scholarly journals New Formulation and Characterization of Topical Films of Tioconazole and Evaluation of Their Antifungal Therapy

Author(s):  
Siddique Akber Ansari

Purpose: New formulation of Scleroglucan (Sclg) films loaded with tioconazole, a medication typically applied for dermal treatments prepared. The feasibility of that treatment relies on                      the penetration of medications through the target layers of the skin in effective                 concentrations. Methods: Dynamic and mechanical characterization and swelling studies of the novel delivery system were analysed. An aqueous solution of Sclg (Cp=1% w/v) and glycerol (2% w/v) was prepared and kept at room temperature under magnetic stirring for 72 hrs. Tioconazole previously solubilised in Labrasol, was added to the polymer/glycerol solution.  4 ml of solution was poured in a plastic plate. The films were dried at 40°C for 1 hr and then allowed to dry at room temperature (about 25°C) for a week. Translucent films were obtained. The fungal strain used to test the film are CO23 sensitive to drugs, CO23 RFLC resistant to fluconazole, CO23 RFK resistant to  micafungin, ATCC  standard strain. Results: The water uptake of the films significantly increased up to 24 hrs. The optical microscope films images show that the presence of the drug did not significantly influence the appearance of the samples. The in vitro studies demonstrated the perceptible fungal activity of the new formulation against Candida albicans infections. Conclusion: The patches showed antimicrobial activity against all tested strains. An evident inhibition zone diameter, about 40 mm, for the strains sensitive to azoles (CO23 RFK and CO23) in comparison to strain resistant to fluconazole (CO23 RFLC) was observed. After 48 hours the inhibition zone diameters were reduced of about 6-7 mm in comparison to those observed after 24 hours of incubation.

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4488
Author(s):  
Aboagye Kwarteng Dofuor ◽  
Temitayo Samson Ademolue ◽  
Cynthia Mmalebna Amisigo ◽  
Kwaku Kyeremeh ◽  
Theresa Manful Gwira

The search for novel antitrypanosomals and the investigation into their mode of action remain crucial due to the toxicity and resistance of commercially available antitrypanosomal drugs. In this study, two novel antitrypanosomals, tortodofuordioxamide (compound 2) and tortodofuorpyramide (compound 3), were chemically derived from the natural N-alkylamide tortozanthoxylamide (compound 1) through structural modification. The chemical structures of these compounds were confirmed through spectrometric and spectroscopic analysis, and their in vitro efficacy and possible mechanisms of action were, subsequently, investigated in Trypanosoma brucei (T. brucei), one of the causative species of African trypanosomiasis (AT). The novel compounds 2 and 3 displayed significant antitrypanosomal potencies in terms of half-maximal effective concentrations (EC50) and selectivity indices (SI) (compound 1, EC50 = 7.3 μM, SI = 29.5; compound 2, EC50 = 3.2 μM, SI = 91.3; compound 3, EC50 = 4.5 μM, SI = 69.9). Microscopic analysis indicated that at the EC50 values, the compounds resulted in the coiling and clumping of parasite subpopulations without significantly affecting the normal ratio of nuclei to kinetoplasts. In contrast to the animal antitrypanosomal drug diminazene, compounds 1, 2 and 3 exhibited antioxidant absorbance properties comparable to the standard antioxidant Trolox (Trolox, 0.11 A; diminazene, 0.50 A; compound 1, 0.10 A; compound 2, 0.09 A; compound 3, 0.11 A). The analysis of growth kinetics suggested that the compounds exhibited a relatively gradual but consistent growth inhibition of T. brucei at different concentrations. The results suggest that further pharmacological optimization of compounds 2 and 3 may facilitate their development into novel AT chemotherapy.


2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Angela Tino ◽  
Alfredo Ambrosone ◽  
Lucia Mattera ◽  
Valentina Marchesano ◽  
Andrei Susha ◽  
...  

In the emerging area of nanotechnology, a key issue is related to the potential impacts of the novel nanomaterials on the environment and human health, so that this technology can be used with minimal risk. Specifically designed to combine on a single structure multipurpose tags and properties, smart nanomaterials need a comprehensive characterization of both chemicophysical properties and adequate toxicological evaluation, which is a challenging endeavour; thein vitrotoxicity assays that are often employed for nanotoxicity assessments do not accurately predictin vivoresponse. To overcome these limitations and to evaluate toxicity characteristics of cadmium telluride quantum dots in relation to surface coatings, we have employed the freshwater polypHydra vulgarisas a model system. We assessedin vivoacute and sublethal toxicity by scoring for alteration of morphological traits, population growth rates, and influence on the regenerative capabilities providing new investigation clues for nanotoxicology purposes.


2011 ◽  
Vol 44 (9) ◽  
pp. 1678-1683 ◽  
Author(s):  
Sagar Umale ◽  
Simon Chatelin ◽  
Nicolas Bourdet ◽  
Caroline Deck ◽  
Michele Diana ◽  
...  

2008 ◽  
Vol 71 (12) ◽  
pp. 610-618
Author(s):  
Hsiang-Ning Luk ◽  
Chu-Pin Lo ◽  
Hui-Chun Tien ◽  
Daniel Lee ◽  
Zong-Li Chen ◽  
...  

2005 ◽  
Vol 498-499 ◽  
pp. 488-493
Author(s):  
Antonio Eduardo Martinelli ◽  
D.M.A. Melo ◽  
E.P. Marinho ◽  
T.W.J. Batista ◽  
R.G.S. Araújo ◽  
...  

Geopolymers are inorganic materials with ceramic characteristics that can be synthesized at room temperature from the setting of slurries. Their structure consists of aluminosilicate units that polymerize in alkaline environment. The setting rate and mechanical behavior of geopolymers strongly depends on the SiO2:Al2O3 molar ratio, polymeric precursor and polymerization cation. The present work reports the synthesis and characterization of 3.5:1 (SiO2:Al2O3) structural geopolymers prepared using either metakaolin (GPMK) or kaolin (GPK) as geopolymeric precursor in potassium hydroxide solution. GPMK depicted quick setting whereas GPK set only after 4 hours. The rheological characterization of the slurries revealed that plastic viscosity and yield point of GPK were 0.40 Pa.s and 14.2 Pa, respectively, whereas GPMK set instantly. The compressive strength of both geopolymers were measured after 24 hours and resulted in similar results, i.e., 4.6 MPa for GPMK and 4.4 MPa for GPK. The strength of both geopolymers was compatible to values typical of structural materials.


2003 ◽  
Vol 46 (3) ◽  
pp. 359-364 ◽  
Author(s):  
Susumu KUMAGAI ◽  
Yasuhide SHINDO ◽  
Katsumi HORIGUCHI ◽  
Tomo TAKEDA

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