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Topical Anesthetics
Published in Marwali Harahap, Adel R. Abadir, Anesthesia and Analgesia in Dermatologic Surgery, 2019
EMLA is a eutectic mixture of the local anesthetics lidocaine 2.5% and prilocaine 2.5% (6). The term “eutectic” refers to the fact that the mixture has a melting point lower than that of either anesthetic alone (7). Thus it consists as an emulsion with a dispersed phase (the mixture) and a continuous phase (water). The absorption is therefore enhanced by the water component.
Chemical Modulation of Topical and Transdermal Permeation
Published in Marc B. Brown, Adrian C. Williams, The Art and Science of Dermal Formulation Development, 2019
Marc B. Brown, Adrian C. Williams
The first commercially successful eutectic formulation for topical use was EMLA cream, a eutectic mixture of the local anaesthetics lidocaine and prilocaine. As with other approaches such as prodrugs, combining the melting point depression effect with a chemical penetration enhancer has been explored. Thus, the melting point depression effect from eutectics generated using between ibuprofen and a series of terpene penetration enhancers was evaluated (Stott et al., 1998); most useful was a system formed between the drug and the enhancer thymol, which generated a eutectic system that melted at 32˚C (i.e., at around skin temperature). More complex behaviour was reported for propranolol with fatty acids where eutectic systems were formed between propranolol with an addition complex formed between propranolol and the enhancer capric acid (Stott et al., 2001). Terpenes have been used to form eutectic mixtures with other drugs, for example, lidocaine with thymol or menthol that provided compositions with melting points near or below skin temperature, and testosterone with menthol.
Hands
Published in Tor Wo Chiu, Stone’s Plastic Surgery Facts, 2018
EMLA (eutectic mixture of LA) 2.5% lignocaine and 2.5% prilocaine that takes 60 minutes for effect (maximal 2–3 hours) and lasts for 1–2 hours after removal. Eutectic means a mixture with a melting point lower than either component alone; being partly solidified makes it more convenient for topical application. Use of an occlusive dressing over a generous application improves absorption; it is a vasoconstrictor.
Assessment of toxic metal ions in tea samples using new microextraction technique based on the solidified deep eutectic solvent followed by GFAAS
Published in Toxin Reviews, 2021
Toraj Ahmadi-Jouibari, Negar Noori, Nazir Fattahi
Currently, cheap, affordable, and green extractants, called deep eutectic solvents (DESs), are being used as an alternative to ionic liquids and conventional organic solvents to extract trace amounts of organic and inorganic analytes (Bajkacz and Adamek 2018, Liu et al.2018, Malaeke et al.2018). DESs consist of two or three components that offer several environmental and economic advantages. These components form eutectic mixture having lowest melting point than each individual components and have the maximum capability to bound them self through hydrogen bonding (Rykowska et al.2018). DESs are formed mostly with the complexation of choline chloride with an inexpensive and nontoxic hydrogen bond donor or metal salts, such as urea, glycerol, carboxylic acid, sugar, etc. DESs not only have the advantages of low volatility, low vapor pressure, high thermal stability, and high ability to extract organic and inorganic compounds, but also have low cost and easy preparation of nontoxic compounds. Choline based DESs also overcome the health and safety challenges toward human and eco-toxicity issues.
Topical anesthetic and pain relief using penetration enhancer and transcriptional transactivator peptide multi-decorated nanostructured lipid carriers
Published in Drug Delivery, 2021
Tao Jiang, Shuangshuang Ma, Yangyang Shen, Yuwen Li, Ruirui Pan, Huaixin Xing
Nanoparticles (NPs) utilized for TDDS include polymeric NPs, liposomes, solid lipid nanoparticles (SLN), and nanostructured lipid carriers (NLC) (Franz-Montan et al., 2017). NLC, as the second generation of SLN, consist of a mixture of solid and liquid lipids (Müller et al., 2011). The inner matrix of NLC decides its advantages over SLN such as more drug loading and physicochemical stability. NLC has been successfully used for targeting drugs by TDDS. In the field of topical anesthesia, the most desirable marketed formulation is the eutectic mixture of lidocaine and prilocaine (EMLA® Cream, AstraZeneca). However, its clinical application is limited because of the low anesthesia pain effect (Franz-Montan et al., 2008). Therefore, we designed multi-functionalized NLC to expect to achieve some breakthrough progress.
Deep eutectic solvents comprising active pharmaceutical ingredients in the development of drug delivery systems
Published in Expert Opinion on Drug Delivery, 2019
Sónia N. Pedro, Mara G. Freire, Carmen S. R. Freire, Armando J. D. Silvestre
One of the oldest eutectic mixtures known is the anesthetic cream EMLA® (Eutectic Mixture of Local Anaesthetic; melting temperature = 16°C) used in transdermal delivery, composed of prilocaine (melting temperature = 38°C) and lidocaine (melting temperature = 68ºC) [49]. This eutectic mixture represents a landmark in drugs’ solubilization enhancement strategies, and this was the first eutectic mixtures to be patented and commercialized [50]. However, EMLA®’s adverse side effects, mainly attributable to prilocaine, led to the creation of other dual function eutectic mixtures, such as lidocaine:procaine and lidocaine:tetracaine. The lidocaine:tetracaine mixture is also liquid at room temperature, presenting a melting temperature similar to lidocaine:prilocaine (ca. 18°C) [51]. More recently, the creation of a remarkable dual function API-DES based on ibuprofen and lidocaine was reported [17]. Moreover, in vivo tests indicated that the anesthetic effect of lidocaine in this eutectic mixtures is faster and stronger when compared with the commercial EMLA® and the lidocaine:tetracaine mixture, having a pharmacological effect in 10 min vs. 1 h and 30 min, respectively.