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Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Nicoboxil is an aromatic carboxylic acid and a member of pyridines with topical vasodilatory (rubefacient) properties. It is indicated for use as an active ingredient in combination with nonivamide in topical analgesics for the temporary relief of the pain of rheumatism, arthritis, lumbago, muscular aches, sprains and strains, sporting injuries, and other conditions where local warmth is beneficial (1).
Incapacitating Agents and Technologies: A Review *
Published in Brian J. Lukey, James A. Romano, Salem Harry, Chemical Warfare Agents, 2019
Pelargonic acid vanillylamide, also known as nonivamide, is a synthetic equivalent of capsaicin. Their structures are compared in Figure 15.2. It is available in a commercial spray product known as Cap-Tor, which is being increasingly used by U.K. police authorities and in European countries to replace Agent CS irritant liquid sprays (BBC, 2001, 2002, 2004b). It is advised that the device should be aimed at the face, particularly the eyes. Most spray devices contain 0.3% PAVA in 50% ethanol with nitrogen as the propellant. The maximum effective range is 8 to 15 feet (COT, 2002), but devices should not be discharged at less than a distance of 3 feet because of risk of pressure injury to the eye. Particle sizes are mainly greater than 100 mm with a small proportion in the range 2 to 10 mm and a trace smaller than 2 mm. The toxicology and clinical experience for PAVA and its formulation, as summarized in Section 15.3.7.1, is not yet adequate to permit a complete assessment of the potential human health effects of the material.
Overcoming hydrolytic degradation challenges in topical delivery: non-aqueous nano-emulsions
Published in Expert Opinion on Drug Delivery, 2022
Arya Kadukkattil Ramanunny, Sachin Kumar Singh, Sheetu Wadhwa, Monica Gulati, Bhupinder Kapoor, Rubiya Khursheed, Gowthamarajan Kuppusamy, Kamal Dua, Harish Dureja, Dinesh Kumar Chellappan, Niraj Kumar Jha, Piyush Kumar Gupta, Sukriti Vishwas
The ability of NANEs to pass this barrier is the major reason for exploring them in dermatological and cosmeceutical application. Certain drug molecules present formulation related challenges due to their high lipophilicity and low stability. ASX [12], cholecalciferol [10], ascorbic acid [11], and deoxyarbutin [13] are examples of drug candidates that are prone to hydrolytic degradation. These drugs require a delivery system which is completely free from aqueous phase to ensure its stability within the system. Another such drug that faces challenge due to its high lipophilicity and has been successfully delivered to the skin is nonivamide. Major challenges addressed by NANEs of nonivamide are its high lipophilicity and tendency to cause burning sensation when it comes in contact with the patient’s skin. NANEs were found to protect the drug and reduce its direct exposure to the skin [14]. Table 6 summarizes the benefits of NANEs and study outcomes for the selected drug candidates that are either highly lipophilic or are prone to aqueous degradation.
Utility of in vitro and in vivo systems for studying the permeability of capsaicin and nonivamide through different intestinal regions
Published in Xenobiotica, 2018
Lian Duan, Huaidong Peng, Guangcan Li, Ruolun Wang, Yanfang Chen
The in vitro studies show that the permeability of capsaicin across the colonic mucosa in the mucosal-serosal direction is remarkably higher than that across the jejunal or ileac mucosa. These results agreed with the previous in vitro study described by the authors (Duan et al., 2013b). Some researchers had also found that though those two compounds have similar physicochemical properties, the plasma profile and bioavailability of nonivamide through percutaneous absorption were higher than those of capsaicin (Fang et al., 1996). The in vitro membrane transport study had also been used to demonstrate that methylated flavones have dramatically higher intestinal permeability than those of the structurally-similar unmethylated forms (Wen & Walle, 2006).
Comparative safety evaluation of riot control agents of synthetic and natural origin
Published in Inhalation Toxicology, 2018
Ravindra M. Satpute, Pramod K. Kushwaha, D. P. Nagar, P. V. L. Rao
Oleoresin capsicum (OC) is an oily resin derivative from the ripe fruit (chili) of genus Capsicum frutescence and composed of several related compounds. The main active ingredient of the OC is capsaicinoids which are the products of endocrine glands found in the plant placenta and are a mixture of two unsaturated and three saturated homologs. It is the presence and percentage of these capsaicinoids which determines the pungency of chilies which further determines their suitability for oleoresin extraction. Capsaicinoids are isolated through a volatile solvent extraction of the dried, ripened fruit of chili peppers. The capsaicinoids are distilled, dried, and compounded together. The final oleoresin contains several branched-chain alkyl vanillylamides, in addition to capsaicin, the major component in OC. The predominant capsaicinoid components of OC are capsaicin (70%), dihydrocapsaicin (20%), norhydrocapsaicin (7%), homocapsaicin (1%), and homodihydrocapsaicin (1%) (Salem et al., 2006). Capsaicinoids cause dermatitis as well as nasal, ocular, pulmonary, and gastrointestinal effects in humans. OC gained popularity in the 1990s as a defensive weapon for civilians (particularly women as pepper spray) and law enforcement agencies because they produce an immediate, temporary immobilization, and incapacitation when sprayed directly into the face or eyes. It is important to note that hand-held pepper spray formulations can contain OC by themselves or a mixture of OC and CS. In addition to OC, Pelargonic acid vanillylamide (PAVA or nonivamide), is a synthetic form of capsaicin. Nonivamide (first synthesized by Nelson in 1919) was originally found to be a minor component in Capsicum annum peppers (Constant & Cordell, 1996); however, the majority of PAVA is derived from synthesis rather than extraction from natural plant sources. As a result, the composition and concentration of PAVA can remain consistent (Haber et al., 2007). Nonivamide has been used both as a food flavor (at up to 10 ppm in the diet) and in human medicine (topical application as a rubifaciant). In USA, it has been given GRAS (Generally Regarded as Safe) status by the Food and Drug Administration as a food flavor. Though it is a potent sensory stimulant, but in order for PAVA to work, it must be directed at the subject’s eyes. It was found to be ineffective against those under the influence of alcohol (ACPO, 2006). The pain to the eyes is reported to be higher than that caused by CS tear gas (ACPO, 2006; Smith et al., 2004).