<br>重振大蒜素用于癌症治疗：提高生物利用度、稳定性和临床疗效的配方策略进

重振大蒜素用于癌症治疗：提高生物利用度、稳定性和临床疗效的配方策略进展
Naunyn-Schmiedeberg's Archives of Pharmacology ( IF 3.1 ) Pub Date : 2023-08-24 , DOI: 10.1007/s00210-023-02675-3
Rajni Bala 1 , Reecha Madaan 1 , Samrat Chauhan 1 , Malika Gupta 1 , Ankit Kumar Dubey 2, 3 , Ishrat Zahoor 4 , Hemavathi Brijesh 5 , Daniela Calina 6 , Javad Sharifi-Rad 7

Affiliation  

Chitkara College of Pharmacy, Chitkara University, Rajpura, Punjab, India.

iGlobal Research and Publishing Foundation, New Delhi, India.

Institute of Scholars, Chikmagalur, India.

Maharishi Markandeshwar College of Pharmacy, Maharishi Markandeshwar (Deemed to Be University), Mullana-Ambala, Haryana, 133207, India.

Department of Biotechnology, School of Applied Sciences, REVA University, Bengaluru, Karnataka, India.

Department of Clinical Pharmacy, University of Medicine and Pharmacy of Craiova, 200349, Craiova, Romania.

Facultad de Medicina, Universidad del Azuay, Cuenca, Ecuador.

本次综述的主要目的是强调大蒜素（大蒜中的一种防御分子，以其多种健康益处而闻名）的治疗潜力，并解决其生物利用度和稳定性的关键挑战。该研究进一步旨在评估各种配方策略和基于纳米技术的输送系统，以解决这些问题并提高大蒜素的临床疗效，特别是在癌症治疗中。我们对现有文献和先前的研究进行了全面回顾，重点关注大蒜素的治疗特性、其生物利用度、稳定性问题和新颖的制剂策略。我们评估了大蒜素在癌症中的作用机制，包括其对信号通路、细胞周期、细胞凋亡、自噬和肿瘤发展的影响。我们还评估了不同类型癌症（如乳腺癌、宫颈癌、结肠癌、肺癌和胃癌）的体外和体内研究结果。尽管大蒜素具有显着的治疗功效，包括心血管、抗高血压、降低胆固醇、抗菌、抗真菌、抗癌和免疫调节活性，但由于稳定性差和不可预测的生物利用度，其临床应用受到限制。大蒜素在胃肠道中的生物利用度取决于蒜氨酸酶的活性，其稳定性会受到胃酸和肠道蛋白酶等多种条件的影响。配方策略和基于纳米技术的药物输送系统的最新进展显示出解决这些挑战的希望，有可能提高大蒜素的溶解度、稳定性和生物利用度。 大蒜素为癌症治疗提供了巨大的潜力，但其应用因其不稳定性和生物利用度差而受到阻碍。新颖的配方策略和基于纳米技术的递送系统可以显着克服这些限制，增强大蒜素的治疗功效。未来的研究应集中于完善这些制剂策略和递送系统，确保这些新大蒜素制剂的安全性和有效性。应进行临床试验和长期研究，以确定最佳剂量，评估潜在的副作用，并评估其现实世界的适用性。不同药物递送方法的比较分析和靶向递送系统的开发也可以为增强大蒜素的治疗潜力提供进一步的见解。

Revitalizing allicin for cancer therapy: advances in formulation strategies to enhance bioavailability, stability, and clinical efficacy

The main objective of this review is to highlight the therapeutic potential of allicin, a defense molecule in garlic known for its diverse health benefits, and address the key challenges of its bioavailability and stability. The research further aims to evaluate various formulation strategies and nanotechnology-based delivery systems that can resolve these issues and improve allicin’s clinical efficacy, especially in cancer therapy. We conducted a comprehensive review of the available literature and previous studies, focusing on the therapeutic properties of allicin, its bioavailability, stability issues, and novel formulation strategies. We assessed the mechanism of action of allicin in cancer, including its effects on signaling pathways, cell cycle, apoptosis, autophagy, and tumor development. We also evaluated the outcomes of both in vitro and in vivo studies on different types of cancers, such as breast, cervical, colon, lung, and gastric cancer. Despite allicin’s significant therapeutic benefits, including cardiovascular, antihypertensive, cholesterol-lowering, antimicrobial, antifungal, anticancer, and immune-modulatory activity, its clinical utility is limited due to poor stability and unpredictable bioavailability. Allicin’s bioavailability in the gastrointestinal tract is dependent on the activity of the enzyme alliinase, and its stability can be affected by various conditions like gastric acid and intestinal enzyme proteases. Recent advances in formulation strategies and nanotechnology-based drug delivery systems show promise in addressing these challenges, potentially improving allicin’s solubility, stability, and bioavailability. Allicin offers substantial potential for cancer therapy, yet its application is hindered by its instability and poor bioavailability. Novel formulation strategies and nanotechnology-based delivery systems can significantly overcome these limitations, enhancing the therapeutic efficacy of allicin. Future research should focus on refining these formulation strategies and delivery systems, ensuring the safety and efficacy of these new allicin formulations. Clinical trials and long-term studies should be carried out to determine the optimal dosage, assess potential side effects, and evaluate their real-world applicability. The comparative analysis of different drug delivery approaches and the development of targeted delivery systems can also provide further insight into enhancing the therapeutic potential of allicin.