Enhanced transdermal permeation and anti-inflammatory potential of phospholipids complex-loaded matrix film of umbelliferone: Formulation development, physico-chemical and functional characterization

Telange, Darshan R.; Nirgulkar, Shivendra B.; Umekar, Milind J.; Patil, Arun T.; Pethe, Anil M.; Bali, Nikhil

doi:10.1016/j.ejps.2019.02.006

Cited by 44 publications

(16 citation statements)

References 56 publications

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“…Pure analytical umbelliferone (purity > 99%) purchased from Sigma-Aldrich was used to prepare the stock solution. Umbelliferone has a molecular mass of 162.1 and reported p K a and aqueous solubility values of about 7.5 and 620 mg L −1 , respectively 43,44 .…”

Section: Methodsmentioning

confidence: 99%

Sorption, persistence, and leaching of the allelochemical umbelliferone in soils treated with nanoengineered sorbents

Real

Gámiz

López-Cabeza

et al. 2019

Sci Rep

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Coumarins represent an important family of allelochemicals with fungicidal, bactericidal, insecticidal, nematicidal, and herbicidal properties. Like for other allelochemicals, the short persistence of coumarins in soils can reduce their biological activity and hamper their application as environmentally friendly agrochemicals. We evaluated the sorption of the coumarin umbelliferone by eight soils and six sorbent materials, and then selected two nanoengineered sorbents, hexadecyltrimethylammonium-modified Arizona montmorillonite (SA-HDTMA) and olive-mill waste biochar (BC), to assess the effect of their addition to two distinct soils on umbelliferone sorption, persistence, and leaching. Umbelliferone was sorbed to a greater extent by the acid soils (A1-A2, K d > 4.0 L kg −1 ) than by the alkaline soils (B1-B6, K d < 0.5 L kg −1 ). The addition of BC and SA-HDTMA at a rate of 4% to alkaline soil (B2) increased the umbelliferone sorption K d value from 0.3 to 1.6–2.0 L kg −1 , whereas their addition to acid soil (A1) increased the K d value from 4.6 to 12.2–19.0 L kg −1 . Incubation experiments showed that BC had more impact than SA-HDTMA on the persistence of umbelliferone in the soils, increasing its half-life from 0.3-2.5 to 1.2–14.4 days, depending on the soil. Furthermore, the addition of BC to the top 0–5 cm of soil columns reduced leaching of umbelliferone and led to accumulation of umbelliferone residues in the top 0–5 cm soil layer. The addition of nanoengineered materials, such as organoclays and biochars, could thus be a suitable strategy to increase the persistence and reduce the mobility of coumarins in the rhizosphere with the aim of prolonging their biological activity.

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Section: Methodsmentioning

confidence: 99%

Sorption, persistence, and leaching of the allelochemical umbelliferone in soils treated with nanoengineered sorbents

Real

Gámiz

López-Cabeza

et al. 2019

Sci Rep

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“…The bioactive compound could enhance the expression of pro-inflammatory molecules, including IL-6, and iNOS in simulated THP-1 monocytes with heat-killed methicillin-resistant S. aureus [32]. In addition, the efficiency of a phospholipid, a natural ingredient in liposomes, has been previously shown to maintain moisturize effect on the skin [33] as well as act as an anti-inflammatory agent [34]. The liposome formulation contains some fatty acids that provide skin hydration, resulting in enhanced efficacy of acne treatment in volunteers.…”

Section: Resultsmentioning

confidence: 99%

Rhodomyrtone as a New Natural Antibiotic Isolated from Rhodomyrtus tomentosa Leaf Extract: A Clinical Application in the Management of Acne Vulgaris

et al. 2021

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Rhodomyrtone, a plant-derived principal compound isolated from Rhodomyrtus tomentosa (Myrtaceae) leaf extract, was assessed as a potential natural alternative for the treatment of acne vulgaris. The clinical efficacy of a 1% liposomal encapsulated rhodomyrtone serum was compared with a marketed 1% clindamycin gel. In a randomized and double-blind controlled clinical trial, 60 volunteers with mild to moderate acne severity were assigned to two groups: rhodomyrtone serum and clindamycin gel. The volunteers were instructed to apply the samples to acne lesions on their faces twice daily. A significant reduction in the total numbers of acne lesions was demonstrated in both treatment groups between week 2 and 8 (p < 0.05). Significant differences in acne numbers compared with the baseline were evidenced at week 2 onwards (p < 0.05). At the end of the clinical trial, the total inflamed acne counts in the 1% rhodomyrtone serum group were significantly reduced by 36.36%, comparable to 34.70% in the clindamycin-treated group (p < 0.05). Furthermore, a commercial prototype was developed, and a clinical assessment of 45 volunteers was performed. After application of the commercial prototype for 1 week, 68.89% and 28.89% of volunteers demonstrated complete and improved inflammatory acne, respectively. All of the subjects presented no signs of irritation or side effects during the treatment. Most of the volunteers (71.11%) indicated that they were very satisfied. Rhodomyrtone serum was demonstrated to be effective and safe for the treatment of inflammatory acne lesions.

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“…The time till the patch detached from the skin sample was recorded and considered as the adhesive time. Results were given as means ± SDs (n = 3) [20]. This study was approved by the Animal Ethical Committee (Reference# AR/PG/2016/02RE), Research Unit, Dubai Pharmacy College for Girls, Dubai, UAE.…”

Section: Moisture Contentmentioning

confidence: 99%

The Optimization of a Dimenhydrinate Transdermal Patch Formulation Based on the Quantitative Analysis of In Vitro Release Data by DDSolver through Skin Penetration Studies

2021

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Dimenhydrinate is an over-the-counter medication that is used to relieve nausea, vomiting, and vertigo caused by motion sickness. It has a short elimination half-life, possibly due to its first-pass metabolism. The current study aimed to prepare and evaluate new transdermal formulations of dimenhydrinate to prolong the drug’s release and improve its cutaneous permeation. First, the patches were fabricated and evaluated to determine their properties. The results were statistically investigated and considered significant at the p < 0.05 level. Additionally, the quantitative analysis of the drug-release data and kinetic modeling was performed by using the DDSolver software to decide the candidate formula dependably. The effect of the penetration enhancers on the permeability of dimenhydrinate from the selected patch was then studied ex vivo compared to the control sample, and the patch’s safety was evaluated in rabbits, using the skin-irritation test.

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Enhanced transdermal permeation and anti-inflammatory potential of phospholipids complex-loaded matrix film of umbelliferone: Formulation development, physico-chemical and functional characterization

Cited by 44 publications

References 56 publications

Sorption, persistence, and leaching of the allelochemical umbelliferone in soils treated with nanoengineered sorbents

Sorption, persistence, and leaching of the allelochemical umbelliferone in soils treated with nanoengineered sorbents

Rhodomyrtone as a New Natural Antibiotic Isolated from Rhodomyrtus tomentosa Leaf Extract: A Clinical Application in the Management of Acne Vulgaris

The Optimization of a Dimenhydrinate Transdermal Patch Formulation Based on the Quantitative Analysis of In Vitro Release Data by DDSolver through Skin Penetration Studies

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