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Bismuth lipophilic nanoparticles (BisBAL NPs) and cetylpyridinium chloride (CPC) are antineoplastic and antimicrobial in vitro. As a next pre-clinical step, a clinically viable dosage form for vaginal application was developed. Compendial pharmacopeial tests (mass uniformity, disintegration, and compressive mechanics) and inductively coupled plasma optical emission spectroscopy were conducted on in-house developed glycerinated gelatin (60:15 v/w) vaginal ovules containing BisBAL NP-CPC. The antimycotic activity of BisBAL NP-CPC vaginal ovules was analyzed using disk diffusion and cell viability XTT assays. The antitumor properties of BisBAL NP-CPC vaginal ovules were assessed by cell viability MTT tests. BisBAL NP-CPC and drug-free vaginal ovules deposited into ex vivo porcine vaginas disaggregated without signs of adverse cytotoxicity within the timespan of clinical efficacy. BisBAL NP-CPC vaginal ovules demonstrated antifungal efficacy comparable to miconazole: C. albicans growth inhibition haloes in diffusion tests were 23 ± 0.968 mm (n = 3) for BisBAL NP-CPC and 20.35 ± 0.899 mm (n = 3) for miconazole. Likewise, BisBAL NP-CPC vaginal ovules reduced HeLa cell growth by 81%, outperforming the clinical reference of 500 µM 5-fluouracil, which induced a 70% growth inhibition. BisBAL NP-CPC incorporated into glycerinated gelatin vaginal ovules constitute an innovative drug delivery system for topical antimycotic and anti-cervical carcinoma treatments.

RESUMO

The oral cavity is an ecosystem that provides ideal conditions for the growth of bacteria, the Streptococcus genus is important for the formation of biofilms that lead to the development of dental caries, which affects the population worldwide. The world health organization encourages the use of plants thanks to its various therapeutic actions. Origanum vulgare L. (oregano), is an aromatic plant with medicinal and culinary properties. The objective of this study was to investigate the in vitro antimicrobial and antibiofilm activity of the ethanolic extract of oregano, against the growth of Streptococcus mutans and Streptococcus sobrinus ATCC. Leaves of the plant were obtained and the ethanolic extract was made by maceration. Antimicrobial activity was evaluated using the Kirby-Bauer method and compared with 2% chlorhexidine, subsequently the extract was incorporated into a hydrogel and its effect on biofilm formation was assessed by fluorescence microscopy and the main compounds were identified. present in the extratco. The study revealed that the extract presented antimicrobial effect against both strains and at 2% it showed high antimicrobial action compared to chlorhexidine at the same concentration, with average inhibition halos of 26.3 mm and 19 mm for each microorganism analyzed, (p < 0.05). Likewise, the hydrogel prepared with 2% extract significantly eliminated the preformed Streptococcus biofilm, at 24 hours of exposure, due to the presence of a variety of chemical groups, such as sterols, triterpenes, flavonoids, flavanones, flavanonol s, lactones. sesquiterpenic, tannins and coumarins. The oregano extract presented high antimicrobial action for both species, with a greater effect towards Streptococcus mutans and an interesting antibiofilm action; These results show the importance of exploring treatment alternatives of plant origin, to be considered as interesting complementary aids in dental therapy.

La cavidad oral es un ecosistema que proporciona condiciones ideales para el crecimiento de bacterias, el género Streptococcus es importante para la formación de biopelículas que conducen al desarrollo de caries dental, que afecta a la población a nivel mundial. La organización mundial de la salud, fomenta el uso de plantas gracias a sus diversas acciones terapéuticas. Origanum vulgare L. (orégano), es una planta aromática con propiedades medicinales y culinarias. El objetivo de este estudio fue investigar la actividad antimicrobiana y antibiofilm in vitro del extracto etanólico de oregano, contra el crecimiento de Streptococcus mutans y Streptococcus sobrinus ATCC. Se obtuvierón hojas de la planta y se realizó el extracto etanólico mediante maceración. La actividad antimicrobiana se evaluó mediante el método de Kirby-Bauer y se comparó con la clorhexidina al 2 %, posteriormente se incorporó el extracto en un hydrogel y se valoró su efecto sobre la formación del biofilm mediante microscopía de fluorescencia y se identificó los principales compuestos presentes en el extratco. El estudio reveló que el extracto presentó efecto antimicrobiano contra ambas cepas y al 2 % mostró alta acción antimicrobiana en comparación con la clorhexidina a la misma concentración, con halos de inhibición promedio de 26.3 mm y de 19 mm para cada microorganismo analizado, (p < 0.05). Así mismo, el hidrogel preparado con extracto al 2 %, eliminó significativamente la biopelícula preformada de Streptococcus, a las 24 horas de exposición, debido a la presencia de una variedad de grupos químicos, como esteroles, triterpenos, flavonoides, flavanonas, flavanonoles, lactonas sesquiterpénicas, taninos y cumarinas. El extracto de orégano presentó alta acción antimicrobiana para ambas especies, con mayor efecto hacia el Streptococcus mutans y una acción antibiofilm interesante; estos resultados muestran la importancia de explorar en alternativas de tratamiento de origen vegetal, para considerarse como auxiliares complementarios interesantes en la terapia dental.

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Multiresistance among microorganisms to common antimicrobials has become one of the most significant concerns in modern medicine. Nanomaterials are a new alternative to successfully treat the multiresistant microorganisms. Nanostructured materials are used in many fields, including biological sciences and medicine. Recently, it was demonstrated that the bactericidal activity of zero-valent bismuth colloidal nanoparticles inhibited the growth of Streptococcus mutans; however the antimycotic potential of bismuth nanostructured derivatives has not yet been studied. The main objective of this investigation was to analyze the fungicidal activity of bismuth oxide nanoparticles against Candida albicans, and their antibiofilm capabilities. Our results showed that aqueous colloidal bismuth oxide nanoparticles displayed antimicrobial activity against C. albicans growth (reducing colony size by 85%) and a complete inhibition of biofilm formation. These results are better than those obtained with chlorhexidine, nystatin, and terbinafine, the most effective oral antiseptic and commercial antifungal agents. In this work, we also compared the antimycotic activities of bulk bismuth oxide and bismuth nitrate, the precursor metallic salt. These results suggest that bismuth oxide colloidal nanoparticles could be a very interesting candidate as a fungicidal agent to be incorporated into an oral antiseptic. Additionally, we determined the minimum inhibitory concentration for the synthesized aqueous colloidal Bi2O3 nanoparticles.

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BACKGROUND AND METHODS: Despite continuous efforts, the increasing prevalence of resistance among pathogenic bacteria to common antibiotics has become one of the most significant concerns in modern medicine. Nanostructured materials are used in many fields, including biological sciences and medicine. While some bismuth derivatives has been used in medicine to treat vomiting, nausea, diarrhea, and stomach pain, the biocidal activity of zerovalent bismuth nanoparticles has not yet been studied. The objective of this investigation was to analyze the antimicrobial activity of bismuth nanoparticles against oral bacteria and their antibiofilm capabilities. RESULTS: Our results showed that stable colloidal bismuth nanoparticles had 69% antimicrobial activity against Streptococcus mutans growth and achieved complete inhibition of biofilm formation. These results are similar to those obtained with chlorhexidine, the most commonly used oral antiseptic agent. The minimal inhibitory concentration of bismuth nanoparticles that interfered with S. mutans growth was 0.5 mM. CONCLUSION: These results suggest that zerovalent bismuth nanoparticles could be an interesting antimicrobial agent to be incorporated into an oral antiseptic preparation.

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