负载叶绿醇的固体脂质纳米粒作为一种新型抗念珠菌纳米生物技术方法

Phytol-Loaded Solid Lipid Nanoparticles as a Novel Anticandidal Nanobiotechnological Approach.

作者信息

Lima Tábata L C, Souza Luanda B F C, Tavares-Pessoa Lannya C S, Santos-Silva Alaine M Dos, Cavalcante Rômulo S, Araújo-Júnior Raimundo F de, Cornélio Alianda M, Fernandes-Pedrosa Matheus F, Chaves Guilherme Maranhão, Silva-Júnior Arnóbio Antônio da

机构信息

Laboratory of Pharmaceutical Technology and Biotechnology, Department of Pharmacy, Federal University of Rio Grande do Norte (UFRN), Gal. Gustavo Cordeiro de Farias, S/N, Petrópolis, Natal-RN 59072-570, Brazil.

Department of Clinical and Toxicological Analyses, Federal University of Rio Grande do Norte (UFRN), Gal, Gustavo Cordeiro de Faria, S/N, Petrópolis, Natal-RN 59084-100, Brazil.

出版信息

Pharmaceutics. 2020 Sep 13;12(9):871. doi: 10.3390/pharmaceutics12090871.

Abstract

Phytol is a diterpene alcohol and can be found as a product of the metabolism of chlorophyll in plants. This compound has been explored as a potential antimicrobial agent, but it is insoluble in water. In this study, we describe a novel approach for an interesting anticandidal drug delivery system containing phytol. Different formulations of phytol-loaded solid lipid nanoparticles (SLN) were designed and tested using a natural lipid, 1,3-distearyl-2-oleyl-glycerol (TG1). Different compositions were considered to obtain three formulations with 1:10, 1:5, and 1:3 phytol/TG1 ratios. All the formulations were prepared by emulsification solvent evaporation method and had their physicochemical properties assessed. The biocompatibility assay was performed in the HEK-293 cell line and the antifungal efficacy was demonstrated in different strains of ssp., including different clinical isolates. Spherical and uniform SLN (<300 nm, PdI < 0.2) with phytol-loading efficiency >65% were achieved. Phytol-loaded SLN showed a dose-dependent cytotoxic effect in the HEK-293 cell line. The three tested formulations of phytol-loaded SLN considerably enhanced the minimal inhibitory concentration of phytol against 15 strains of spp. Considering the clinical isolates, the formulations containing the highest phytol/TG1 ratios showed MICs at 100%. Thus, the feasibility and potential of phytol-loaded SLN was demonstrated in vitro, being a promising nanocarrier for phytol delivery from an anticandidal approach.

摘要

叶绿醇是一种二萜醇,可作为植物中叶绿素代谢的产物被发现。这种化合物已被探索作为一种潜在的抗菌剂,但它不溶于水。在本研究中,我们描述了一种含有叶绿醇的有趣抗念珠菌药物递送系统的新方法。使用天然脂质1,3 - 二硬脂酰 - 2 - 油酰甘油(TG1)设计并测试了不同配方的载叶绿醇固体脂质纳米粒(SLN)。考虑了不同的组成以获得三种叶绿醇/TG1比例为1:10、1:5和1:3的配方。所有配方均通过乳化溶剂蒸发法制备,并对其理化性质进行了评估。在HEK - 293细胞系中进行了生物相容性测定,并在不同的白色念珠菌菌株(包括不同的临床分离株)中证明了抗真菌效果。获得了球形且均匀的SLN(<300 nm,PdI < 0.2),叶绿醇负载效率>65%。载叶绿醇的SLN在HEK - 293细胞系中显示出剂量依赖性的细胞毒性作用。三种测试的载叶绿醇SLN配方显著提高了叶绿醇对15株白色念珠菌的最小抑菌浓度。考虑到临床分离株,含有最高叶绿醇/TG1比例的配方显示出100%的最低抑菌浓度。因此,载叶绿醇SLN的可行性和潜力在体外得到了证明,从抗念珠菌方法来看,它是一种有前途的叶绿醇递送纳米载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62b8/7558427/f8335622e06b/pharmaceutics-12-00871-g001.jpg

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