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使用固体脂质纳米粒提高姜黄素的生物利用度和稳定性（CLEN）：对其有效性的一种保证

Enhancing Bioavailability and Stability of Curcumin Using Solid Lipid Nanoparticles (CLEN): A Covenant for Its Effectiveness.

作者信息

Gupta Tanvi, Singh Joga, Kaur Sandeep, Sandhu Simarjot, Singh Gurpal, Kaur Indu Pal

机构信息

University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.

出版信息

Front Bioeng Biotechnol. 2020 Oct 15;8:879. doi: 10.3389/fbioe.2020.00879. eCollection 2020.

DOI:10.3389/fbioe.2020.00879
PMID:33178666
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7593682/
Abstract

Curcumin, very rightly referred to as "a wonder drug" is proven to be efficacious in a variety of inflammatory disorders including cancers. Antiaging, anti-inflammatory, antioxidant, antitumor, chemosensitizing, P-gp efflux inhibiting, and antiproliferative activity are some of the striking features of curcumin, highlighting its importance in chemotherapy. Curcumin inhibits Bcl-2, Bcl-XL, VEGF, c-My, ICAM-1, EGFR, STAT3 phosphorylation, and cyclin D1 genes involved in the various stages of breast, prostate, and gastric cancer proliferation, angiogenesis, invasion, and metastasis. The full therapeutic potential of curcumin however remains under explored mainly due to poor absorption, rapid metabolism and systemic elimination culminating in its poor bioavailability. Furthermore, curcumin is insoluble, unstable at various pH and is also prone to undergo photodegradation. Nanotechnology can help improve the therapeutic potential of drug molecules with compromised biopharmaceutical profiles. Solid lipid nanoparticles (SLNs) are the latest offshoot of nanomedicine with proven advantages of high drug payload, longer shelf life, biocompatibility and biodegradability, and industrial amenability of the production process. We successfully developed CLEN (Curcumin encapsulated lipidic nanoconstructs) containing 15 mg curcumin per ml of the SLN dispersion with highest (till date, to our knowledge) increase in solubility of curcumin in an aqueous system by 1.4 × 10 times as compared to its intrinsic solubility of 11 ng/ml and high drug loading (15% w/v with respect to lipid matrix). Zero-order release kinetics observed for CLEN versus first order release for free curcumin establish controlled release nature of the developed CLEN. It showed 69.78 times higher oral bioavailability with respect to free curcumin; 9.00 times higher than a bioavailable marketed formulation (CurcuWIN). The formulation showed 104, 13.3, and 10-times enhanced stability at pH 6.8, 1.2, and 7.4, respectively. All these factors ensure the efficacy of CLEN in treating cancer and other inflammatory diseases.

摘要

姜黄素被恰如其分地称为“神奇药物”，已被证明对包括癌症在内的多种炎症性疾病有效。抗衰老、抗炎、抗氧化、抗肿瘤、化学增敏、抑制P-糖蛋白外排和抗增殖活性是姜黄素的一些显著特性，突出了其在化疗中的重要性。姜黄素抑制参与乳腺癌、前列腺癌和胃癌增殖、血管生成、侵袭和转移各个阶段的Bcl-2、Bcl-XL、VEGF、c-My、ICAM-1、EGFR、STAT3磷酸化以及细胞周期蛋白D1基因。然而，姜黄素的全部治疗潜力仍有待探索，主要原因是其吸收差、代谢快和全身清除，最终导致其生物利用度低。此外，姜黄素不溶，在不同pH值下不稳定，还容易发生光降解。纳米技术有助于提高生物制药特性不佳的药物分子的治疗潜力。固体脂质纳米粒（SLNs）是纳米医学的最新成果，具有高载药量、保质期长、生物相容性和生物可降解性以及生产过程易于工业化等已被证实的优点。我们成功开发了CLEN（姜黄素包封脂质纳米结构体），每毫升SLN分散体中含有15毫克姜黄素，与姜黄素在水系统中的固有溶解度11纳克/毫升相比，其在水系统中的溶解度提高了1.4×10倍（据我们所知，这是迄今为止最高的），且载药量高（相对于脂质基质为15% w/v）。观察到CLEN呈现零级释放动力学，而游离姜黄素为一级释放，这证实了所开发的CLEN具有控释性质。与游离姜黄素相比，其口服生物利用度高出69.78倍；比市售生物可利用制剂（CurcuWIN）高出9.00倍。该制剂在pH 6.8、1.2和7.4时的稳定性分别提高了104倍、13.3倍和10倍。所有这些因素都确保了CLEN在治疗癌症和其他炎症性疾病方面的疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/08750c53988b/fbioe-08-00879-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/5e15e5a8c73f/fbioe-08-00879-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/b27ddbc26803/fbioe-08-00879-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/7af31ceab41c/fbioe-08-00879-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/5ba8f99b18f6/fbioe-08-00879-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/2e870691a59d/fbioe-08-00879-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/2123411280e0/fbioe-08-00879-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/b131173df6dd/fbioe-08-00879-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/08750c53988b/fbioe-08-00879-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/5e15e5a8c73f/fbioe-08-00879-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/b27ddbc26803/fbioe-08-00879-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/7af31ceab41c/fbioe-08-00879-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/5ba8f99b18f6/fbioe-08-00879-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/2e870691a59d/fbioe-08-00879-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/2123411280e0/fbioe-08-00879-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/b131173df6dd/fbioe-08-00879-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7503/7593682/08750c53988b/fbioe-08-00879-g008.jpg

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本文引用的文献

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