Transdermal Permeation of Kaempferia parviflora Methoxyflavones from Isopropyl Myristate-Based Vehicles

Abstract

Kaempferia parviflora (K. parviflora) rhizomes have long been used in traditional folk medicines and as general health-promoting agents. Several biological activities of K. parviflora, especially its antiinflammatory effect, are due to its major constituents, methoxyflavones. However, the oral bioavailability of these methoxyflavones has been shown to be low. The aim of this study was to investigate the permeation behaviors of K. parviflora methoxyflavones from isopropyl myristate (IPM)-based vehicles. We studied the effects of ethanol and propylene glycol (PG) as the hydrophilic, solvent-type vehicles as well as fatty acids as the permeation enhancers. A permeation experiment was performed in vitro, using side-by-side diffusion cells through the full thickness of pig ear skin. The solubility and permeation of methoxyflavones were able to be modified by choice and ratio of vehicles. The ethanol/IPM vehicle was shown to be more effective in enhancing the solubility and permeation of methoxyflavones when compared to the PG/IPM vehicle. Regarding an optimal balance between solubility or affinity to vehicle and skin to vehicle partition coefficient, the ethanol/IPM vehicle in the ratio of 1:9 maximized the flux. Among the investigated fatty acids, oleic acid showed the greatest enhancing effect on the permeation of methoxyflavones, indicating that saturated fatty acids are less effective than unsaturated fatty acids. Long chain fatty acids increased diffusion coefficient parameter and shortened the lag time. The number of carbon atoms and double bonds of fatty acids did not show direct relation to the profile of permeation of methoxyflavones.

Optimization of Ultrasound-Assisted Extraction of Yields and Total Methoxyflavone Contents from Kaempferia parviflora Rhizomes

“…Under the aforementioned HPLC conditions, the respective compounds (PMF, DMF, and TMF) were clearly separated and eluted at retention times of 16 min, 19 min, and 21 min, respectively, as illustrated in Figure 1. The developed method revealed sharp symmetrical peaks, whereas the earlier study revealed broad asymmetries [15]. For the developed HPLC-DAD method, a highly accurate and precise separation of marker components was achieved.…”

GC-MS Profiling, in vitro Antioxidant and Antimicrobial Activities of Kaempferia parviflora Wall. ex. Baker Rhizome Extract

“…Furthermore, high-performance liquid chromatography (HPLC) analysis of methoxyflavones in Kaempferia parviflora ethanolic extract revealed 5,7,4ʹ trimethoxyflavone, 5,7 dimethoxyflavone, and 3,5,7,3ʹ,4ʹ pentamethoxyflavone as major components. 36,37 However, to the best of our knowledge, there are no reports on the putative identification of phytoconstituents present in the chloroform extract of Kaempferia parviflora Wall ex Baker rhizome and its evaluation for antioxidant/ antimicrobial/antifungal activities. In general, dissolution of bioactive compounds present in the plant sample is higher with higher polarity of the solvent and thus plant extracts prepared using polar solvents like water, and ethanol contain generally a large number of bioactive compounds with close retention factor (Rf) values.…”

Selective Cytotoxicity of Kaempferia parviflora Extracts in Human Cell Lines

“…Considering its low oral bioavailability of 1 to 4% reported in rats, toxic dose of KP extract in endothelial cells can be very difficult to identify (Mekjaruskul et al, 2012). However, current pharmaceutical studies have been trying to improve the dissolution rate, drug permeability and bioavailability of methoxyflavones in KP (Mekjaruskul et al, 2013;Tuntiyasawasdikul et al, 2014;Chairuk et al, 2020).…”