含青蒿素和姜黄素的固体脂质纳米颗粒的制备和体外表征

Q2 Pharmacology, Toxicology and Pharmaceutics Pharmaceutical nanotechnology Pub Date : 2024-07-19 DOI:10.2174/0122117385296893240626061552
Bhagyashri Khatri, Vaishali Thakkar, Saloni Dalwadi, Avani Shah, Hardik Rana, Purvi Shah, Tejal Gandhi, Bhupendra Prajapati
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引用次数: 0

摘要

背景:疟疾仍然是非洲、东南亚和南美洲部分地区的一个严重公共卫生障碍,对青蒿素类复方制剂等抗疟药物的抗药性加剧了这一问题。姜黄素和青蒿素的复方制剂具有减少剂量、降低毒性、协同增效以及改善给药方式的潜力,因此前景广阔:本研究旨在利用固体脂质纳米颗粒(SLNs)提高姜黄素和青蒿素的溶解度和溶出率。由于这两种药物的水溶性差、吸收效率低、代谢和消除速度快,口服给药面临挑战:研究重点是配制和优化包裹青蒿素(ART)和姜黄素(CUR)的固体脂质纳米颗粒(SLNs)。固体脂质纳米颗粒是采用热均质法和超声波法研制而成的。使用差示扫描量热法(DSC)评估了药物与赋形剂的相容性。对脂质和表面活性剂进行了筛选,以选出合适的成分。采用 3² 全因子设计研究了脂质和表面活性剂浓度对夹持效率(%EE)和累积药物释放率(%CDR)等关键参数的影响。此外,还对夹带率、药物负载、粒度、ZETA电位和体外药物释放进行了评估:结果:采用全因子设计成功开发了青蒿素和姜黄素 SLNs,显示出药物释放受控和较高的夹持效率。优化后的纳米颗粒大小为 114.7nm,均匀度(PDI:0.261)和 zeta 电位为 -9.24 mV。青蒿素和姜黄素的 %EE 值分别为 79.1% 和 74.5%,累积药物释放率分别为 85.1% 和 80.9%。全因子设计表明,增加脂质浓度可提高释放率,而增加表面活性剂浓度则可提高药物释放率和释放率。对优化批次的稳定性研究表明,其物理和化学特性没有发生变化:该研究成功开发了青蒿素和姜黄素的固体脂质纳米颗粒(SLNs),实现了药物的可控释放、高包埋效率以及理想的粒度和均匀性。这一进步有望提高草药制剂的给药效果。
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Preparation and In-Vitro Characterization of Solid Lipid Nanoparticles Containing Artemisinin and Curcumin.

Background: Malaria remains a formidable public health obstacle across Africa, Southeast Asia, and portions of South America, exacerbated by resistance to antimalarial medications, such as artemisinin-based combinations. The combination of curcumin and artemisinin shows promise due to its potential for dose reduction, reduced toxicity, synergistic effects, and suitability for drug delivery improvement.

Objective: This research aims to enhance the solubility and dissolution rates of curcumin and artemisinin by employing Solid Lipid Nanoparticles (SLNs). Oral delivery of both drugs faces challenges due to their poor water solubility, inefficient absorption, and rapid metabolism and elimination.

Method: The study focuses on formulating and optimizing Solid Lipid Nanoparticles (SLNs) encapsulating artemisinin (ART) and curcumin (CUR). SLNs were developed using the hot homogenization method, incorporating ultrasonication. Drug-excipient compatibility was evaluated using Differential Scanning Calorimetry (DSC). Lipid and surfactant screening was performed to select suitable components. A 3² full factorial design was utilized to investigate the influence of lipid and surfactant concentrations on key parameters, such as entrapment efficiency (%EE) and cumulative drug release (%CDR). Additionally, evaluations of % entrapment efficiency, drug loading, particle size, zeta potential, and in-vitro drug release were conducted.

Results: Successful development of artemisinin and curcumin SLNs was achieved using a full factorial design, demonstrating controlled drug release and high entrapment efficiency. The optimized nanoparticles exhibited a size of 114.7nm, uniformity (PDI: 0.261), and a zeta potential of -9.24 mV. Artemisinin and curcumin showed %EE values of 79.1% and 74.5%, respectively, with cumulative drug release of 85.1% and 80.9%, respectively. The full factorial design indicated that increased lipid concentration improved %EE, while higher surfactant concentration enhanced drug release and %EE. Stability studies of the optimized batch revealed no alterations in physical or chemical characteristics.

Conclusion: The study successfully developed Solid Lipid Nanoparticles (SLNs) for artemisinin and curcumin, achieving controlled drug release, high entrapment efficiency, and desired particle size and uniformity. This advancement holds promise for enhancing drug delivery of herbal formulations.

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来源期刊
Pharmaceutical nanotechnology
Pharmaceutical nanotechnology Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
4.20
自引率
0.00%
发文量
46
期刊介绍: Pharmaceutical Nanotechnology publishes original manuscripts, full-length/mini reviews, thematic issues, rapid technical notes and commentaries that provide insights into the synthesis, characterisation and pharmaceutical (or diagnostic) application of materials at the nanoscale. The nanoscale is defined as a size range of below 1 µm. Scientific findings related to micro and macro systems with functionality residing within features defined at the nanoscale are also within the scope of the journal. Manuscripts detailing the synthesis, exhaustive characterisation, biological evaluation, clinical testing and/ or toxicological assessment of nanomaterials are of particular interest to the journal’s readership. Articles should be self contained, centred around a well founded hypothesis and should aim to showcase the pharmaceutical/ diagnostic implications of the nanotechnology approach. Manuscripts should aim, wherever possible, to demonstrate the in vivo impact of any nanotechnological intervention. As reducing a material to the nanoscale is capable of fundamentally altering the material’s properties, the journal’s readership is particularly interested in new characterisation techniques and the advanced properties that originate from this size reduction. Both bottom up and top down approaches to the realisation of nanomaterials lie within the scope of the journal.
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