The poor solubility of itraconazole (ITZ) has limited its efficacy in the treatment of vaginal candidiasis. Accordingly, the improvement of ITZ solubility using a solid dispersion technique was important to enhance its antifungal activity. Besides, as the purpose of this research was to develop local-targeting formulations, bioadhesivethermosensitive in situ vaginal gel combined with the gel-flake system was found to be the most suitable choice. To obtain optimum solubility, entrapment efficiency, and drug-loading capacity, optimization of solid dispersion (SD) and gel-flake formulations of ITZ was performed using a composite central design. The results showed that the optimized formulation of SD-ITZ was able to significantly enhance its solubility in both water and simulated vaginal fluid to reach the values of 4.211 ± 0.23 and 4.291 ± 0.21 mg/mL, respectively. Additionally, the optimized formulation of SD-ITZ gel flakes possessed desirable entrapment efficiency and drug-loading capacity. The in situ vaginal gel containing SD-ITZ gel flakes was prepared using PF-127 and PF-68, as the gelling agents, with the addition of hydroxypropyl methylcellulose (HPMC) as the mucoadhesive polymer. It was found that the obtained in situ vaginal gel provided desirable physicochemical properties and was able to retain an amount of more than 4 mg of ITZ in the vaginal tissue after 8 h. Importantly, according to the in vivo antifungal activity using infection animal models, the incorporation of the solid dispersion technique and gelflake system in the formulation of the bioadhesive-thermosensitive in situ vaginal gel led to the most significant decrease of the growth of Candida albicans reaching <1 log colony-forming units (CFU)/mL or equivalent to <10% of the total colony after 14 days, indicating the improvement of ITZ antifungal activity compared to other treated groups. Therefore, these studies confirmed a great potential to enhance the efficacy of ITZ in treating vaginal candidiasis. Following these findings, several further experiments need to be performed to ensure acceptability and usability before the research reaches the clinical stage.
As one of vegetable plants in South Sulawesi, cabbage (Brassica oleracea L.) crops has generated cellulose fibers biomass which is potentially modified into nano-crystalline cellulose, a valuable material in the pharmaceutical formula. Therefore, this study aims to manipulate the natural cellulose fibers of cabbage biomass through acid hydrolysis method within product preliminary evaluation through FT-IR and XRD. The fibers were modified through the bleaching process produce micro crystalline cellulose, which was then hydrolyzed with 65% sulfuric acid to obtain nanocrystalline cellulose. The products have yellow pale to brown colour, with a yield of 10.06% and 31.16% respectively. Based on FT-IR spectra, both products inherit cellulose characteristics, C-O (1232.16 cm-1); C = O (1743.65 cm-1); -OH (1625.99 cm-1); C-H (2920.23 cm-1); O-H (3414 cm-1). The increasing trend of crystallinity index during the process was also observed in XRD diffractogram. It is identifiable from 7.41% for natural fiber, 69.68% for crystalline microcrystalline, and 78.01% for nano crystalline cellulose. Through Match®, the estimated crystalline product size reaches 58.91 nm.
Tea (Camellia sinensis L.) has an activity as an antibacterial, widely studied to plankton cells, without further researching into biofilm cell. Therefore, this research had been conducted to initially evaluate the activity of green- and black-tea extracts in inhibiting Streptococcus mutans biofilm. Green and black tea leaves were extracted using 70% methanol. Determination of MIC was subsequently performed by microdilution method. Next, the biofilm formation and inhibition were run through microtiter plate method using flexible U-bottom PVC 96 wells, which then observed using microplate reader on λ = 515 nm. As The results, MIC for green and black tea extract stood at 4 mg/mL, 6 mg/mL respectively. The biofilm inhibitory activity of black tea extract was at 8 and 10 mg/mL inhibiting 6 % and 12.5 % S. mutans. Green tea extract showed that concentration of 4 to 10 mg/mL was able to inhibit biofilm growth by 24%; 45%; 48% and 53%. Thus, through microtiter plate assay, it could be concluded that tea extract has potent antibiofilm to S. mutans, where green tea extract has better activity than black tea extract.
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