Therapeutic deep eutectic system of capric acid and menthol: Characterization and pharmaceutical application

Al-Akayleh, Faisal; Ali, Hiba Hani Mohammed; Ghareeb, Mowafaq M.; Al-Remawi, Mayyas

doi:10.1016/j.jddst.2019.101159

Cited by 50 publications

(32 citation statements)

References 47 publications

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“…DES have been mainly studied as vehicles for topical applications. In vivo studies on albino rabbits have confirmed that topical application of DES, such as capric acid-menthol, do not cause skin irritation [94]. The use of these systems for the solubilization of fluconazole and mometasone, antifungal and anti-allergic drugs, respectively, and their formulation and application as a topical cream has been studied as well [94].…”

Section: Des In Drug Delivery Systemsmentioning

confidence: 99%

“…In vivo studies on albino rabbits have confirmed that topical application of DES, such as capric acid-menthol, do not cause skin irritation [94]. The use of these systems for the solubilization of fluconazole and mometasone, antifungal and anti-allergic drugs, respectively, and their formulation and application as a topical cream has been studied as well [94]. It was found that the drug, the DES and cream components do not cause skin edema or inflammation after topical application.…”

Section: Des In Drug Delivery Systemsmentioning

confidence: 99%

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Deep Eutectic Solvents and Pharmaceuticals

et al. 2021

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Deep eutectic solvents (DES) are eutectic mixtures that present a deviation from the ideal thermodynamic solid–liquid phase behavior, where a significant depression in the melting temperature occurs. If properly designed and chosen, DES may be liquid at room and the human body’s temperatures and display a biocompatible character, thus representing relevant options in the pharmaceutical field. Accordingly, DES have been studied as alternative solvents or in formulations of pharmaceuticals to improve their solubility and stability. Depending on the DES components, these mixtures might exhibit interesting biological activities compatible with several applications. The use of DES as functional agents or as novel liquid forms of active pharmaceutical ingredients (API-DES) with the goal of improving bioavailability, permeability and therapeutic efficacy of a given API stands as alternative strategies in the pharmaceutical field for drug delivery purposes.

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Section: Des In Drug Delivery Systemsmentioning

confidence: 99%

Section: Des In Drug Delivery Systemsmentioning

confidence: 99%

Deep Eutectic Solvents and Pharmaceuticals

et al. 2021

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“…Hydrogen bond has been formed between the drugs by menthol and capric acid. (Al-Akayleh et al, 2019). THEDES system is the most simple and effective way to improve the bioavailability of APIs by altering the state from solid to liquid.…”

Section: Application Of Eutectic Systemmentioning

confidence: 99%

A brief review on eutectic mixture and its role in pharmaceutical field

Balakrishnan¹,

Jawahar²,

Senthil³

et al. 2020

ijrps

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Eutectic mixture (EM) is as a mixture of more than one substance that does not interact individually to create a new entity but in a particular ratio that exhibits a lower range of melting point than it had in individual. EM should be formulated in such a way that it should have major advantages in pharmaceutical industries. EM can be a mixture of Active Pharmaceutical Ingredients (APIs), or different ratios of APIs and excipients, or various excipients. Deep eutectic solvents containing APIs (API-DES) considered as an innovative approach to form different APIs in the liquid state. This new approach of liquid form is versatile and plays an important role in drug delivery. The selection of ideal hydrogen bond-donor (HBD) and hydrogen bond-acceptor (HBA) is an essential parameter. Ionic liquids (IL), derivatives of deep eutectic solvents (DES) have got much attention since it can replace harmful organic solvent by their extraordinary properties. Therapeutic deep eutectic solvents (THEDESs) are considered to be an exceptional option in the advancement of biomedicine. This can be utilized for improvising drug solubility, bioavailability as well as drug permeation through the skin. Natural deep eutectic solvent (NADES) can be considered as an alternate option, replacing harsh solvents. It has special characteristics of better biodegradability and biocompatibility. These NADES mainly used to separate and purification of natural compounds. This review focuses on the eutectic mixture and its application in the area of drug delivery systems, and pharmaceutical and pharmacological fields.

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“…Most of the active pharmaceutical ingredients (APIs) may act as HBDs or HBAs and can, therefore, be used as DES phase–forming. In this case, they are called Therapeutic Deep Eutectic Systems (THEDES), and in their constitution, one or both constituents are pharmaceutical relevant molecules [ 1 , 2 , 5 , 18 , 19 , 20 ]. THEDES can be obtained by combining the API with a variety of compounds depending on the aim, for example, metabolites [ 21 ] or permeation enhancers [ 13 , 22 ].…”

Section: Introductionmentioning

confidence: 99%

Solids Turn into Liquids—Liquid Eutectic Systems of Pharmaceutics to Improve Drug Solubility

et al. 2022

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The low solubility of active pharmaceutical ingredients (APIs) is a problem in pharmaceutical development. Several methodologies can be used to improve API solubility, including the use of eutectic systems in which one of the constituents is the API. This class of compounds is commonly called Therapeutic Deep Eutectic Systems (THEDES). THEDES has been gaining attention due to their properties such as non−toxicity, biodegradability, and being non−expensive and easy to prepare. Since the knowledge of the solid liquid diagram of the mixture and the ideal eutectic point is necessary to ascertain if a mixture is a deep eutectic or just a eutectic mixture that is liquid at ambient temperature, the systems studied in this work are called Therapeutic Liquid Eutectic Systems (THELES). Therefore, the strategy proposed in this work is to improve the solubility of chlorpropamide and tolbutamide by preparing THELES. Both APIs are sulfonylurea compounds used for the treatment of type 2 diabetes mellitus and have low solubility in water. To prepare the THELES, several coformers were tested, namely, tromethamine, L(+)−arginine, L−tryptophan, citric acid, malic acid, ascorbic acid, and p−aminobenzoic acid, in molar ratios of 1:1 and 1:2. To improve viscosity, water was added in different molar ratios to all systems. THELES were characterized by mid−infrared spectroscopy (MIR), and differential scanning calorimetry. Their viscosity, solubility, and permeability were also determined. Their stability at room temperature and 40 °C was accessed by MIR. Cytocompatibility was performed by metabolic activity and cell lysis evaluation, according to ISO10993−5:2009, and compared with the crystalline APIs. THELES with TRIS were successfully synthesized for both APIs. Results showed an increased solubility without a decrease in the permeability of the APIs in the THELES when compared with the pure APIs. The THELES were also considered stable for 8 weeks at ambient temperature. The cells studied showed that the THELES were not toxic for the cell lines used.

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Therapeutic deep eutectic system of capric acid and menthol: Characterization and pharmaceutical application

Cited by 50 publications

References 47 publications

Deep Eutectic Solvents and Pharmaceuticals

Deep Eutectic Solvents and Pharmaceuticals

A brief review on eutectic mixture and its role in pharmaceutical field

Solids Turn into Liquids—Liquid Eutectic Systems of Pharmaceutics to Improve Drug Solubility

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