Onychomycosis is the most common infection of nails caused majorly by Trichophyton rubrum and Trichophyton mentagrophytes and minorly by yeasts. Topical delivery of available ciclopirox formulations as nail lacquer, cream, lotion, gel is hindered by the low permeability of human nail plates, and so there is need of repeated dosing for a longer period of time for effective treatment. In the present research work an attempt is made for effective delivery of ciclopirox olamine (CIC) across human nail plates by enahancing the penetration of CIC and retention time in skin layers. For this purpose nanoemulsion gel, composed of oil, surfactant, cosurfactant, and cabopol was developed by aqueous phase titration method and was evaluated for various in-vitro attributes. Oleic acid, tween 80, and PEG 400 were selected as oil, surfactant and co-surfactant respectively. Pseudoternary phase diagrams were plotted to get the range of nanoemulsion area. For the optimization of the formulation Box Benkhem model (RSM) was applied by taking size and zeta potential as dependant variables and formulation components were taken as independent variables. Total 17 formulations were suggested by the model, which were formulated and subjected to thermodynamic 2 stability study and permeation study. Among thermodynamically stable formulation, SF4 had shown lowest permeation across skin (56.672 µg/cm /h). SF4 formulation was further evaluated for skin retention study by fluorescent microscopy. Fluorescence microscopy studies were done over a period of 6 hrs clearly giving an indication of longer retention capability of the nano-gel formulation, for the desired topical action.
Objective: Periodontitis is an oral disease categorized by disturbance of periodontal tissue and creation of periodontal pockets. Thymol (TH) loaded microsponge in situ gelling system was formulated for local action in the periodontal cavity for the management of periodontitis. Method: Solvent evaporation technique was utilized for preparation of microsponges. A Fractional factorial design (FFD) was used to screen the high risk variables impacting the characteristics of the (TH) microsponges and further optimized using Box-Behnken design. The optimized microsponges were then characterized by DSC, SEM, antimicrobial activity, in– vitro release and then incorporated in the in situ gelling system. Ligature model was used to induce periodontitis in Sprague Dawley rats. Results: The microsponges showed good characteristics such as particle size, entrapment efficiency and mucoadhesiveness 45 µm, 92.99±0.2%, 96±0.26% respectively. SEM revealed the spherical morphology of the microsponges with sustained release of TH for 10h and antimicrobial activity against S.mutans and C.albicans. Treatment with thymol loaded in situ gel (THLMG) showed decrease in gingival inflammation and tooth mobility as well as in serum biochemical parameters like serum C-reactive proteins, leucocyte count, alkaline phosphatase and tartrate-resistant acid phosphatase when compared to disease group. The histopathological study of the periodontium confirmed significant reduction of inflammation and alveolar bone destruction (p<0.05) in rats. Conclusion: Thus THLMG decreased infiltration of inflammatory cells and prevented osteoclatogenesis and osteoblast apoptosis which further favored decrease in inflammation and alveolar bone loss in periodontitis. Thus THLMG could be a better alternative to synthetic antimicrobials and antibiotics to treat periodontitis.
Objective: The objective of the study was to investigate the solubilization of poorly water-soluble drug Lamotrigine in pure & mixed Pluronic polymeric micelles. Method: Two different Pluronic (Pluronic F68, Pluronic L81) were chosen and micelle formulations were prepared by using various drug:polymer ratios and model drug Lamotrigine. Formulations were characterized by critical micellization concentration (CMC) values, cloud point of copolymers, micelle size and size distribution, zeta potential, loading efficiency ,drug release and stability. Result: Mixed micelles(hydrophilic and hydrophobic) also helped to overcome the limitations of monosystem of Pluronic L81 and Pluronic F68. The solubilized drug and salt decreased the cloud point of copolymers. Results show that the solubilization of Lamotrigine enhances with the rise in concentration of block copolymers, negative Gs0 and temperature, but no significant increase was observed with added salt and at a lower pH the drug show highest solubility. Conclusion: Mixed micelles showed fairly high entrapment efficiency, loading capacity and sustained release profile for Lamotrigine, a model hydrophobe than that of plain Pluronic micelles.
D oxazosin mesylate has some of the ideal characteristics required for an orally disintegrating tablet. There were some challenges faced during this formulation development. The aims of the present research were to mask the bitter taste of Doxazosin mesylate and to formulate orally disintegrating tablets of taste masked drug. Taste masking was performed by coating Doxazosin Mesylate with suitable polymer Eudragit powdered E-100 using spray drying technique. The resultant microspheres were then evaluated for thermal analysis, yield, particle size, entrapment efficiency and in vitro taste masking. The tablets were formulated by mixing the taste masked microspheres with different types and concentration of super-disintegrants and granulated Mannitol was selected as diluent and compressed using direct compression method. The tablets prepared were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in vitro disintegration time and in vitro drug release and compared with marketed IR tablet of Doxazosin mesylate.
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