Gel-based Microemulsion Design and Evaluation for Topical Application of Rivastigmine

2020 ◽  
Vol 21 (4) ◽  
pp. 298-304
Author(s):  
Chih-Wen Fang ◽  
Ling-Chun Tsai ◽  
Yaw-Syan Fu ◽  
Ting-Yu Cheng ◽  
Pao-Chu Wu
Keyword(s):  
Topical Application ◽  
Skin Irritation ◽  
Topical Administration ◽  
Lag Time ◽  
Enhancement Effect ◽  
Microemulsion Formulation ◽  
Rat Skin ◽  
Glycol Monobutyl Ether ◽  
Loading Amount ◽  
Hydrophilic Gel

Objective: The aim of the present study was to design nanocarriers for the topical application of rivastigmine. Methods: The effect of cosurfactants, hydrophilic gel and loading amount on the permeability of rivastigmine through rat skin was evaluated. Skin irritation tests and stability tests were performed to evaluate the utility of tested formulations. Results: The results showed that the microemulsion formation and characteristics of drug-loaded formulations were related to many parameters of the components. When using microemulsion systems as a vehicle, the permeation rate remarkably increased about 13.2~24.3-fold and the lag time was significantly shortened from 24 h to 4.7 h. Formulations containing a cosurfactant of Diethylene Glycol Monobutyl Ether (DEGBE) showed higher enhancement effect, while increasing the loading dose from 0.5% to 5% further increased the flux about 2.1-fold and shortened the lag time. Conclusion: The drug-loaded experimental formulation did not cause skin irritation and had good stability at 20ºC and 40ºC storage for at least 3 months. The result showed that gel-based microemulsion formulation could be a promising approach for topical administration.

scholarly journals Formulation of meloxicam gel for topical application: In vitro and in vivo evaluation

2010 ◽  
Vol 60 (2) ◽  
pp. 153-163 ◽  
Author(s):  
Yogeshwar Bachhav ◽  
Vandana Patravale
Keyword(s):  
Topical Application ◽  
Skin Irritation ◽  
Inflammatory Activity ◽  
Rat Skin ◽  
In Vivo Evaluation ◽  
Topical Gel ◽  
Skin Delivery ◽  
Anti Inflammatory

Formulation of meloxicam gel for topical application: In vitro and in vivo evaluation Skin delivery of NSAIDs offers several advantages over the oral route associated with potential side effects. In the present investigation, topical gel of meloxicam (MLX) was formulated using N-methyl pyrrolidone (NMP) as a solubilizer and Carbopol Ultrez 10® as a gelling polymer. MLX gel was evaluated with respect to different physicochemical parameters such as pH, viscosity and spreadability. Irritation potential of MLX gel was studied on rabbits. Permeation of MLX gel was studied using freshly excised rat skin as a membrane. Anti-inflammatory activity of MLX gel was studied in rats and compared with the commercial formulation of piroxicam (Pirox® gel, 0.5% m/m). Accelerated stability studies were carried out for MLX gel for 6 months according to ICH guidelines. MLX gel was devoid of any skin irritation in rabbits. After 12 h, cumulative permeation of MLX through excised rat skin was 3.0 ± 1.2 mg cm-2 with the corresponding flux value of 0.24 ± 0.09 mg cm-2 h-1. MLX gel exhibited significantly higher anti-inflammatory activity in rats compared to Pirox® gel. Physicochemically stable and non-irritant MLX gel was formulated which could deliver significant amounts of active substance across the skin in vitro and in vivo to elicit the anti-inflammatory activity.

scholarly journals The metabolic transformations of columbinic acid and the effect of topical application of the major metabolites on rat skin.

1985 ◽  
Vol 260 (2) ◽  
pp. 987-992
Author(s):  
W J Elliott ◽  
A R Morrison ◽  
H W Sprecher ◽  
P Needleman
Keyword(s):  
Topical Application ◽  
Rat Skin

In vivo distribution of linoleic acid in hairless rat skin following topical administration

1986 ◽  
Vol 278 (6) ◽  
pp. 503-506 ◽  
Author(s):  
R. Roguet ◽  
C. Lotte ◽  
C. Berrebi ◽  
D. Rouers ◽  
D. Dupuis ◽  
...  
Keyword(s):  
Linoleic Acid ◽  
Topical Administration ◽  
Rat Skin ◽  
In Vivo Distribution

2 Final Report on the Safety Assessment of p-Aminophenol, m-Aminophenol, and o-Aminophenol

1988 ◽  
Vol 7 (3) ◽  
pp. 279-333 ◽  
Keyword(s):  
Topical Application ◽  
Guinea Pigs ◽  
Safety Assessment ◽  
Mutagenic Activity ◽  
Skin Irritation ◽  
Final Report ◽  
Hair Dyes ◽  
Hair Dye ◽  
Mutagenicity Tests

p-Aminophenol (PAP), m-Aminophenol (MAP), and o-Aminophenol (OAP) are used in permanent (oxidative) hair dyes at concentrations from 0.1 to 5%. In vivo and in vitro skin absorption studies indicated that 11% of the dermally applied 14C-PAP was detected in the excreta, viscera, and skin of the test animals. The oral LD50s of PAP, MAP, and OAP in rats ranged from 600 to 1300 mg/kg. Topical application of PAP at concentrations up to 8.00 g/kg to the skin of New Zealand white (NZW) rabbits produced no skin irritation and no mortality. PAP, MAP, and OAP were irritating to eyes of NZW rabbits at a concentration of 2.5%. MAP at 3% was nonsensitizing in guinea pigs; PAP at 2% sensitized 9 of 10 guinea pigs. Neither PAP nor MAP produced photosensitization in guinea pigs. No treatment-related toxicity was found in three separate four-generation chronic dermal toxicity and reproduction studies of hair dye formulations containing the three Aminophenols. Additional studies on the pure ingredients were also nonteratogenic; embryotoxicity was reported. A range of results was obtained from studies assessing the mutagenic activity of the Aminophenols. PAP tested positive in six of eight mutagenicity tests. MAP and OAP gave positive results in two of eight and five of seven mutagenicity tests, respectively. Oxidative hair dye formulations containing PAP, MAP, and OAP did not produce gross or microscopic alterations or have carcinogenic effects after chronic topical application to mice. Feeding of OAP-HCl and PAP to rats at a dose of 8 mmol/kg produced neither hepatic cirrhosis nor neoplastic lesions. A 3% solution of MAP in an aqueous vehicle was neither a significant irritant nor sensitizer in two clinical studies. A variety of epidemiological studies have not indicated that occupational exposure to, and personal use of, hair dyes containing the Aminophenols presented a carcinogenic risk. A discussion of the significance of the mutagenic data in the safety assessment and the potential for human effects is presented. On the basis of the available animal and clinical data presented in this report it is concluded that p-, m-, and o-Aminophenols are safe as cosmetic ingredients in the present practices of use and concentrations.

scholarly journals Effects of Flavonoids from French Marigold (Florets ofTagetes patulaL.) on Acute Inflammation Model

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Ken Yasukawa ◽  
Yoshimasa Kasahara
Keyword(s):  
Arachidonic Acid ◽  
Oral Administration ◽  
Topical Application ◽  
Acute Inflammation ◽  
Topical Administration ◽  
Tagetes Patula ◽  
Paw Edema ◽  
Ear Edema ◽  
Inflammation Model ◽  
Anti Inflammatory

The major components patuletin and patulitrin were isolated from French marigold (florets ofTagetes patula). Patuletin and patulitrin were found to inhibit acute inflammation in mice. Oral administration of patuletin and patulitrin significantly suppressed hind-paw edema induced by carrageenin and histamine, while topical application of patuletin and patulitrin significantly inhibited ear edema induced by 12-O-tetradecanoylphorbol-13-acetate and arachidonic acid. Thus, oral and topical administration of patuletin and patulitrin inhibited acute inflammation in mice. These results suggest the anti-inflammatory efficacy of French marigold.

Evaluation of percutaneous absorption and skin irritation of ketoprofen through rat skin: in vitro and in vivo study

2001 ◽  
Vol 222 (2) ◽  
pp. 225-235 ◽  
Author(s):  
Pao-Chu Wu ◽  
Jin-Sheng Chang ◽  
Yaw-Bin Huang ◽  
Chee-Yin Chai ◽  
Yi-Hung Tsai
Keyword(s):  
Percutaneous Absorption ◽  
Skin Irritation ◽  
In Vivo Study ◽  
Rat Skin
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