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1.
Crit Rev Anal Chem ; : 1-17, 2020 Feb 16.
Artigo em Inglês | MEDLINE | ID: mdl-32064916

RESUMO

Micafungin is characterized as one of the most active available drugs for candidemia treatment; however, their use is also associated in prophylaxis protocols in cases of invasive fungal infections. The use of this drug is widely appreciated in the medical field due to be the most active echinocandin available for invasive fungal infections. In order to provide important parameters related to the chemical, physical, biological and therapeutic characteristics, this review article gathers important research results that demonstrate the biological potential of this drug, as well as to present analytical methods that can be used to determine the antifungal potential and a monitoring of administered dosages. Important studies about the methods most commonly used in biological activity evaluation and determination/quantification by analytical methods are provided in this review article. With the data provided, the scientific community will have the possibility to choose the analytical methods and biological that can be employed in clinical and scientific research to provide greater safety and reliability of the results to be found.

2.
Future Microbiol ; 15: 21-33, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32043361

RESUMO

Aim: This study aimed to evaluate the activity of 2'-hydroxychalcone-loaded in nanoemulsion (NLS + 2'chalc), the cytotoxic effect and toxicity against Paracoccidioides brasiliensis and Paracoccidioides lutzii using a zebrafish model. Materials & methods: Preparation and physical-chemical characterization of nanoemulsion (NLS) and NLS + 2'chalc were performed. MIC and minimum fungicide concentration, cytotoxicity and toxicity were also evaluated in the Danio rerio model. Results: NLS + 2'chalc showed fungicidal activity against Paracoccidioides spp. without cytotoxicity in MRC5 and HepG2 lines. It also had high selectivity index values and no toxicity in the zebrafish model based on MIC values. Conclusion: NLS + 2'chalc is a potential new alternative treatment for paracoccidioidomycosis.

3.
Curr Med Chem ; 2020 Jan 21.
Artigo em Inglês | MEDLINE | ID: mdl-31965938

RESUMO

Monoclonal antibodies carried in nanosystems have been extensively studied and reported as a promising tool for the treatment of various types of cancers. Monoclonal antibodies have great advantages for the treatment of cancer because their protein structure can bind to the target tissue; however, it has some challenges such as denaturation following heat exposure and extreme values of pH, temperature and solvents, the ability to undergo hydrolysis, oxidation and deamination and the formation of non-native aggregates, which totally compromises drug stability. In addition to these characteristics, they suffer rapid elimination when in the blood, which results in a short half-life and the production of neutralizing antibodies, rendering the doses ineffective. These challenges are overcome with encapsulation in nanosystems (liposomes, polymer nanoparticles, cyclodextrins, solid lipid nanoparticles, nanostructured lipid carriers, dendrimers and micelles) due to the characteristics of improving solubility, permeability, and selectivity only with tumor tissue; with that, there is a decrease in side effects beyond controlled release, which is critical to improving the therapeutic efficacy of cancer treatment. The article was divided into the different types of nanosystems, with a description of their definitions and applications in various types of cancers. Therefore, this review summarizes the use of monoclonal antibodies encapsulated in nanosystems and the description of clinical studies with biosimilars. Biosimilars are defined as products that are similar to monoclonal antibodies which are produced when the patent for the monoclonal antibodies expires.

4.
Mater Sci Eng C Mater Biol Appl ; 108: 110462, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31923986

RESUMO

Breast cancer is a serious public health problem that causes thousands of deaths annually. Chemotherapy continues to play a central role in the management of breast cancer but is associated with extreme off-target toxicity. Therefore, treatments that directly target the tumor and display reduced susceptibility to resistance could improve the outcome and quality of life for patients suffering from this disease. Photodynamic therapy is a targeted treatment based on the use of light to activate a photosensitizer (PS) that then interacts with molecular oxygen and other biochemical substrates to generate cytotoxic levels of Reactive Oxygen Species. Currently approved PS also tends to have poor aqueous solubility that can cause problems when delivered intravenously. In order to circumvent this limitation, in this manuscript, we evaluate the potential of a phthalocyanine-loaded nanostructured lipid carrier (NLC) functionalized with folic acid (FA). To prepare the FA labelled NLC, the polymer PF127 was first esterified with FA and emulsified with an oil phase containing polyoxyethylene 40 stearate, capric/caprylic acid triglycerides, ethoxylated hydrogenated castor oil 40 and the PS zinc phthalocyanine. The resulting PS loaded FA-NLC had a hydrodynamic diameter of 180 nm and were stable in suspension for >90 days. Interestingly, the amount of singlet oxygen generated upon light activation for the PS loaded FA-NLC was substantially higher than the free PS, yet at a lower PS concentration. The PS was released from the NLC in a sustained manner with 4.13 ±â€¯0.58% and 27.7 ±â€¯3.16% after 30 min and 7 days, respectively. Finally, cytotoxicity assays showed that NLC in the concentrations of 09.1 µM of PS present non-toxic with >80 ±â€¯6.8% viable and after 90 s of the light-exposed the results show a statistically significant decrease in cell viability (57 ±â€¯4%). The results obtained allow us to conclude that the functionalized NLC incorporated with PS associated with the PDT technique have characteristics that make them potential candidates for the alternative treatment of breast cancer.

5.
Crit Rev Anal Chem ; 50(1): 62-77, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-30810335

RESUMO

Piperine (PIP) is a natural alkaloid isolated from Piper longum L. that presents antioxidant, anticonvulsant, antimicrobial, neuroprotective, larvicidal, antiparasitic, anticancer effect and other pharmacological properties. However, the low aqueous solubility is the main barrier to its development from the laboratory to the clinic as a drug. Several strategies have been used to overcome this obstacle, like the incorporation of PIP into different drug delivery systems turned out to be highly efficient. In addition, several methods for the quantitative and qualitative analysis of PIP in various raw materials, including biological fluids (plasma, urine, metabolites, brain), plants and drug delivery systems, were investigated. Most recently high-performance liquid chromatography was used together with several detectors for this purpose. Therefore, this review presents a summary of characteristics chemical and biological properties of PIP as well as several techniques and analytical methods to optimize the analytical signal, increase sensitivity, selectivity and reduce the effects of interference for this drug.


Assuntos
Alcaloides/análise , Benzodioxóis/análise , Portadores de Fármacos/química , Piperidinas/análise , Alcamidas Poli-Insaturadas/análise , Disponibilidade Biológica , Encéfalo/metabolismo , Cromatografia Líquida de Alta Pressão/métodos , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Humanos , Solubilidade , Espectrometria de Massas em Tandem/métodos , Água
6.
Pharm Dev Technol ; 25(2): 159-167, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31623500

RESUMO

Films of gellan gum:pectin blends were prepared by solvent casting method. Gellan gum:pectin mass ratios were varied (4:1; 1:1; 1:4) at different concentrations (3% or 4%) and glycerol was used as plasticizer (1 or 2%). The films were thin (18-30 µm), translucent, flexible, and homogeneous. The surface pH was suitable for buccal application. All films reached high mechanical resistance and the mucoadhesive ability of them was evidenced. High ratio of gellan gum improved the mechanical resistance and the mucoadhesion of the films as well as the control of drug release rates. The films did not disintegrate in simulate saliva up to 24 h and curcumin release could be sustained up to 12 h. The set of data evidence that the films designed in this work represent a potential platform for buccal drug delivery.

7.
Front Microbiol ; 10: 2642, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31803166

RESUMO

We have previously reported on the activity of different extracts from Astronium sp. against Candida albicans, with the hydroethanolic extract prepared from leaves of A. urundeuva, an arboreal species widely distributed in arid environments of South America and often used in folk medicine, displaying the highest in vitro activity. Here we have further evaluated the antifungal activity of this extract against strains of C. albicans and C. glabrata, the two most common etiological agents of candidiasis. The extract was tested alone and loaded into a nanostructured lipid system (10% oil phase, 10% surfactant and 80% aqueous phase, 0.5% Poloxamer 407®). In vitro susceptibility assays demonstrated the antifungal activity of the free extract and the microemulsion against both Candida species, with increased activity against C. glabrata, including collection strains and clinical isolates displaying different levels of resistance against the most common clinically used antifungal drugs. Checkerboard results showed synergism when the free extract was combined with amphotericin B against C. albicans. Serial passage experiments confirmed development of resistance to fluconazole but not to the free extract upon prolonged exposure. Although preformed biofilms were intrinsically resistant to treatment with the extract, it was able to inhibit biofilm formation by C. albicans at concentrations comparable to those inhibiting planktonic growth. Cytotoxicity assays in different cell lines as well as an alternative model using Artemia salina L. confirmed a good safety profile of the both free and loaded extracts, and an in vivo assay demonstrated the efficacy of the free and loaded extracts when used topically in a rat model of vaginal candidiasis. Overall, these results reveal the promise of the A. urundeuva leaves extract to be further investigated and developed as an antifungal.

8.
Nanomedicine ; 24: 102117, 2019 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-31676375

RESUMO

Vitamin C (Vit C) is a potent antioxidant with several applications in the cosmetic and pharmaceutical fields. However, the biggest challenge in the utilization of Vit C is to maintain its stability and improve its delivery to the active site. Several strategies have been developed such as: controlling the oxygen levels during formulation and storage, low pH, reduction of water content in the formulation and the addition of preservative agents. Additionally, the utilization of derivatives of Vit C and the development of micro and nanoencapsulated delivery systems have been highlighted. In this article, the multiple applications and mechanisms of action of vitamin C will be reviewed and discussed, as well as the new possibilities of delivery and improvement of stability.

10.
Artigo em Inglês | MEDLINE | ID: mdl-31512818

RESUMO

The pivotal issue of skin regeneration research is the development of effective biomaterials that exhibit biological activities as fungicide and bactericide, combining simple and low cost manufacturing technologies. In this context, nanocomposite scaffolds based on chitosan (Ch)/Laponite (Lap) were produced by using different concentrations of Lap via freeze-drying process for potential application in skin regeneration. The influence of Lap concentration on the scaffold properties was evaluated. The prepared scaffolds were characterized by x-ray diffraction (XRD), scanning electron microscopy (SEM), porosity, swelling capacity, and mechanical analyses. The results revealed that the scaffolds exhibited a porous architecture, besides the increase in the clay content, leads to an increase in the porosity, an improvement of mechanical strength, and a decrease of swelling capacity. In vitro tests were also carried out to evaluate the biocompatibility of the materials, such as bioadhesion, antibacterial activity, viability, and cell adhesion. Viability and cell adhesion demonstrated that all scaffolds were not cytotoxic and the fibroblast cells readily attached on the surface of the scaffolds. Thereby, the results suggested that the nanocomposite scaffolds are biomaterials potentially useful as wound dressings.

11.
Int J Nanomedicine ; 14: 6407-6424, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31496694

RESUMO

Chagas disease is one of the most important public health problems in Latin America due to its high mortality and morbidity levels. There is no effective treatment for this disease since drugs are usually toxic with low bioavailability. Serious efforts to achieve disease control and eventual eradication have been unsuccessful to date, emphasizing the need for rapid diagnosis, drug development, and a reliable vaccine. Novel systems for drug and vaccine administration based on nanocarriers represent a promising avenue for Chagas disease treatment. Nanoparticulate systems can reduce toxicity, and increase the efficacy and bioavailability of active compounds by prolonging release, and therefore improve the therapeutic index. Moreover, nanoparticles are able to interact with the host's immune system, modulating the immune response to favour the elimination of pathogenic microorganisms. In addition, new advances in diagnostic assays, such as nanobiosensors, are beneficial in that they enable precise identification of the pathogen. In this review, we provide an overview of the strategies and nanocarrier-based delivery systems for antichagasic agents, such as liposomes, micelles, nanoemulsions, polymeric and non-polymeric nanoparticles. We address recent progress, with a particular focus on the advances of nanovaccines and nanodiagnostics, exploring new perspectives on Chagas disease treatment.


Assuntos
Doença de Chagas/tratamento farmacológico , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Nanopartículas/química , Portadores de Fármacos/administração & dosagem , Humanos , Micelas , Nanopartículas/administração & dosagem , Polímeros/química
12.
Front Microbiol ; 10: 1667, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31417503

RESUMO

Currently 75-88% of fungal infections are caused by Candida species, and Candida albicans is the main microorganism that causes these infections, especially oral candidiasis. An option for treatment involves the use of the antifungal peptide Histatin 5 (Hst 5), which is naturally found in human saliva but undergoes rapid degradation when present in the oral cavity, its site of action. For this reason, it is important to develop a way of applying this peptide to the oral lesions, which promotes the gradual release of the peptide. In the present study, we have evaluated the development of liposomes of different lipid compositions, loaded with the peptide as a way to promote its release slowly and gradually, preserving its antifungal potential. For this, the peptide 0WHistatin 5, an analog of the peptide Hst 5, was synthesized, which contains the amino acid tryptophan in its sequence. The solid phase synthesis method was used, followed by cleavage and purification. The liposomes were produced by thin film hydration technique in three different lipid compositions, F1, F2, and F3 and were submitted to an extrusion and sonication process to standardize the size and study the best technique for their production. The liposomes were characterized by dynamic light scattering, and tests were performed to determine the encapsulation efficiency, release kinetics, stability, and evaluation of antifungal activity. The extruded liposomes presented average size in the range of 100 nm, while sonicated liposomes presented a smaller size in the range of 80 nm. The encapsulation efficiency was higher for the sonicated liposomes, being 34.5% for F1. The sonicated F3 presented better stability when stored for 60 days at 4°C. The liposomes showed the ability to release the peptide for the total time of 96 h, with the first peak after 5 h, and a further increase of the released after 30 h. Time-kill assay showed that the liposomes were able to control yeast growth for 72 h. The data suggest that the liposomes loaded with 0WHistatin 5 maintained the action of the peptide and were able to limit the growth of C. albicans, being a suitable system for use in the treatment of oral candidiasis.

13.
AAPS PharmSciTech ; 20(7): 253, 2019 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-31309346

RESUMO

Drug delivery systems (DDS) can be designed to enrich the pharmacological and therapeutic properties of several drugs. Many of the initial obstacles that impeded the clinical applications of conventional DDS have been overcome with nanotechnology-based DDS, especially those formed by chitosan (CS). CS is a linear polysaccharide obtained by the deacetylation of chitin, which has potential properties such as biocompatibility, hydrophilicity, biodegradability, non-toxicity, high bioavailability, simplicity of modification, aqueous solubility, and excellent chemical resistance. Furthermore, CS can prepare several DDS as films, gels, nanoparticles, and microparticles to improve delivery of drugs, such as photosensitizers (PS). Thus, CS-based DDS are broadly investigated for photodynamic therapy (PDT) of cancer and fungal and bacterial diseases. In PDT, a PS is activated by light of a specific wavelength, which provokes selective damage to the target tissue and its surrounding vasculature, but most PS have low water solubility and cutaneous photosensitivity impairing the clinical use of PDT. Based on this, the application of nanotechnology using chitosan-based DDS in PDT may offer great possibilities in the treatment of diseases. Therefore, this review presents numerous applications of chitosan-based DDS in order to improve the PDT for cancer and fungal and bacterial diseases.


Assuntos
Quitosana/química , Sistemas de Liberação de Medicamentos , Fotoquimioterapia , Fármacos Fotossensibilizantes/administração & dosagem , Infecções Bacterianas/tratamento farmacológico , Humanos , Micoses/tratamento farmacológico , Nanopartículas/química , Neoplasias/tratamento farmacológico , Fármacos Fotossensibilizantes/química , Polissacarídeos
14.
Crit Rev Anal Chem ; : 1-20, 2019 Jul 29.
Artigo em Inglês | MEDLINE | ID: mdl-31353930

RESUMO

Trans-resveratrol (TR) is the biological active isomer of resveratrol and the one responsible for therapeutic effects; both molecules are non-flavonoid phenolics of the stilbenes class found mainly in berries and red grapes. TR biological properties lie in modulation of various enzymatic classes. It is a promising candidate to novel drugs due its applications in pharmaceutical and cosmetic industries, such as anticarcinogenic, antidiabetic, antiacne, antioxidant, anti-inflammatory, neuroprotective, and photoprotector agent. It has effects on bone metabolism, gastrointestinal tract, eyes, kidneys, and in obesity treatment as well. Nevertheless, its low solubility in water and other polar solvents may be a hindrance to its therapeutic effects. Various strategies been developed to overcome these issues, such as the drug delivery systems. The present study performed a research about methods to identify TR and RESV in several samples (raw materials, wines, food supplements, drug delivery systems, and blood plasma). Most of the studies tend to analyze TR and RESV by high performance liquid chromatography (HPLC) coupled with different detectors, even so, there are reports of the use of capillary electrophoresis, electron spin resonance, gas chromatography, near-infrared luminescence, UV-Vis spectrophotometer, and vibrational spectrophotometry, for this purpose. Thus, the review evaluates the biological activity of TR and demonstrates the currently used analytical methods for its quantification in different matrices.

15.
Curr Med Chem ; 2019 Jun 24.
Artigo em Inglês | MEDLINE | ID: mdl-31232233

RESUMO

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have been shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the noninvasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes.The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presentsan innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.

17.
AAPS PharmSciTech ; 20(6): 225, 2019 Jun 18.
Artigo em Inglês | MEDLINE | ID: mdl-31214798

RESUMO

The vaginal mucosa is a very promising route for drug administration due to its high permeability and the possibility to bypass first pass metabolism; however, current vaginal dosage forms present low retention times due to their dilution in vaginal fluids, which hampers the efficacy of many pharmacological treatments. In order to overcome these problems, this study proposes to develop a mucoadhesive in situ gelling liquid crystalline precursor system composed of 30% of oleic acid and cholesterol (7:1), 40% of ethoxylated and propoxylated cetyl alcohol, and 30% of a dispersion of 16% Poloxamer 407. The effect of the dilution with simulated vaginal fluid (SVF) on this system was evaluated by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), rheological studies, texture profile analysis (TPA), mucoadhesion study, in vitro drug release test using hypericin (HYP) as drug model, and cytotoxicity assay. PLM and SAXS confirmed the formation of an isotropic system. After the addition of three different concentrations of SVF (30, 50, and 100%), the resultant formulations presented anisotropy and characteristics of viscous lamellar phases. Rheology shows that formulations with SVF behaved as a non-Newtonian fluid with suitable shear thinning for vaginal application. TPA and mucoadhesion assays indicated the formation of long-range ordered systems as the amount of SVF increases which may assist in the fixation of the formulation on the vaginal mucosa. The formulations were able to control about 75% of the released HYP demonstrating a sustained release profile. Finally, all formulations acted as safe vaginal drug delivery systems.


Assuntos
Administração Intravaginal , Géis/metabolismo , Membrana Mucosa/metabolismo , Animais , Líquidos Corporais , Cristalização , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Feminino , Poloxâmero/metabolismo , Reologia , Espalhamento a Baixo Ângulo , Vagina , Viscosidade , Difração de Raios X
18.
Int J Pharm ; 567: 118460, 2019 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-31247278

RESUMO

As a new strategy for treatment of ductal carcinoma in situ, biocompatible and bioadhesive nanoemulsions for intraductal administration of the cytotoxic agent piplartine (piperlongumine) were optimized in this study. To confer bioadhesive properties, the nanoemulsion was modified with chitosan or hyaluronic acid. Tricaprylin was selected as the nanoemulsion non-polar phase due to its ability to dissolve larger drug amounts compared to isopropyl myristate and monocaprylin. Use of phosphatidylcholine as sole surfactant did not result in a homogeneous nanoemulsion, while its association with polysorbate 80 and glycerol (in a surfactant blend) led to the formation of nanoemulsions with droplet size of 76.5 ±â€¯1.2 nm. Heating the aqueous phase to 50 °C enabled sonication time reduction from 20 to 10 min. Inclusion of either chitosan or hyaluronic acid resulted in nanoemulsions with similar in vitro bioadhesive potential, and comparable ability to prolong mammary tissue retention (to 120 h) in vivo without causing undesirable histological alterations. Piplartine was stable in both nanoemulsions for 60 days; however, the size of loaded NE-HA was maintained at a similar range for longer periods of time, suggesting that this nanoemulsion may be a stronger candidate for intraductal delivery.


Assuntos
Antineoplásicos Fitogênicos/administração & dosagem , Dioxolanos/administração & dosagem , Glândulas Mamárias Animais/metabolismo , Nanopartículas/administração & dosagem , Piperidonas/administração & dosagem , Adesividade , Animais , Antineoplásicos Fitogênicos/química , Galinhas , Quitosana/administração & dosagem , Quitosana/química , Membrana Corioalantoide/efeitos dos fármacos , Dioxolanos/química , Vias de Administração de Medicamentos , Emulsões , Feminino , Glicerol/administração & dosagem , Glicerol/química , Ácido Hialurônico/administração & dosagem , Ácido Hialurônico/química , Nanopartículas/química , Fosfatidilcolinas/administração & dosagem , Fosfatidilcolinas/química , Piperidonas/química , Polissorbatos/administração & dosagem , Polissorbatos/química , Ratos Wistar , Pele/química , Suínos
19.
J Biomed Nanotechnol ; 15(6): 1334-1344, 2019 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-31072440

RESUMO

The treatments of oral candidiasis involve azole-based antifungals; however, the fungal resistance of these drug compounds has been detected in worldwide. Therefore, the discovery of new molecules from natural sources, such as curcumin, has been reported for the treatment of fungal diseases. However, this drug has poor solubility in aqueous solvents and presents low bioavailability. Thus, the system was designed for a low viscosity precursor of a liquid crystal phase, and saliva leads a phase behaviour increasing the viscosity of system and the residence time in the mucosa and promotes antifungal activity Formulation composed of PPG-5-CETETH-20, oleic acid and water (30, 30, 40% w/w) denominated F. This formulation was diluted with artificial saliva at 10, 20 and 30% (w/v). These formulations were characterized by polarized light microscopy (PLM), mechanical behaviour, oscillatory rheology and performance studies on mucosa. In vitro studies were performed against a standard strain (ATTC 18804) or buccal isolated clinical strains for determinate the minimum inhibitory concentrations (MIC). PLM and Small-Angle X-ray Scattering (SAXS) revealed that formulation F is lamellar mesophase, whereas its dilution with artificial saliva changed the system to anisotropic hexagonal mesophase. Textural profiles show the increasing with the dilution of precursor system. Rheological measurements show that diluted systems exhibit elastic modulus values (G') than viscous modulus (G'') and it indicates more micro-structured system. Mucoadhesive force against excised porcine oesophageal mucosa showed that systems have properties mucoadhesive. Ex vivo retention studies on porcine oesophageal mucosa exhibited an increase of 5-fold and 3-fold in the retention of curcumin from F and F30, respectively. In vitro antifungal assay against Candida albicans revealed that curcumin-loaded systems were more potent against a standard strain (ATTC 18804) and buccal isolated strains compared with a curcumin solution. Hence, the physicochemical characterization, combined with ex vivo and in vitro studies, revealed that formulation designed could form a in situ gelling mucoadhesive with buccal retention of curcumin and the increase of its antifungal activity with great potential in the treatment of oral candidiasis.


Assuntos
Candidíase Bucal , Cristais Líquidos , Administração Bucal , Animais , Curcumina , Sistemas de Liberação de Medicamentos , Espalhamento a Baixo Ângulo , Suínos , Difração de Raios X
20.
Int J Pharm ; 564: 379-409, 2019 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-31028801

RESUMO

Mesoporous silica nanoparticles (MSNs) displays interesting properties for biomedical applications such as high chemical stability, large surface area and tunable pores diameters and volumes, allowing the incorporation of large amounts of drugs, protecting them from deactivation and degradation processes acting as an excellent nanoplatform for drug delivery. However, the functional MSNs do not present the ability to transport the therapeutics without any leakage until reach the targeted cells causing side effects. On the other hand, the hydroxyls groups available on MSNs surface allows the conjugation of specific molecules which can binds to the overexpressed Enhanced Growth Factor Receptor (EGFR) in many tumors, representing a potential strategy for the cancer treatment. Beyond that, the targeting molecules conjugate onto mesoporous surface increase its cell internalization and act as gatekeepers blocking the mesopores controlling the drug release. In this context, multifunctional MSNs emerge as stimuli-responsive controlled drug delivery systems (CDDS) to overcome drawbacks as low internalization, premature release before to reach the region of interest, several side effects and low effectiveness of the current treatments. This review presents an overview of MSNs fabrication methods and its properties that affects drug delivery as well as stimuli-responsive CDDS for cancer treatment.


Assuntos
Antineoplásicos/administração & dosagem , Sistemas de Liberação de Medicamentos , Nanopartículas/administração & dosagem , Neoplasias/tratamento farmacológico , Dióxido de Silício/administração & dosagem , Animais , Antineoplásicos/química , Antineoplásicos/farmacocinética , Humanos , Nanopartículas/química , Porosidade , Dióxido de Silício/química , Dióxido de Silício/farmacocinética , Distribuição Tecidual
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