RESUMEN
BACKGROUND AND PURPOSE: The essential oil derived from clove buds (Syzygium aromaticum) has been used as a chemopreventive agent in Ayurvedic medicine. The antiviral, antibacterial, and anticancer properties of its chemo-skeleton have motivated this study to explore its efficacy in pharmaceutics. METHODS: Nanoscale-based emulsions were prepared by employing a spontaneous emulsification technique through self-assembly using varying concentrations of Tween 20 and Tween 80 surfactants. Their physicochemical properties and stability were studied in order to choose an optimum formulation which was clear and stable. The cytotoxicity of the stable oil-based emulsion system was evaluated using MTT assay, colony formation assay, and Annexin V-FITC assay against the thyroid cancer cell line (HTh-7). RESULTS: All three methods verified apoptosis and reduction in cancer cell proliferation, making the formulation a promising candidate as an alternative cancer drug. The oil-based emulsion system was also tested for its antibacterial properties against Staphylococcus aureus. Membrane permeability studies proved its efficacy to permeate through cell membrane, thereby increasing the leakage of cytoplasmic contents. CONCLUSION: Many current treatments for cancers are aggressive yet ineffective. This study positions the clove bud-based nanoscale emulsion as a suitable candidate for further in vivo studies and trials as a cancer drug.
Asunto(s)
Antibacterianos/farmacología , Antineoplásicos/farmacología , Aceites Volátiles/farmacología , Syzygium/química , Línea Celular Tumoral , Permeabilidad de la Membrana Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Composición de Medicamentos , Emulsiones , Humanos , Concentración de Iones de Hidrógeno , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/química , Staphylococcus aureus/efectos de los fármacos , Tensoactivos/química , ViscosidadRESUMEN
The plant derived essential oil nanoemulsion was prepared using a mixture of components containing eucalyptus oil as organic phase, water as continuous phase, and non ionic surfactant, Tween 80, as emulsifier at a particular proportion of 1:1 v/v%. The ultrasonication was applied for varied processing time from 0 to 30 min to study the effect of time on the formation of nanoemulsion and physical stability of formulation by this method. The transparency and stability of emulsion was enhanced when the sonication time was increased compared to hand blender emulsion. The most stable nanoemulsion was obtained in 30 min sonication having the mean droplet diameter of 3.8 nm. The antibacterial studies of nanoemulsion against Staphylococcus aureus by time kill analysis showed complete loss of viability within 15 min of interaction. Observations from scanning electron microscopy of treated bacterial cells confirmed the membrane damage compared to control bacteria. Furthermore, the wound healing potential and skin irritation activity of the formulated nanoemulsion in Wistar rats, suggested non-irritant and higher wound contraction rate with respect to control and neomycin treated rats. These results proposed that the formulated system could be favourable for topical application in pharmaceutical industries.
Asunto(s)
Eucalyptus/química , Nanoestructuras , Aceites de Plantas/química , Aceites de Plantas/farmacología , Staphylococcus aureus/efectos de los fármacos , Ultrasonido , Cicatrización de Heridas/efectos de los fármacos , Animales , Antibacterianos/efectos adversos , Antibacterianos/química , Antibacterianos/farmacología , Membrana Celular/efectos de los fármacos , Emulsiones , Masculino , Aceites de Plantas/efectos adversos , Ratas , Ratas Wistar , Piel/citología , Piel/efectos de los fármacos , Staphylococcus aureus/citología , Factores de TiempoRESUMEN
Candida albicans is a common fungal pathogen that causes systemic and superficial infections in most immunocompromised patients. Fluconazole, a synthetic triazole antifungal agent, is the most prescribed drug used in treating this pathogen. But because of its poor solubilization in water and the emergence of resistant strains against this antimycotic drug, we aimed at devising a unique microemulsion drug delivery system for fluconazole against candidiasis. A clear oil-in-water microemulsion system, consisting of clove oil as oil phase, Tween 20 as surfactant, and water as aqueous phase was developed using a ternary phase diagram. Physicochemical characterization was done to understand the internal physicochemical state. The bulk drug, fluconazole, that measured several microns in length was reduced to a 10-65 nm range with no means of high-energy methods as confirmed by transmission electron microscopy. The very small and uniform spherical structure of the drug-loaded microemulsion system could be of high impact to the biological system as the efficacy of fluconazole is greatly improved when compared with its conventional bulk form. The optimized microemulsion exhibited significantly higher antifungal activity at a minimum concentration (8 µg/ml) of fluconazole as examined by fluorescence and scanning electron microscopy. Thus, our report discloses an excellent oral drug delivery system.