Extraction, Isolation, Characterization, and Development of Phospholipids Complex Nanocarrier for Improved Solubility, Antiasthmatic, and Pharmacokinetic Potential of Curcuminoids.

IF 2.2 4区医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY Current pharmaceutical biotechnology Pub Date : 2024-10-03 DOI:10.2174/0113892010326636240919094339

Darshan R Telange, Pragati V Pandhare, Krutika R Sawarkar, Ujwala N Mahajan, Saurabh B Ganorkar, Amol S Warokar

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Abstract

Background: Curcuma longa Linn. (Zingiberaceae) is a medicinal plant with significant biological activities owing to curcuminoids (CURs). Nevertheless, its low oral bioavailability because of low water solubility, inadequate absorption, short half-life, and rapid clearance hampered its clinical applications.

Objective: The study aimed to extract, isolate, characterize, and formulate the Phospholipon ®90H complex and evaluate for improved solubility, antiasthmatic and pharmacokinetic potential of CURs.

Methods: Phospholipon®90H-based complex of curcuminoids (CPLC) was synthesized via solvent evaporation technique and reported an improvement of solubility, antiasthmatic, and pharmacokinetic potential of CURs. CPLC was physico-chemically and functionally evaluated by Fourier transforms infrared spectroscopy, differential scanning calorimetry, powder x-ray diffractometry, oral bioavailability, and antiasthmatic activity.

Results: Ethyl acetate rhizome extracts (EARE) displayed ~17.42 % w/w extraction yield of CURs. CPLC revealed high entrapment of CURs (~ 92.55 % w/w) within the polar head of phospholipids. Small particle size ~ 194 nm with zeta potential value ~ -20.4 mV suggests the physical stability of CPLC. Physical analysis evidenced the formation of stable and amorphous CPLC by establishing hydrophobic and weak intermolecular forces between CURs and Phospholipon ®90H. Undoubtedly, the amorphous CPLC raised the aqueous solubility of CURs (~2-fold) compared to pure CURs. CPLC formulations (~ 20 mg/kg of CURs, p.o.) significantly lowered the leucocyte and eosinophil count compared to pure CURs. CPLC improved the oral bioavailability of CURs compared to pure CURs.

Conclusion: Results highlight that CPLC could be established as a breakthrough respiratory nanocarrier for CURs and other phytocompounds with respiratory potential.

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提取、分离、表征和开发磷脂复合纳米载体，以提高姜黄素的溶解度、抗哮喘性和药代动力学潜力。

背景：姜黄（姜科）是一种药用植物，其姜黄素（CURs）具有显著的生物活性。然而，由于水溶性低、吸收不足、半衰期短、清除快等原因，其口服生物利用度较低，阻碍了其临床应用：本研究旨在提取、分离、表征和配制磷脂素 ®90H复合物，并评估其在改善 CURs 的溶解度、抗哮喘和药代动力学潜力方面的作用：方法：通过溶剂蒸发技术合成了以磷脂酰 ®90H为基础的姜黄素复合物（CPLC），并报道了该复合物改善了姜黄素的溶解性、抗哮喘性和药动学潜力。通过傅立叶变换红外光谱法、差示扫描量热法、粉末 X 射线衍射仪、口服生物利用度和抗哮喘活性对 CPLC 进行了物理化学和功能评价：醋酸乙酯根茎提取物（EARE）的 CURs 提取率约为 17.42%（重量百分比）。液相色谱（CPLC）显示，CURs（约 92.55 % w/w）在磷脂的极性头中有很高的吸附率。小粒径 ~ 194 nm，zeta 电位值 ~ -20.4 mV，这表明 CPLC 具有物理稳定性。物理分析表明，通过在 CURs 和磷脂 ®90H 之间建立疏水和微弱的分子间作用力，形成了稳定的无定形 CPLC。毫无疑问，与纯 CURs 相比，无定形 CPLC 提高了 CURs 的水溶性（约 2 倍）。与纯 CURs 相比，CPLC 制剂（约 20 毫克/千克 CURs，口服）显著降低了白细胞和嗜酸性粒细胞计数。与纯 CURs 相比，CPLC 提高了 CURs 的口服生物利用度：结论：研究结果表明，CPLC 可以作为一种突破性的呼吸道纳米载体，用于 CURs 和其他具有呼吸道潜力的植物化合物。

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来源期刊

Current pharmaceutical biotechnology 医学-生化与分子生物学

CiteScore

5.60

自引率

3.60%

发文量

203

审稿时长

6 months

期刊介绍： Current Pharmaceutical Biotechnology aims to cover all the latest and outstanding developments in Pharmaceutical Biotechnology. Each issue of the journal includes timely in-depth reviews, original research articles and letters written by leaders in the field, covering a range of current topics in scientific areas of Pharmaceutical Biotechnology. Invited and unsolicited review articles are welcome. The journal encourages contributions describing research at the interface of drug discovery and pharmacological applications, involving in vitro investigations and pre-clinical or clinical studies. Scientific areas within the scope of the journal include pharmaceutical chemistry, biochemistry and genetics, molecular and cellular biology, and polymer and materials sciences as they relate to pharmaceutical science and biotechnology. In addition, the journal also considers comprehensive studies and research advances pertaining food chemistry with pharmaceutical implication. Areas of interest include: DNA/protein engineering and processing Synthetic biotechnology Omics (genomics, proteomics, metabolomics and systems biology) Therapeutic biotechnology (gene therapy, peptide inhibitors, enzymes) Drug delivery and targeting Nanobiotechnology Molecular pharmaceutics and molecular pharmacology Analytical biotechnology (biosensing, advanced technology for detection of bioanalytes) Pharmacokinetics and pharmacodynamics Applied Microbiology Bioinformatics (computational biopharmaceutics and modeling) Environmental biotechnology Regenerative medicine (stem cells, tissue engineering and biomaterials) Translational immunology (cell therapies, antibody engineering, xenotransplantation) Industrial bioprocesses for drug production and development Biosafety Biotech ethics Special Issues devoted to crucial topics, providing the latest comprehensive information on cutting-edge areas of research and technological advances, are welcome. Current Pharmaceutical Biotechnology is an essential journal for academic, clinical, government and pharmaceutical scientists who wish to be kept informed and up-to-date with the latest and most important developments.