Lycopene (LYC), a natural compound responsible for the red color of some fruits like pink grapefruit, red guava, watermelon, papaya and, mainly, present in tomatoes (Solanum lycopersicum). LYC has ...been extensively studied because of its various pharmacological properties such as antioxidant, cardioprotective, hypocholesterolemic, antineophasic, photoprotection, antidiabetic and antimicrobial activity. However, LYC uses in therapy is limited due to its insolubility in aqueous solvents, resulting in low bioavailability and stability. In order to overcome these drawbacks, it is essential to use of organic nanocarriers for LYC controlled release. Up to now, the description of LYC-loaded organic nanocarriers are scarce, mainly related to organic nanosystems based on lipid nanostructures such as nanoemulsions (NE), liposomes (LP), niosomes (NI), nanostructured lipid carriers (NLC) and solid lipid nanoparticles (SLN). Taking into account the development of new formulations, is indispensable the use of sensitive and suitable analytical methods previously validated. Among the analytical methods described here, high-performance liquid chromatography (HPLC) stands out due to its good accuracy, precision and desirable detection limit. In this review, we highlights the main biological and physicochemical properties of LYC, as well as LYC-based organic nanocarriers for controlled drug delivery and the analytical methods described in literature to determine LYC in any kind of matrix.
Commonly found colonizing the human microbiota,
is a microorganism known for its ability to cause infections, mainly in the vulvovaginal region known as vulvovaginal candidiasis (VVC). This pathology ...is, in fact, one of the main
clinical manifestations, changing from a colonizer to a pathogen. The increase in VVC cases and limited antifungal therapy make
an increasingly frequent risk in women's lives, especially in immunocompromised patients, pregnant women and the elderly. Therefore, it is necessary to develop new therapeutic options, especially those involving natural products associated with nanotechnology, such as lycopene and mesoporous silica nanoparticles. From this perspective, this study sought to assess whether lycopene, mesoporous silica nanoparticles and their combination would be an attractive product for the treatment of this serious disease through microbiological in vitro tests and acute toxicity tests in an alternative in vivo model of
. Although they did not show desirable antifungal activity for VVC therapy, the present study strongly encourages the use of mesoporous silica nanoparticles impregnated with lycopene for the treatment of other human pathologies, since the products evaluated here did not show toxicity in the in vivo test performed, being therefore, a topic to be further explored.
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Vaginal infections represent a clear women health problem due to the several issues as high recurrence rate, drug resistence and emergence of persistent strains. However, achieving ...improvements in therapeutic efficacy by using conventional formulations intended to vaginal drug delivery remains as a challenge due to anatomy and physiology of the vagina, since the secretion and renewal of vaginal fluids contribute to the removal of the dosage form. Hydrogels have been widely exploited aiming to achieve drug delivery directly into vaginal mucosa for local therapy due to their attractive features as increased residence time of the drug at the action site and control of drug release rates. Some polymers can aggregate specific properties to hydrogels as mucoadhesive, stimuli-responsive and antimicrobial, improving their interaction with the biological interface and therapeutic response. In this review, we highlight the advances, advantages and challenges of the hydrogels as drug and/or nanocarrier vehicles intended to the treatment of vaginal infections, emphasizing also the polymers and their properties more explored on the design these systems to improve the therapeutic effect on the vaginal tissue. In addition, this review can contribute for better exploitation these systems in search of new local treatments for bacterial vaginosis, candidiasis and trichomoniasis.
Lycopene, a red-colored carotenoid, has several biological properties, such as antioxidant, cardioprotective, antihypercholesterolemic, antidiabetic, antimicrobial, photoprotector and anticancer, ...making desirable its use as nutraceutical. Despite the fact that it can be found in several foods, tomato deserves great prominence because it is the major extraction source and the cheapest raw material, being therefore the human most ingested source. Tomato also stands out for being the source where lycopene was first discovered.
This review article seeks to highlight the entire route that lycopene passes until its use as a nutraceutical, highlighting the main methods of extraction, concentration and quantification.
Solvent extraction and super-critical fluid extraction, centrifugation and evaporation and HPLC and UV–vis spectrophotometer were the researchers most chosen methods of extraction, concentration and quantification, respectively. It also was noted that its association with nanotechnology is desirable to circumvent limitations related to its physicochemical characteristics that limit, not only its extraction process but also its nutraceutical use.
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•Lycopene has several biological properties.•Tomatoes is lycopene major extraction source.•Lycopene has limitations what can be circumvent with the association with nanocarriers.
Pharmaceutical nanotechnology has become a trend with incalculable advantages in the applicability of systems in the controlled, safe and effective release of drugs. Among the nanotechnological ...nanoparticles, the mesoporous silica nanoparticles stand out, a system with significant biocompatibility, good physical chemical stability, greater surface contact area with desirable and adjustable pore structure. Once developed and well defined, these pores can carry drugs and control their release. However, to create this type of nanoparticle is essencial to use surfactants since they act as pore template. Among the most important surfactants, cetyltrimethylammonium bromide (CTAB) highlights, a quaternary ammonium compound widely used as a surfactant in the synthesis of mesoporous silica nanoparticles (MSNs), hollow mesoporous silica (HMSNs) and core-shell MSNs. However, for achieving good results of drug-loaded pores it is necessary to remove CTAB by extraction techniques, which provides pores formation throughout the silica and the incorporation of molecules. During and after the removal process, it is possible that CTAB residues remains inside the pores, despide several removal processes are described as efficient in the complete removal of surfactants. In turn, the presence of CTAB residues can be advantageous, especially when considering its antimicrobial activity. Meanwhile, it should be noted that the presence of CTAB may present high toxicity risks. This review seeks to explore not only general aspects of the use of CTAB in the synthesis of MSNs, but also to assess its toxicity in prokaryotic and eukaryotic cells, in order to determine whether CTAB residues are acceptable in MSNs that will be used as drug delivery systems for further in vivo and clinical assays.
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•Greener methods for CTAB removal are desirable.•CTAB can be responsible for nanoparticles toxicity.•CTAB residues can be a potential tool against microorganism.
ABSTRACT
Infectious diseases are a major global concern being responsible for high morbidity and mortality mainly due to the development and enhancement of multidrug-resistant microorganisms exposing ...the fragility of medicines and vaccines commonly used to these treatments. Taking into account the scarcity of effective formulation to treat infectious diseases, nanotechnology offers a vast possibility of ground-breaking platforms to design new treatment through smart nanostructures for drug delivery purposes. Among the available nanosystems, mesoporous silica nanoparticles (MSNs) stand out due their multifunctionality, biocompatibility and tunable properties make them emerging and actual nanocarriers for specific and controlled drug release. Considering the high demand for diseases prevention and treatment, this review exploits the MSNs fabrication and their behavior in biological media besides highlighting the most of strategies to explore the wide MSNs functionality as engineered, smart and effective controlled drug release nanovehicles for infectious diseases treatment.
Graphical Abstract
Schematic representation of multifunctional MSNs-based nanoplatforms for infectious diseases treatment
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•Mucoadhesive systems for vaginal administration.•Mucoadhesive systems composed of chitosan.•Mucoadhesive systems composed of chitosan intended for the treatment of infectious vaginal ...diseases.
Vaginal administration is a promising route for the local treatment of infectious vaginal diseases since it can bypass the first-pass metabolism, drug interactions, and adverse effects. However, the commercial products currently available for topical vulvovaginal treatment have low acceptability and do not adequately explore this route. Mucoadhesive systems can optimize the efficacy of drugs administered by this route to increase the retention time of the drug in the vaginal environment. Several polymers are used to develop mucoadhesive systems, among them chitosan, a natural polymer that is highly biocompatible and technologically versatile. Thus, the present review aimed to analyze the studies that used chitosan to develop mucoadhesive systems for the treatment of local vaginal infections. These studies demonstrated that chitosan as a component of mucoadhesive drug delivery systems (DDS) is a promising device for the treatment of vaginal infectious diseases, due to the intrinsic antimicrobial activity of this biopolymer and because it does not interfere with the effectiveness of the drugs used for the treatment.
Breast cancer is the commonest cancer among women, with more than 2 million cases per year and a lethality rate of 17.7%. The treatment of breast cancer still being a challenge due to the high ...heterogeneity of tumor cells. In this scenario, the development of targeted nanosystems for drug delivery has been investigated. Thus, the aim of this study was the development and characterization of folic acid-modified curcumin-loaded liposomes (LIP-CCM-FA) for the treatment of breast cancer. For this purpose, LIP-CCM-FA and unmodified liposomes (LIP-CCM) were developed and characterized in vitro using MCF-7 cells culture in two-dimensional (2D) and three-dimensional (3D) models. LIP-CCM and LIP-CCM-FA showed low particles size (~ 138 nm), narrow polydispersity indexes (~ 0.140), negative zeta potential (~ −13 mV), and high drug encapsulation efficiency (> 73%). Furthermore, LIP-CCM-FA showed a significantly greater cytotoxicity effect when compared with free curcumin and LIP-CCM using 2D and 3D cell culture models. In addition, in vitro cellular uptake assays using 2D and 3D models indicated higher cellular internalization and spheroid penetration of LIP-CCM-FA when compared with free curcumin and LIP-CCM, suggesting the potential of folic acid modification for improving drug internalization in breast cancer cells through its recognition by folate receptors overexpressed. In summary, this novel nanosystem demonstrated a greater in vitro antitumoral effect due to its ability to permeate tissues and be specifically recognized by folate receptors.
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Fungi are becoming increasingly resistant, especially the new strains. Therefore, this work developed nanoemulsions (NE) containing micafungin (MICA), in order to improve its action against ...infections caused by Candida auris. The NEs were composed of the surfactants polyoxyethylene (20) cetyl ether (Brij 58®)/soy phosphatidylcholine at 10%, sunflower oil/cholesterol at 10%, and 80% PBS. The NEs were characterized by Dynamic Light Scattering (DLS). For the microbiological in vitro evaluation the determination of the minimum inhibitory concentration (MIC), ergosterol/sorbitol, time kill and biofilms tests were performed. Additionally, the antifungal activity was also evaluated in a Galleria mellonella model. The same model was used in order to evaluate acute toxicity. The NE showed a size of ∼ 42.12 nm, a polydispersion index (PDI) of 0.289, and a zeta potential (ZP) of -3.86 mV. NEM had an average size of 41.29 nm, a PDI of 0.259, and a ZP of -4.71 mV. Finally, both nanoemulsions showed good stability in a storage period of 3 months. Although NEM did not show activity in planktonic cells, it exhibited action against biofilm and in the in vivo infection model. In the alternative in vivo model assay, it was possible to observe that both, NEM and free MICA at 0.2 mg/l, was effective against the infection, being that NEM presented a better action. Finally, NEM and free MICA showed no acute toxicity up to 4 mg/l. NEM showed the best activities in in vitro in mature antibiofilm and in alternative in vivo models in G. mellonella. Although, NEs showed to be attractive for MICA transport in the treatment of infections caused by C. auris in vitro and in vivo studies with G. mellonella, further studies should be carried out, in mice, for example.
Vulvovaginal candidiasis is a public health problem with a high incidence among female patients. Currently, there is an increase in the identification of Candida spp. resistant to current therapy, ...making it necessary to search for new therapeutic alternatives. The synergistic potential of curcumin with fluconazole is described in the literature. However, due to its high lipophilicity, it is necessary to use drug‐delivery systems to adequately explore its potential, among which is the nanostructured lipid carrier. However, to date, there is no validated method of high‐performance liquid chromatography for simultaneous determination of fluconazole and curcumin in the literature. Thus, the present work developed a high‐performance liquid chromatography method for simultaneous determination of fluconazole and curcumin co‐encapsulated in nanostructured lipid carrier which was validated according to the International Conference on Harmonization (Technical Requirements for Registration of Pharmaceuticals for Human Use) – Q2 (R1) and the Food and Drug Administration ‐ Guidance for Bioanalytical Method. The method was applied to determine the encapsulation efficiency and drug‐loading of curcumin and fluconazole in nanostructured lipid carriers. The developed method proved to be selective, precise, accurate, and robust for the simultaneous determination of both drugs, enabling the quantification of encapsulation efficiency and drug‐loading of curcumin and fluconazole in nanostructured lipid carriers.
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