Previous experiments indicated that 1-bromopropane (1-BP), an alternative to chloroflurocarbons, is neurotoxic and inhibits spermiation in the testis. Here we investigated the reversibility of the toxic effects of 1-BP in rats. Male Wistar rats were divided into three equal groups of 24 each and exposed by inhalation to 0, 400 or 1000 ppm of 1-BP for 6 weeks (8 hrs/day, 7 days/week). Eight rats from each group were sacrificed at the end of 6 weeks exposure, and at 4 and 14 weeks after the end of exposure, to assess the recovery processes. We studied sperm count, motility, morphology and testicular histopathology, as well as blood pressure, skin temperature and hindlimb muscle strength. At the end of 6 weeks of exposure to 1000 ppm (0 week recovery), testicular weight, epididymal weight, sperm count and motility were low, morphologically abnormal sperm were increased and spermatogenic cells showed diffuse degeneration. These changes did not show full recovery at 14 weeks recovery, with the exception of the prostate and seminal vesicular weights, which recovered back to control values. At 400 ppm, increased retained spermatids at 0 week recovery returned to normal at 4 weeks recovery. Exposure to 1000 ppm produced sustained reduction of hindlimb muscle strength at 14 weeks recovery, whereas normalization of the skin temperature and blood pressure was noted after transient changes. Our study showed that the effect of 1-BP on spermatogenesis is dose-dependent; low exposure inhibited spermiation and hormone-dependent organ weight reduction and these changes were transient, while a higher dose of 1000 ppm 1-BP caused persistent depletion of spermatogenic cells.
Objective: This research work aimed to develop bucco-adhesive patches, which release curcumin in the oral cavity for an extended duration thereby assisting in the cure of oral thrush (candidiasis). Fluconazole containing patches were also developed in order to compare the effectiveness of curcumin patches against Candida albicans. Method: After suitable preformulation studies, five formulations of curcumin were prepared using Eudragit S100 and polyvinyl alcohol (PVA) in varying ratios. Three batches of fluconazole formulations were prepared without PVA. Patches were evaluated for their physical properties and chemical integrity. Newer techniques were developed to determine their bioadhesion and tensile strength. Sterile formulations of P3 and F2 were prepared and compared for the antifungal activity against C. albicans, by zone of inhibition method. Results: All formulations exhibited satisfactory tensile strength ranging from 0.282 to 0.411 Kg/m2 with good folding endurance. Formulations containing higher amount of PVP exhibited better bioadhesive strength. P3 formulation containing curcumin and F2 formulation of fluconazole were found to sustain the drug release upto 5 hours. An increasing amount of PVA retarded the drug release. In antifungal studies, the zone of inhibition for P3 patches was 19mm, and for F2 patches, it was 13mm, indicating a better in vitro antifungal activity for curcumin against fluconazole. SEM analysis of P3 formulations revealed continuous, non-porous but non homogenous structure of the polymer film. Conclusion: The effectiveness of curcumin buccal patches in superior to fluconazole patches was well demonstrated. Mathematical modelling of drug release data indicated a first order anomalous transport causing the drug release. Kinetic modelling with zero, first order, Higuchi and Korsmeyer- peppas are explained in this article. Keywords: Buccal, curcumin, candidiasis, antifungal, tensile strength, drug release, korsmeyer-peppas.