Objective: Capsaicin is a bioactive compound with poor solubility in water. Transfersomes can increase the solubility and thus the penetration of capsaicin into the epidermis. Transfersomes also offer the advantage of being ultradeformable vesicles that are made using the thin layer hydration method. The aim of this study is to determine the effect of the hydrophilicity of surfactants on the characterization and in vitro penetrative ability of capsaicin transfersomes in gels using non-ionic surfactants with different hydrophile-lipophile balances, namely, Span 80, Tween 80, and a mixture of Span 80, and Tween 80. Methods:The best characterization result for transfersomes is the formula using Tween 80. The total cumulative amount of capsaicin penetrated from the transfersome gel using Tween 80 is 1663.89±1.58 mg/cm 2 , the percentage is 57.96±0.05%, and the flux is 166.38±0.15 µg/cm 2 .hr −1 . Results:In terms of the transfersome gel using a mixture of Span 80 and Tween 80, the cumulative amount of capsaicin penetrated is 1539.8±21.23 µg/cm 2 , the percentage is 54.47±0.75%, and the flux is 153.98±2.12 µg/cm 2 .hr −1 . Finally, from the transfersome gel using Span 80, the cumulative amount of capsaicin penetrated is 1395.10±7.23 mg/cm 2 , the percentage is 50.80±0.26%, and the flux is 139.51±0.72 mg/cm 2 .hr −1 . Conclusions:The best characteristics resulted from the transfersome formulation using Tween 80, which demonstrated the highest entrapment efficiency calculation result, the smallest particle size, the best deformability index, and the highest penetration when compared to the other two formulations.
Objective: Capsaicin is an active compound found in chili pepper and has been shown to have analgesic, antioxidant, anticancer, and anti-obesity properties. To improve its penetration into the skin, capsaicin was prepared in a transethosome vesicle. Importantly, transethosomes are vesicles that consist of phosphatidylcholine, surfactant, and ethanol. In this study, capsaicin was prepared in a transethosome vesicle using two different methods: Direct transethosome formation and thin layer hydration. The aims of this study were to determine the effects of various methods of transethosome formation on capsaicin characteristics and to evaluate the penetration capabilities of transethosome capsaicin gel.Methods: Ultimately, transethosome formation via the thin layer method yielded more favorable characteristics; these formations had particle sizes of 174.9±2.02 nm and an entrapment efficiency of 84.85±1.15%. The transethosome suspension was then developed into a gel formulation using 1% carbomer. An in vitro penetration test was performed using a Franz diffusion cell of mice abdomen skin, and the performance of the transethosome capsaicin gel was compared to that of the standard capsaicin gel.Results: Penetration rate of capsaicin from either the transethosome gel preparation and the standard gel substance was 1549.68±49.6 and 846.05±10.1 µg/cm 2 , respectively. Conclusions:According to these results, it can be concluded that gel preparations containing transethosome increase capsaicin penetration into the skin.
Rod-shaped nanoparticles have been identified as promising drug delivery candidates. In this report, the in vitro cell uptake and in vivo pharmacokinetic/bio-distribution behavior of molecular bottle-brush (BB) and cyclic peptide self-assembled nanotubes were studied in the size range of 36–41 nm in length. It was found that BB possessed the longest plasma circulation time ( t 1\2 > 35 h), with the cyclic peptide system displaying an intermediate half-life (14.6 h), although still substantially elevated over a non-assembling linear control (2.7 h). The covalently bound BB underwent substantial distribution into the liver, whereas the cyclic peptide nanotube was able to mostly circumvent organ accumulation, highlighting the advantage of the inherent degradability of the cyclic peptide systems through their reversible aggregation of hydrogen bonding core units.
Objective: Grape is one of the most well-known fruits. People usually consume only the fruit and the skin; however, the seed is the part of the fruit that contains important antioxidant rich polyphenol. However, grape seed and its extract have an unpleasant taste. Therefore, this study aimed to formulate effervescent tablets containing grape seed extract (GSE) to overcome the unpleasant taste.Methods: Effervescent tablets of GSE were formulated using three formulas, each with a different percentage of the effervescent mix. The tablets were prepared using wet granulation method at 40% relative humidity (RH) (the ratio of the partial pressure of water vapor to the equilibrium vapor pressure of water) and 25°C temperature. The effervescent granules and the tablets were evaluated for various characteristics in term of granules flowability, moisture content, as well as tablets appearance, size and weight uniformity, hardness, friability, effervescence time, pH, and total phenol content. In addition, all three formulations of the effervescent tablets and solutions were evaluated for appearance, taste, and flavor using the hedonic test that involved 30 panelists. Results:The evaluation of the effervescent granules and tablets showed that they had good characteristics. The disintegration time of the three formulations was within the acceptable range, between 3.67 minutes and 4.69 minutes. The pH of the effervescent solution was between 5.18 and 5.80. Based on the hedonic test, all the effervescent solutions had favorable appearance, taste, and flavor. Conclusions:Clinical Streptococcus salivarius isolates from the dorsum of the tongue had greater potential for inhibiting Enterococcus faecalis growth compared to the saliva isolates and control bacteria. Therefore, we can conclude that the effervescent tablets containing grape seed extract are potential be used as a nutraceutical dosage form.
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