Honey, a concentrated natural product, is produced by honeybees (Apis mellifera) from the nectar of flowers. It contains over 200 compounds that exert various biological or pharmacological activities, ranging from antioxidant, anti-inflammatory, antimicrobial, and antihypertensive to hypoglycemic effects. Due to the presence of a plethora of bioactive compounds, as well as unique physicochemical properties, honey has been widely used as medicine throughout human history along with its extensive utilization as common food and flavoring agent. The application of neat honey for therapeutic purpose, however, poses some difficulties such as the maintenance of a required therapeutic concentration over an adequate timeframe due to the problem of liquefaction and leakage. This has driven researchers to incorporate honey into a range of formulations, for example, hydrogels, dressings, ointments, pastes, or lozenges. After a brief discussion of the chemistry and medicinal use of honey, this review focuses on commercial honey-based medicinal formulations as well as in vitro, in vivo, and clinical studies on noncommercial honey formulations for the treatment of various ailments. In addition to this, it also covers the application of honey formulations and the evidence underpinning their use.
Honey, a naturally sweet and viscous substance is mainly produced by honeybees (Apis mellifera) from flower nectar. Honey exerts a plethora of biological and pharmacological activities, namely, antioxidant, antimicrobial and anti-inflammatory activity, because of the presence of an extensive variety of bioactive compounds. The antibacterial activity is one of the most reported biological properties, with many studies demonstrating that honey is active against clinically important pathogens. As a result, beside honey’s widespread utilization as a common food and flavouring agent, honey is an attractive natural antimicrobial agent. However, the use of neat honey for therapeutic purposes poses some problems, for instance, its stickiness may hamper its appeal to consumers and health care professionals, and the maintenance of an adequate therapeutic concentration over a sufficient timeframe may be challenging due to honey liquidity and leakage. It has motivated researchers to integrate honey into diverse formulations, for example, hydrogels, dressings, ointments, pastes and lozenges. The antibacterial activity of these formulations should be scientifically determined to underscore claims of effectiveness. Some researchers have made efforts to adapt the disc carrier and suspension test to assess the antimicrobial activity of topical products (e.g., silver-based wound dressings). However, there is currently no established and validated method for determining the in vitro antimicrobial potential of natural product-based formulations, including those containing honey as the active principle. Against the backdrop of a brief discussion of the parameters that contribute to its antibacterial activity, this review provides an outline of the methods currently used for investigating the antibacterial activity of neat honey and discusses their limitations for application to honey-based formulations.
Methylglyoxal (MGO) is considered to be one of the vital components responsible for the anti-bacterial activity of Leptospermum spp. (Manuka) honey. While many studies have demonstrated a dose-dependent antibacterial activity for MGO in vitro, from a therapeutic viewpoint, it is also important to confirm its release from Manuka honey and also from Manuka honey-based formulations. This study is the first to report on the release profile of MGO from five commercial products containing Manuka honey using a Franz diffusion cell and High-Performance Liquid Chromatography (HPLC) analysis. The release of MGO expressed as percentage release of MGO content at baseline was monitored over a 12 h period and found to be 99.49 and 98.05% from an artificial honey matrix and NZ Manuka honey, respectively. For the investigated formulations, a time-dependent % MGO release between 85% and 97.18% was noted over the 12 h study period.
Honey has widespread use as a nutritional supplement and flavouring agent. Its diverse bioactivities, including antioxidant, antimicrobial, antidiabetic, anti-inflammatory, and anticancer properties, have also made it an aspirant natural product for therapeutic applications. Honey is highly viscous and very sticky, and its acceptance as a medicinal product will require formulation into products that are not only effective but also convenient for consumers to use. This study presents the design, preparation, and physicochemical characterisation of three types of alginate-based topical formulations incorporating a honey. The honeys applied were from Western Australia, comprising a Jarrah honey, two types of Manuka honeys, and a Coastal Peppermint honey. A New Zealand Manuka honey served as comparator honey. The three formulations were a pre-gel solution consisting of 2–3% (w/v) sodium alginate solution with 70% (w/v) honey, as well as a wet sheet and a dry sheet. The latter two formulations were obtained by further processing the respective pre-gel solutions. Physical properties of the different honey-loaded pre-gel solutions (i.e., pH, colour profile, moisture content, spreadability, and viscosity), wet sheets (i.e., dimension, morphology, and tensile strength) and dry sheets (i.e., dimension, morphology, tensile strength, and swelling index) were determined. High-Performance Thin-Layer Chromatography was applied to analyse selected non-sugar honey constituents to assess the impacts of formulation on the honey chemical composition. This study demonstrates that, irrespective of the honey type utilised, the developed manufacturing techniques yielded topical formulations with high honey content while preserving the integrity of the honey constituents. A storage stability study was conducted on formulations containing the WA Jarrah or Manuka 2 honey. The samples, appropriately packaged and stored over 6 months at 5, 30, and 40 °C, were shown to retain all physical characteristics with no loss of integrity of the monitored honey constituents.
This paper presents a simple and rapid approach to the quantification of various glycosides using high-performance thin-layer chromatography (HPTLC). Different classes of glycosides, represented by genistin and ononin (both monosaccharidic O-glycosides), rutin (a disaccharidic O-glycoside) and luteolin-6-C-glucoside (a monosaccharidic C-glycoside), were successfully separated using a mixture of ethyl acetate‒methanol‒glacial acetic acid‒formic acid (11:1:1:1, V/V) as the mobile phase followed by derivatisation with natural product–polyethylene glycol (NP–PEG) reagent. The method was validated for the quantification of these glycosides in accordance with the guidelines of the International Council for Harmonisation. The general applicability of the validated approach is demonstrated with the analysis of a large number of glycosides including two glycosides (i.e. rutin, naringin) in commercial products.
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