Design of Optimized Solid Lipid Nanoparticles of Montelukast Sodium and Assessment of Oral Bioavailability in Experimental Model.

IF 2.2 4区医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY Current pharmaceutical biotechnology Pub Date : 2024-06-24 DOI:10.2174/0113892010300965240612054349

Pankaj Dangre, Paresh Wankhede, Kailas Moravkar, Mohan Kalaskar, Atish Mundadad, Shailesh Chalikwar

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Abstract

Introduction: The objective of the reported work was to develop Montelukast sodium (MS) solid lipid nanoparticles (MS-SLNs) to ameliorate its oral bio-absorption. Herein, the highpressure homogenization (HPH) principle was utilized for the fabrication of MS-SLNs.

Method: The study encompasses a 23 full factorial statistical design approach where mean particle size (Y1) and percent entrapment efficiency (Y2) were screened as dependent variables while, the concentration of lipid (X1), surfactant (X2), and co-surfactant (X3) were screened as independent variables. The investigation of MS-SLNs by DSC and XRD studies unveiled the molecular dispersion of MS into the SLNs while TEM study showed the smooth surface of developed MSSLNs. The optimized MS-SLNs exhibited mean particle size (MPS) = 115.5 ± 1.27 nm, polydispersity index (PDI) = 0.256 ± 0.04, zeta potential (ζ) = -21.9 ± 0.32 mV and entrapment efficiency (EE) = 90.97 ± 1.12 %. The In vivo pharmacokinetic study performed in Albino Wistar rats revealed 2.87-fold increments in oral bioavailability.

Results: The accelerated stability studies of optimized formulation showed good physical and chemical stability. The shelf life estimated for the developed MS-SLN was found to be 22.38 months.

Conclusion: At the outset, the developed MS-SLNs formulation showed a significant increment in oral bioavailability and also exhibited excellent stability in exaggerated storage conditions.

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设计优化的孟鲁司特钠固体脂质纳米颗粒并在实验模型中评估其口服生物利用度

导言：报告的目的是开发孟鲁司特钠（MS）固体脂质纳米颗粒（MS-SLNs），以改善其口腔生物吸收。本研究利用高压均质（HPH）原理制备 MS-SLNs：本研究采用 23 全因子统计设计方法，将平均粒径（Y1）和夹带效率（Y2）作为因变量，将脂质（X1）、表面活性剂（X2）和辅助表面活性剂（X3）的浓度作为自变量。通过 DSC 和 XRD 对 MS-SLNs 进行的研究揭示了 MS 分子在 SLNs 中的分散情况，而 TEM 研究则显示所制备的 MSSLNs 表面光滑。优化后的 MS-SLNs 平均粒径 (MPS) = 115.5 ± 1.27 nm，多分散指数 (PDI) = 0.256 ± 0.04，Zeta 电位 (ζ) = -21.9 ± 0.32 mV，包埋效率 (EE) = 90.97 ± 1.12 %。在白化 Wistar 大鼠体内进行的药代动力学研究显示，口服生物利用度增加了 2.87 倍：结果：对优化制剂的加速稳定性研究表明其具有良好的物理和化学稳定性。结果：加速稳定性研究表明，优化配方具有良好的物理和化学稳定性，所开发的 MS-SLN 的保质期估计为 22.38 个月：从一开始，所开发的 MS-SLNs 制剂就显示出口服生物利用度的显著提高，并且在苛刻的储存条件下也表现出良好的稳定性。

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

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.