pH的5.9倍。结论:at - nlcs可阻止沉淀，促进皮肤渗透和SK-MEL 28细胞内化。由于皮肤与壳聚糖凝胶的静电相互作用，NLCs定位于真皮上层，减少了不良全身效应的发生。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of microencapsulation 工程技术-工程：化工

CiteScore

6.30

自引率

2.60%

发文量

审稿时长

3 months

期刊介绍： The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.