The objective of this work was to characterize the toxicological profile of a newly developed sunscreen formulation based on polymeric nanocapsules (NCs) loading benzophenone-3 (BZP3). NCs composed of poly(ε-caprolactone) carrot oil and Pluronic® F68 were produced by emulsification-diffusion method. Their mean particle size (Z-Ave) ranged from 280 to 420 nm, polydispersity index (PDI) was below 0.37, while zeta potential (ZP) reached about |+11 mV|. No cytotoxic effects were observed in L929 fibroblast cell line for the blank (i.e., non-loaded) NCs and BZP3-loaded NCs (BZP3-NCs). The semi-solid sunscreen formulation was stable over time (centrifugation testing) and exhibited non-Newtonian pseudoplastic behavior, which is typical of products for topical application onto the skin. The sun protection factor (SPF) value reached 8.84, when incorporating BZP3-NCs (SPF of 8.64) into the semi-solid formulation. A synergistic effect was also observed when combining the formulation ingredients of nanocapsules, i.e., SPF of carrot oil was 6.82, blank NCs was 6.84, and BZP3-loaded NCs was 8.64. From the hen’s egg-chorioallantoic membrane test (HET-CAM) test, the non-irritation profile of the developed formulations could also be confirmed. The obtained results show a promising use of poly(ε-caprolactone) nanocapsules to be loaded with lipophilic sunscreens as benzophenone-3.
RESUMO Hiperidrose é a produção excessiva de suor pelo corpo, podendo ser primária ou secundária e generalizada ou localizada. As regiões craniofacial, axilar, palmar, dorso, face interna das coxas, plantar são comumente afetadas. A hiperidrose primária (HP), embora seja uma doença benigna, apresenta um eminente impacto negativo na qualidade de vida do paciente. Essa doença é classificada quantitativamente de acordo com a Escala de Gravidade da Doença da Hiperidrose, com base em como ela pode afetar as atividades diárias, podendo ser de leve a grave intensidade. Os acadêmicos de medicina enfrentam situações desgastantes físicas e emocionais durante seus afazeres e, quando portadores de doenças crônicas como a HP, podem ser estigmatizados como inseguros na sua profissão. Objetivou-se definir a prevalência, os critérios diagnósticos, a gravidade e o impacto na qualidade de vida que a HP proporciona nos âmbitos profissional e extracurricular dos acadêmicos de medicina. Trata-se de um estudo transversal de abordagem quantitativa de caráter descritivo, que inclui 300 acadêmicos do curso de Medicina da Universidade Tiradentes, em Aracaju/SE, no período de agosto a novembro de 2017. Utilizaram-se frequências absolutas e relativas no caso de variáveis categóricas e medidas de tendência e variabilidade central no caso de variáveis numéricas. O valor de p < 0,05 foi considerado significativo. A prevalência de HP em estudantes de medicina foi de 18% sem diferença entre os sexos e com predomínios das cores branca e parda. A doença ocorreu principalmente em sítios combinados, como palmoplantar, sendo a região palmar a mais acometida. Os sintomas iniciaram-se, principalmente, durante a infância e adolescência, com prejuízo importante nas atividades diárias pessoais e laborativas, e exacerbação do suor com situações de estresse. A gravidade da HP mais encontrada foi a moderada, sendo o impacto negativo na qualidade de vida principalmente relatado nos graus mais avançados da doença, dificultando as atividades acadêmicas. É importante a inclusão do conhecimento da HP no currículo médico para uma maior divulgação da doença, de modo a permitir um diagnóstico precoce e relacionado à intensidade da sudorese na sua abordagem terapêutica.
Nanomedicine manipulates materials at atomic, molecular, and supramolecular scale, with at least one dimension within the nanometer range, for biomedical applications. The resulting nanoparticles have been consistently shown beneficial effects for antifungal drugs delivery, overcoming the problems of low bioavailability and high toxicity of these drugs. Due to their unique features, namely the small mean particle size, nanoparticles contribute to the enhanced drug absorption and uptake by the target cells, potentiating the therapeutic drug effect. The topical route is desirable due to the adverse effects arising from oral administration. This review provides a comprehensive analysis of the use of nano compounds for the current treatment of topical fungal infections. A special emphasis is given to the employment of lipid nanoparticles, due to their recognized efficacy, versatility and biocompatibility, attracting the major attention as novel topical nanocompounds used for the administration of antifungal drugs.
The low solubility and high volatility of perillyl alcohol (POH) compromise its bioavailability and potential use as chemotherapeutic drug. In this work, we have evaluated the anticancer activity of POH complexed with β-cyclodextrin (β-CD) using three complexation approaches. Molecular docking suggests the hydrogen-bond between POH and β-cyclodextrin in molar proportion was 1:1. Thermal analysis and Fourier-transform infrared spectroscopy (FTIR) confirmed that the POH was enclosed in the β-CD cavity. Also, there was a significant reduction of particle size thereof, indicating a modification of the β-cyclodextrin crystals. The complexes were tested against human L929 fibroblasts after 24 h of incubation showing no signs of cytotoxicity. Concerning the histopathological results, the treatment with POH/β-CD at a dose of 50 mg/kg promoted approximately 60% inhibition of tumor growth in a sarcoma S180-induced mice model and the reduction of nuclear immunoexpression of the Ki67 antigen compared to the control group. Obtained data suggest a significant reduction of cycling cells and tumor proliferation. Our results confirm that complexation of POH/β-CD not only solves the problem related to the volatility of the monoterpene but also increases its efficiency as an antitumor agent.
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