Gupta Anshita, Joshi Renjil, Dewangan Lokkanya, Shah Kamal, Soni Deependra, Patil Umesh K, Chauhan Nagendra Singh
Rungta College of Pharmaceutical Sciences and Research, Raipur, 492009, C.G., India.
Rungta College of Pharmaceutical Sciences and Research, Bhilai, 490024, C.G., India.
J Pharm Pharmacol. 2025 Apr 3;77(4):459-474. doi: 10.1093/jpp/rgae150.
A primary objective of this review is to summarize the evidence-based pharmacological applications of capsaicin, particularly its use to manage pain and treat various health conditions. A second goal of the review is to research how recent technological advances are improving the bioavailability and therapeutic index of capsaicin, as well as the development of novel capsaicin-mimetics that are able to enhance therapeutic responses in various human diseases.
In the review, numerous human clinical trials and preclinical studies are examined to determine how effective, safe, and optimal dosages of capsaicin can be used in pain management and therapeutic applications. Furthermore, it discusses capsaicin's mechanisms of action, specifically its interactions with the transient receptor potential vanilloid 1 (TRPV1) channel. As a result of this review, the potential of nanotechnology systems for bypassing the limits of capsaicin's pungency is discussed. The review takes into account individual factors such as pain tolerance and skin sensitivity.
For topical applications, capsaicin is typically used in concentrations ranging from 0.025% to 0.1%, with higher concentrations being used under medical supervision for neuropathic pain. The formulation can come in the form of creams, gels, or patches, which provide sustained release over the course of time. A condition such as arthritis or neuropathy can be relieved with capsaicin as it depletes substance P from nerves. Neuropathy and osteoarthritis as well as musculoskeletal disorders have been treated successfully with this herbal medicine. A major mechanism through which capsaicin relieves pain is through activating TRPV1 channels, which induce calcium influx and neurotransmitter release. Additionally, it affects the transcription of genes related to pain modulation and inflammation, particularly when disease conditions or stress are present. There have been recent developments in technology to reduce capsaicin's pungency and improve its bioavailability, including nanotechnology.
It is proven that capsaicin is effective in pain management as well as a variety of therapeutic conditions because of its ability to deplete substance P and desensitize nerve endings. Although capsaicin is highly pungent and associated with discomfort, advancements in delivery technologies and the development of capsaicin-mimetics promise improved therapeutic outcomes. There is a great deal of complexity in the pharmacological action of capsaicin due to its interaction with TRPV1 channels and its ability to affect gene transcription. There is a need for further research and development in order to optimize capsaicin's clinical applications and to enhance its therapeutic index in a variety of human diseases.
本综述的主要目的是总结辣椒素基于证据的药理学应用，特别是其在管理疼痛和治疗各种健康状况方面的应用。本综述的第二个目标是研究近期的技术进步如何提高辣椒素的生物利用度和治疗指数，以及新型辣椒素模拟物的开发，这些模拟物能够增强在各种人类疾病中的治疗反应。
在本综述中，研究了大量人体临床试验和临床前研究，以确定辣椒素在疼痛管理和治疗应用中的有效性、安全性和最佳剂量。此外，还讨论了辣椒素的作用机制，特别是其与瞬时受体电位香草酸受体1（TRPV1）通道的相互作用。作为本综述的结果，讨论了纳米技术系统绕过辣椒素辛辣味限制的潜力。本综述考虑了个体因素，如疼痛耐受性和皮肤敏感性。
对于局部应用，辣椒素通常使用浓度范围为0.025%至0.1%，在医学监督下，更高浓度用于治疗神经性疼痛。制剂可以是乳膏、凝胶或贴片的形式，它们在一段时间内提供持续释放。辣椒素可以缓解关节炎或神经病变等疾病，因为它能耗尽神经中的P物质。这种草药已成功治疗神经病变、骨关节炎以及肌肉骨骼疾病。辣椒素缓解疼痛的主要机制是通过激活TRPV1通道，诱导钙内流和神经递质释放。此外，它会影响与疼痛调节和炎症相关基因的转录，特别是在存在疾病状况或压力时。最近在技术方面有进展，可降低辣椒素的辛辣味并提高其生物利用度，包括纳米技术。
事实证明，辣椒素因其能够耗尽P物质和使神经末梢脱敏，在疼痛管理以及各种治疗状况中是有效的。尽管辣椒素具有高度辛辣味并会带来不适，但给药技术的进步和辣椒素模拟物的开发有望改善治疗效果。由于辣椒素与TRPV1通道的相互作用及其影响基因转录的能力，其药理作用存在很大复杂性。需要进一步的研究和开发，以优化辣椒素的临床应用并提高其在各种人类疾病中的治疗指数。
