Mucoadhesive assessment of different antifungal nanoformulations.

Oral candidiasis is an important opportunistic fungal infection and polyenes and azoles are still the most used antifungal agents. However, the oral absorption resulting from most available treatments is generally poor and, consequently, a very high frequency of administrations of antifungal agents is strongly required. Therefore, the major challenge is to improve the retention of the antifungal agents in buccal mucosa, and the encapsulation into mucoadhesive systems may be considered as a possible strategy to achieve this objective. Three types of mucoadhesive polymeric nanoparticles (polylactic acid (PLA), polylactic-co-glycolic acid (PLGA) and alginate) were prepared using nystatin as model drug. The drug-loaded nanoparticles were then included in toothpaste, oral gel and oral films, respectively. The results demonstrated that the loaded nanoparticles were successfully produced, presenting a mean size between 300-900 nm and with a negative surface charge. Also, the determination of the encapsulation efficiency of all nanoparticles showed values above 70%. In terms of the in vitro mucoadhesion, the best formulation was the oral film loaded with the PLGA nanoparticles followed by the oral gel with PLA nanoparticles and thirdly the toothpaste with alginate nanoparticles. This was confirmed in an in vitro rinsing model with mucus producing HT29-MTX cells, where the percentage of nystatin retained to the cells after 40 min of simulated saliva flow was between 10-27% when formulations were used and only 4% for free nystatin. Further studies will include in vivo testing using animal models.

Integrated approach in the assessment of skin compatibility of cosmetic formulations with green coffee oil.

OBJECTIVE: Green coffee oil (GCO) has been used in cosmetic formulations due to its emollient and anti-ageing properties. However, there are insufficient studies about its safety when applied in cosmetic formulations. METHODS: Cytotoxicity of GCO and of formulations containing 2.5-15% of GCO was evaluated by the MTT reduction assay, in human keratinocytes. Formulations containing 15% of GCO and the vehicle were applied under in use conditions in the volar forearm of human volunteers during 3 days. Transepidermal water loss, stratum corneum water content and erythema index were evaluated each 24 h using biophysical techniques. The same formulations were probed for skin tolerance through a patch test. RESULTS: Neither pure GCO nor its formulations showed cytotoxic effects in concentrations up to 100 µg mL(-1) . Transepidermal water loss values showed a slight reduction when the formulation containing GCO was applied. Stratum corneum water content and erythema index did not show significant differences, as the results observed in the first day of the study were maintained throughout 3 days. None of the volunteers display any reaction after using an occlusive patch. CONCLUSION: The results obtained in the study indicate that GCO seems to be safe for topical applications and showed good skin compatibility under the experimental conditions of the study.

Abietanes from Plectranthus grandidentatus and P. hereroensis against methicillin- and vancomycin-resistant bacteria.

The antimicrobial activity of 10 natural abietanes isolated from Plectranthus grandidentatus and P. hereroensis acetonic extract was evaluated against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecalis (VRE). The results revealed that the most active diterpenes were coleon U (1), 7alpha-acetoxy-6beta-hydroxyroyleanone (2) and horminone (3). Minimum inhibitory concentration (MIC) values ranging 0.98-15.63 microg/ml were obtained for MRSA clinical strains, and MIC values of 15.63 and 31.25 microg/ml were obtained for VRE clinical strains. Some structure-activity relationships are emphasized.