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载有薯蓣皂苷元的聚合物纳米粒具有潜在的抗癌功效。

Diosgenin Loaded Polymeric Nanoparticles with Potential Anticancer Efficacy.

机构信息

Department of Biotechnology, School of Life Sciences, Central University of Rajasthan, Ajmer 305817, India.

Department of Biotechnology, IIS (Deemed to be University), Jaipur 302020, India.

出版信息

Biomolecules. 2020 Dec 16;10(12):1679. doi: 10.3390/biom10121679.

DOI:10.3390/biom10121679
PMID:33339083
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7765552/
Abstract

This study aims to determine the anticancer efficacy of diosgenin encapsulated poly-glycerol malate co-dodecanedioate (PGMD) nanoparticles. Diosgenin loaded PGMD nanoparticles (variants 7:3 and 6:4) were synthesized by the nanoprecipitation method. The synthesis of PGMD nanoparticles was systematically optimized employing the Box-Behnken design and taking into account the influence of various independent variables such as concentrations of each PGMD, diosgenin and PF-68 on the responses such as size and PDI of the particles. Mathematical modeling was done using the Quadratic second order modeling method and response surface analysis was undertaken to elucidate the factor-response relationship. The obtained size of PGMD 7:3 and PGMD 6:4 nanoparticles were 133.6 nm and 121.4 nm, respectively, as measured through dynamic light scattering (DLS). The entrapment efficiency was in the range of 77-83%. The in vitro drug release studies showed diffusion and dissolution controlled drug release pattern following Korsmeyer-Peppas kinetic model. Furthermore, in vitro morphological and cytotoxic studies were performed to evaluate the toxicity of synthesized drug loaded nanoparticles in model cell lines. The IC after 48 h was observed to be 27.14 µM, 15.15 µM and 13.91 µM for free diosgenin, PGMD 7:3 and PGMD 6:4 nanoparticles, respectively, when administered in A549 lung carcinoma cell lines.

摘要

本研究旨在确定薯蓣皂苷元包封聚甘油马来酸-co-十二烷二酸（PGMD）纳米粒子的抗癌功效。采用纳米沉淀法合成了负载薯蓣皂苷元的 PGMD 纳米粒子（变体 7:3 和 6:4）。通过 Box-Behnken 设计系统地优化了 PGMD 纳米粒子的合成，并考虑了各种独立变量（如 PGMD、薯蓣皂苷元和 PF-68 的浓度）对粒径和 PDI 等响应的影响。采用二次方模型方法进行数学建模，并进行响应面分析以阐明因素-响应关系。通过动态光散射（DLS）测量，得到 PGMD 7:3 和 PGMD 6:4 纳米粒子的粒径分别为 133.6nm 和 121.4nm。包封效率在 77-83%之间。体外药物释放研究表明，药物释放模式遵循 Korsmeyer-Peppas 动力学模型，即扩散和溶解控制药物释放。此外，还进行了体外形态学和细胞毒性研究，以评估合成载药纳米粒子在模型细胞系中的毒性。在 A549 肺癌细胞系中，游离薯蓣皂苷元、PGMD 7:3 和 PGMD 6:4 纳米粒子的 48 h 后 IC 分别为 27.14µM、15.15µM 和 13.91µM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/6ab835e034bb/biomolecules-10-01679-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/d2f981e3fe26/biomolecules-10-01679-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/90a00a4d24b7/biomolecules-10-01679-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/dfc88a9bbaa5/biomolecules-10-01679-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/f7835566c653/biomolecules-10-01679-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/a403f3e932bb/biomolecules-10-01679-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/46dd9071530b/biomolecules-10-01679-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/7704cd81f64d/biomolecules-10-01679-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/3f5797cb7d82/biomolecules-10-01679-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/6ab835e034bb/biomolecules-10-01679-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/d2f981e3fe26/biomolecules-10-01679-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/90a00a4d24b7/biomolecules-10-01679-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/dfc88a9bbaa5/biomolecules-10-01679-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/f7835566c653/biomolecules-10-01679-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/a403f3e932bb/biomolecules-10-01679-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/46dd9071530b/biomolecules-10-01679-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/7704cd81f64d/biomolecules-10-01679-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/3f5797cb7d82/biomolecules-10-01679-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fef0/7765552/6ab835e034bb/biomolecules-10-01679-g009.jpg

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