Use of 18β-glycyrrhetinic acid nanocrystals to enhance anti-inflammatory activity by improving topical delivery

2021 ◽  
pp. 111791
Author(s):  
Quan Weiyan ◽  
Kong Songzhi ◽  
Ouyang Qianqian ◽  
Tao Jinlong ◽  
Lu Sitong ◽  
...  
Keyword(s):  
Topical Delivery ◽  
Glycyrrhetinic Acid ◽  
Inflammatory Activity ◽  
Anti Inflammatory

scholarly journals Topical Delivery of Rapamycin by Means of Microenvironment-Sensitive Core-Multi-Shell Nanocarriers: Assessment of Anti-Inflammatory Activity in an ex vivo Skin/T Cell Co-Culture Model

2021 ◽  
Vol Volume 16 ◽  
pp. 7137-7151
Author(s):  
Fiorenza Rancan ◽  
Xiao Guo ◽  
Keerthana Rajes ◽  
Polytimi Sidiropoulou ◽  
Fatemeh Zabihi ◽  
...  
Keyword(s):  
T Cell ◽  
Ex Vivo ◽  
Topical Delivery ◽  
Inflammatory Activity ◽  
Culture Model ◽  
Anti Inflammatory

scholarly journals Breaking the Barrier - Potent Anti-Inflammatory Activity following Efficient Topical Delivery of Etanercept using Thermoresponsive Nanogels

Theranostics ◽  
2018 ◽  
Vol 8 (2) ◽  
pp. 450-463 ◽  
Author(s):  
M. Giulbudagian ◽  
G. Yealland ◽  
S. Hönzke ◽  
A. Edlich ◽  
B. Geisendörfer ◽  
...  
Keyword(s):  
Topical Delivery ◽  
Inflammatory Activity ◽  
Anti Inflammatory

scholarly journals Anti-Inflammatory Activity of Babassu Oil and Development of a Microemulsion System for Topical Delivery

2017 ◽  
Vol 2017 ◽  
pp. 1-14 ◽  
Author(s):  
Mysrayn Y. F. A. Reis ◽  
Simone M. dos Santos ◽  
Danielle R. Silva ◽  
Márcia V. Silva ◽  
Maria Tereza S. Correia ◽  
...  
Keyword(s):  
Topical Delivery ◽  
Oil Extraction ◽  
Inflammatory Activity ◽  
Microemulsion System ◽  
Skin Wounds ◽  
Income Source ◽  
Ear Edema ◽  
Babassu Oil ◽  
Microemulsion Droplet ◽  
Anti Inflammatory

Babassu oil extraction is the main income source in nut breakers communities in northeast of Brazil. Among these communities, babassu oil is used for cooking but also medically to treat skin wounds and inflammation, and vulvovaginitis. This study aimed to evaluate the anti-inflammatory activity of babassu oil and develop a microemulsion system with babassu oil for topical delivery. Topical anti-inflammatory activity was evaluated in mice ear edema using PMA, arachidonic acid, ethyl phenylpropiolate, phenol, and capsaicin as phlogistic agents. A microemulsion system was successfully developed using a Span® 80/Kolliphor® EL ratio of 6 : 4 as the surfactant system (S), propylene glycol and water (3 : 1) as the aqueous phase (A), and babassu oil as the oil phase (O), and analyzed through conductivity, SAXS, DSC, TEM, and rheological assays. Babassu oil and lauric acid showed anti-inflammatory activity in mice ear edema, through inhibition of eicosanoid pathway and bioactive amines. The developed formulation (39% A, 12.2% O, and 48.8% S) was classified as a bicontinuous to o/w transition microemulsion that showed a Newtonian profile. The topical anti-inflammatory activity of microemulsified babassu oil was markedly increased. A new delivery system of babassu microemulsion droplet clusters was designed to enhance the therapeutic efficacy of vegetable oil.

scholarly journals Trioxolone Methyl, a Novel Cyano Enone-Bearing 18βH-Glycyrrhetinic Acid Derivative, Ameliorates Dextran Sulphate Sodium-Induced Colitis in Mice

Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2406 ◽  
Author(s):  
Andrey V. Markov ◽  
Aleksandra V. Sen’kova ◽  
Oksana V. Salomatina ◽  
Evgeniya B. Logashenko ◽  
Dina V. Korchagina ◽  
...  
Keyword(s):  
Acid Derivative ◽  
Influenza A ◽  
In Silico Analysis ◽  
Glycyrrhetinic Acid ◽  
Inflammatory Activity ◽  
Colon Tissue ◽  
Inflammatory Infiltration ◽  
Anti Inflammatory

Semi-synthetic triterpenoids, bearing cyano enone functionality in ring A, are considered to be novel promising therapeutic agents with complex inhibitory effects on tissue damage, inflammation and tumor growth. Previously, we showed that the cyano enone-containing 18βH-glycyrrhetinic acid derivative soloxolone methyl (SM) effectively suppressed the inflammatory response of macrophages in vitro and the development of influenza A-induced pneumonia and phlogogen-stimulated paw edema in vivo. In this work, we reported the synthesis of a novel 18βH-glycyrrhetinic acid derivative trioxolone methyl (TM), bearing a 2-cyano-3-oxo-1(2)-en moiety in ring A and a 12,19-dioxo-9(11),13(18)-dien moiety in rings C, D, and E. TM exhibited a high inhibitory effect on nitric oxide (II) production by lipopolysaccharide-stimulated J774 macrophages in vitro and dextran sulfate sodium (DSS)-induced colitis in mice, displaying higher anti-inflammatory activity in comparison with SM. TM effectively suppressed the DSS-induced epithelial damage and inflammatory infiltration of colon tissue, the hyperproduction of colonic neutral mucin and TNFα and increased glutathione synthesis. Our in silico analysis showed that Akt1, STAT3 and dopamine receptor D2 can be considered as mediators of the anti-colitic activity of TM. Our findings provided valuable information for a better understanding of the anti-inflammatory activity of cyano enone-bearing triterpenoids and revealed TM as a promising anti-inflammatory candidate.

scholarly journals 18α-Glycyrrhetinic acid monoglucuronide as an anti-inflammatory agent through suppression of the NF-κB and MAPK signaling pathway

MedChemComm ◽  
2017 ◽  
Vol 8 (7) ◽  
pp. 1498-1504 ◽  
Author(s):  
Bo Li ◽  
Yongan Yang ◽  
Liuzeng Chen ◽  
Shichao Chen ◽  
Jing Zhang ◽  
...  
Keyword(s):  
Signaling Pathway ◽  
Mapk Signaling ◽  
Mapk Signaling Pathway ◽  
Glycyrrhetinic Acid ◽  
Inflammatory Activity ◽  
Inflammatory Agent ◽  
Cox 2 ◽  
Anti Inflammatory

18α-GAMG exhibited strong anti-inflammatory activity through inhibiting the expression of iNOS, COX-2, and MAPKs, as well as activation of NF-κB.

scholarly journals LORNOXICAM-LOADED NANOSPONGES FOR CONTROLLED ANTI-INFLAMMATORY EFFECT: IN VITRO/IN VIVO ASSESSMENT

2020 ◽  
pp. 217-223
Author(s):  
SEHAM M. SHAWKY ◽  
MAHA K. A. KHALIFA ◽  
HEBA A. EASSA
Keyword(s):  
Skin Permeation ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Inflammatory Activity ◽  
Carboxymethyl Cellulose Sodium ◽  
Anti Inflammatory

Objective: To design a controlled topical delivery system of lornoxicam (LX) in order to enhance skin permeation and treatment efficacy. Nanosponges were selected as a novel carrier for this purpose. Methods: Nanosponges were formulated via the emulsion solvent evaporation method using ethyl cellulose (polymer) and polyvinyl alcohol (surfactant). Nanosponge dispersions were characterized for colloidal properties, entrapment efficiency and in vitro release study. The nanosponge formulation (LS1) was then incorporated into carboxymethyl cellulose sodium hydrogels and evaluated for pH, viscosity and in vitro drug release. Skin irritation was evaluated, and anti-inflammatory activity was assessed via rat hind paw edema method. Results: Nanosponges were in the nano-sized range and attained a uniform round shape with a spongy structure. LS1exhibited the highest LX release after 6 h, so it was incorporated as hydrogel. Formulated hydrogels showed acceptable physicochemical parameters (pH, drug content and rheological properties). Skin irritation testing proved LX-loaded nanosponge hydrogel formulation (G1) to be non-irritant. In vivo study revealed an enhanced anti-inflammatory activity of G1 for 6 h (p<0.001). Conclusion: The developed nanosponge hydrogel is an efficient nanocarrier for improved and controlled topical delivery of LX.

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