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1.
Eur J Pharm Biopharm ; 170: 1-9, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34798283

RESUMO

In previous studies, lecithin-based nanoemulsions (NEs) have been shown to be skin friendly drug carrier systems. Due to their nontoxic properties, NEs might also be suitable as wound healing agents. Hence, different O/W NEs based on lecithin Lipoid® S 75 and plant oils or medium chain triglycerides were produced and characterised. Two lipophilic natural wound healing agents, a betulin-enriched extract from birch bark (BET) and a purified spruce balm (PSB), were successfully incorporated and their effects on primary human skin cells were studied in vitro. MTT, BrdU and scratch assays uncovered the positive influence of the drug-loaded NEs on cell viability, proliferation and potential wound closure. Compared to control formulations, the NEs loaded with either BET or PSB led to higher cell viability rates of fibroblasts and keratinocytes. Higher proliferative activity of keratinocytes and fibroblasts was observed after the treatment, which is a prerequisite for wound closure. Indeed, in scratch assays NEs with PSB and notably BET showed significantly ameliorated wound closure rates than the negative control (unloaded NEs) and the positive control (NEs with dexpanthenol). Our findings suggest that BET and PSB are outstanding wound healing drugs and their incorporation into lecithin-based NEs may represent a valid strategy for wound care.


Assuntos
Lecitinas/farmacologia , Óleos de Plantas/farmacologia , Pele/citologia , Pele/efeitos dos fármacos , Triglicerídeos/farmacologia , Cicatrização/efeitos dos fármacos , Betula , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Emulsões , Humanos , Técnicas In Vitro , Picea , Triterpenos/farmacologia
2.
Pharmaceutics ; 13(4)2021 Mar 24.
Artigo em Inglês | MEDLINE | ID: mdl-33804924

RESUMO

(1) Background: The aim of the study was to evaluate the effect of pure lecithins in comparison to a conventional surfactant on skin in vivo. (2) Methods: Physiological skin parameters were evaluated at the beginning and the end of the study (day 1 and day 4) (n = 8, healthy forearm skin) with an Aquaflux®, skin-pH-Meter, Corneometer® and an Epsilon® sensor. Confocal Raman spectroscopy was employed to monitor natural moisturizing factor, urea and water content of the participants' skin. Tape strips of treated skin sites were taken and the collected corneocytes were subjected to atomic force microscopy. Circular nano objects were counted, and dermal texture indices were determined. (3) Results: Transepidermal water loss was increased, and skin hydration was decreased after treatment with SDS and LPC80. Natural moisturizing factor and urea concentrations within the outermost 10 µm of the stratum corneum were lower than after treatment with S75 or water. Dermal texture indices of skin treated with SDS were higher than skin treated with water (control). (4) Conclusions: Results suggest very good (S75) or good (LPC80) skin-tolerability of lecithin-based surfactants in comparison to SDS and encourage further investigation.

3.
Int J Pharm ; 580: 119209, 2020 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-32165223

RESUMO

Surfactants are important ingredients in pharmaceutical and cosmetic formulations, as in creams, shampoos or shower gels. As conventional emulsifiers such as sodium dodecyl sulfate (SDS) have fallen into disrepute due to their skin irritation potential, the naturally occurring lecithins are being investigated as a potential alternative. Thus, lecithin-based nanoemulsions with and without the drug curcumin, known for its wound healing properties, were produced and characterised in terms of their particle size, polydispersity index (PDI) and zeta potential and compared to SDS-based formulations. In vitro toxicity of the produced blank nanoemulsions was assessed with primary human keratinocytes and fibroblasts using two different cell viability assays (BrdU and EZ4U). Further, we investigated the penetration profiles of the deployed surfactants and oil components using combined ATR-FTIR/tape stripping experiments and confirmed the ability of the lecithin-based nanoemulsions to deliver curcumin into the stratum corneum in tape stripping-UV/Vis experiments. All manufactured nanoemulsions showed droplet sizes under 250 nm with satisfying PDI and zeta potential values. Viability assays with human skin cells clearly indicated that lecithin-based nanoemulsions were superior to SDS-based formulations. ATR-FTIR tests showed that lecithin and oil components remained in the superficial layers of the stratum corneum, suggesting a low risk for skin irritation. Ex vivo tape stripping experiments revealed that the kind of oil used in the nanoemulsion seemed to influence the depth of curcumin penetration into the stratum corneum.


Assuntos
Bromodesoxiuridina/metabolismo , Curcumina/metabolismo , Sistemas de Liberação de Medicamentos/métodos , Lecitinas/metabolismo , Absorção Cutânea/fisiologia , Tensoativos/metabolismo , Adulto , Idoso , Animais , Bromodesoxiuridina/administração & dosagem , Bromodesoxiuridina/química , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/fisiologia , Curcumina/administração & dosagem , Curcumina/química , Citotoxinas/administração & dosagem , Citotoxinas/química , Citotoxinas/metabolismo , Emulsões/administração & dosagem , Emulsões/química , Emulsões/metabolismo , Feminino , Aromatizantes/administração & dosagem , Aromatizantes/química , Aromatizantes/metabolismo , Humanos , Lecitinas/administração & dosagem , Lecitinas/química , Masculino , Pessoa de Meia-Idade , Nanopartículas/administração & dosagem , Nanopartículas/química , Nanopartículas/metabolismo , Absorção Cutânea/efeitos dos fármacos , Tensoativos/administração & dosagem , Tensoativos/química , Suínos , Fatores de Tempo , Adulto Jovem
4.
Int J Pharm ; 566: 383-390, 2019 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-31158455

RESUMO

As constituents of cellular membranes, lecithins feature high biocompatibility and great emulsifying properties due to their amphiphilicity. Additionally, there are expectations that these naturally occurring emulsifying agents can replace other skin damaging emulsifiers like sodium dodecyl sulfate or sodium laureth sulfate. However, cytotoxicity data of lecithin-based formulations on primary human skin cells are scarce. Thus, we developed nanoemulsions with different kinds of surfactants (amphoteric, anionic and non-ionic), studied the skin permeation of a model drug from this formulations employing Franz-type diffusion cells and monitored their cytotoxicity potential on primary human keratinocytes and fibroblasts using a cell proliferation assay. The skin diffusion studies demonstrated that the amphoteric lecithin-based emulsifiers were superior to non-ionic surfactants in terms of skin permeation, but inferior to anionic emulsifiers. Further, we found that the nanoemulsions containing the amphoteric lecithins as emulsifying agents lead to significantly higher viability rates of both epidermal keratinocytes and dermal fibroblasts than the investigated anionic and non-ionic surfactants. This renders them a promising alternative to conventional emulsifiers used in daily products.


Assuntos
Emulsificantes/administração & dosagem , Fibroblastos/efeitos dos fármacos , Queratinócitos/efeitos dos fármacos , Lecitinas/administração & dosagem , Nanopartículas/administração & dosagem , Pele/metabolismo , Adulto , Idoso , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Emulsões , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Pele/citologia , Absorção Cutânea , Suínos , Adulto Jovem
5.
BMC Infect Dis ; 9: 216, 2009 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-20043842

RESUMO

BACKGROUND: Tuberculosis is one of the most prominent health problems in the world, causing 1.75 million deaths each year. Rapid clinical diagnosis is important in patients who have co-morbidities such as Human Immunodeficiency Virus (HIV) infection. Direct microscopy has low sensitivity and culture takes 3 to 6 weeks 123. Therefore, new tools for TB diagnosis are necessary, especially in health settings with a high prevalence of HIV/TB co-infection. METHODS: In a public reference TB/HIV hospital in Brazil, we compared the cost-effectiveness of diagnostic strategies for diagnosis of pulmonary TB: Acid fast bacilli smear microscopy by Ziehl-Neelsen staining (AFB smear) plus culture and AFB smear plus colorimetric test (PCR dot-blot).From May 2003 to May 2004, sputum was collected consecutively from PTB suspects attending the Parthenon Reference Hospital. Sputum samples were examined by AFB smear, culture, and PCR dot-blot. The gold standard was a positive culture combined with the definition of clinical PTB. Cost analysis included health services and patient costs. RESULTS: The AFB smear plus PCR dot-blot require the lowest laboratory investment for equipment (US$ 20,000). The total screening costs are 3.8 times for AFB smear plus culture versus for AFB smear plus PCR dot blot costs (US$ 5,635,760 versus US$ 1,498, 660). Costs per correctly diagnosed case were US$ 50,773 and US$ 13,749 for AFB smear plus culture and AFB smear plus PCR dot-blot, respectively. AFB smear plus PCR dot-blot was more cost-effective than AFB smear plus culture, when the cost of treating all correctly diagnosed cases was considered. The cost of returning patients, which are not treated due to a negative result, to the health service, was higher in AFB smear plus culture than for AFB smear plus PCR dot-blot, US$ 374,778,045 and US$ 110,849,055, respectively. CONCLUSION: AFB smear associated with PCR dot-blot associated has the potential to be a cost-effective tool in the fight against PTB for patients attended in the TB/HIV reference hospital.


Assuntos
Mycobacterium tuberculosis/isolamento & purificação , Reação em Cadeia da Polimerase/economia , Tuberculose Pulmonar/diagnóstico , Tuberculose Pulmonar/economia , Brasil , Infecções por HIV/complicações , Humanos , Mycobacterium tuberculosis/genética , Reação em Cadeia da Polimerase/métodos , Escarro/microbiologia , Tuberculose Pulmonar/etiologia , Tuberculose Pulmonar/microbiologia
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