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1.
Data Brief ; 38: 107391, 2021 Oct.
Article in English | MEDLINE | ID: mdl-34604482

ABSTRACT

Cochliomyia hominivorax is the dipteran that causes the worst and most serious types of myiasis in animals and humans in the Americas. The data described here show the effects of a commercial product formulated on the basis of citronella essential oil nanoemulsified (Nano Citronela Plus®) directly on eggs, first, second and third stage larvae of the C. hominivorax blowfly, in addition to the indirect effect on the oviposition of adult flies. These data make up the gross base that was used in the preparation of the article "Repellent, ovicidal, larvicidal and adulticidal action of a nanoemulsion of Citronella essential oil (Cymbopogon winterianus) on Cochliomyia hominivorax (Diptera: Calliphoridae)" Bricarello et al., 2021. Counting data of larvae, eggs and adult flies live and dead after contact with the product, data on weighing and counting of eggs from the repellency test are available, as well as photos of cuticular changes that occurred in the larvae and malformations observed after contact with Nano Citronela Plus®.

2.
Colloids Surf B Biointerfaces ; 198: 111390, 2021 Feb.
Article in English | MEDLINE | ID: mdl-33208279

ABSTRACT

Cutaneous leishmaniasis is a worldwide public health problem. Conventional therapies, in addition to the high cost, have many adverse effects and cases of parasite's resistance. Chalcones are secondary metabolites precursors in the flavonoid pathway and can be obtained naturally, but with low yield from plant raw material. Thus, the use of synthetic chalcones has been a promising strategy for the development of molecules with leishmanicidal activity. Thus, this work aimed to develop a controlled release system of two synthetic chalcone (trans-chalcones and 3'-(trifluormethyl)-chalcone) using polyvinyl alcohol nanofibers (PVA) as scaffold. The association of chalcones to the nanofibers was made by nanoemulsions (NE) thereof, i.e., a colloidal system on a nanometric scale, which allows compounds with opposite polarities to remain miscible and stable throughout their manipulation. Chalcone nanoemulsions were developed using the spontaneous emulsification technique. The NE were characterized regarding their particle size, polydispersion index (PDI), and zeta potential. The results showed NE with spherical shape, absolute values of zeta potential were higher than 30 mV and homogeneous distribution pattern (PDI < 0.3). Dynamics light scattering (DLS) analysis showed similar hydrodynamic rays, i.e., 180 nm (trans-chalcone NE) and 178 nm (NE containing 3'-(trifluormethyl)-chalcone, in addition to presenting encapsulation efficiency values close to 100 %. Subsequently, the NE were added to a polymeric solution of polyvinyl alcohol (PVA) and processed via the electrospinning technique affording a PVA matrix (15 %, w/v) nanofiber containing the chalcones NE at 1 mg.mL-1. In a follow-up experiment, the skin permeation assay of the PVA matrix-chalcone NE was performed in vitro using Franz type diffusion cells and porcine ear as biological model of study. The results showed that the treatments with the nanofibers containing the chalcone NE were retained mainly in the stratum corneum, while the NE suspensions containing chalcone were retained in the epidermis and dermis. This result is thought to be relevant, since parasites are located mainly in the dermis. Further, in vitro assay against the amastigote form of L. (L) amazonensis, showed IC50 values to trans-chalcone and 3'-(trifluormethyl)-chalcone of 24.42 ± 6.76 µg.mL-1 and 15.36 ± 4.61 µg.mL-1, respectively. In addition to improving the solubility of the compounds tested in culture medium without using organic solvents, chalcones in nano-emulsified form reduced the IC50 to 9.09 ± 1.24 µg.mL-1 (trans-chalcone) and 10.27 ± 2.27 µg.mL-1 (3'-(trifluormethyl)-chalcone) which confirmed the potential of the nanoemulsion containing chalcone for cutaneous leishmaniasis treatment.


Subject(s)
Chalcone , Chalcones , Leishmania , Leishmaniasis, Cutaneous , Animals , Polyvinyl Alcohol , Swine
3.
An Acad Bras Cienc ; 92(4): e20200134, 2020.
Article in English | MEDLINE | ID: mdl-33237141

ABSTRACT

Pectin (PC) extracted from a solid residue from cassava roots (Manihot esculenta Crantz) was used to coat nanoparticles (NP) containing ß-carotene (BC) aiming at the gastrointestinal administration of this lipophilic nutraceutical. The NP were prepared by spontaneous emulsification method using food grade components. Pectin-coated NP have been successfully prepared as confirmed by the increased particle size and negative surface charges due to the pectin's anionic nature. NP showed spherical shape and monodisperse distribution, with a mean size of 21.3 nm (polydispersity index (PDI) 0.29) for BC PC T80-NP (nanoparticle with ß-carotene, pectin and Tween 80) and 261.4 nm (PDI 0.1) for BC PC T20-NP (nanoparticle with ß-carotene, pectin and Tween 20). BC was encapsulated at amounts of 530 and 324 µg/ml for BC PC T80-NP and BC PC T20-NP, respectively, with high encapsulation efficiency (> 95%), increasing its antioxidant capacity in vitro, besides no cytotoxic effect. However, only BC PC T20-NP was stable over a 90 days storage period (4°C) and revealed a strong interaction between pectin and mucin. These results suggest that pectin-coated BC PC T20-NP is a promising strategy to improve the bioavailability and permeation of BC for administration through mucosal surfaces.


Subject(s)
Manihot , Nanoparticles , Cellulose , Pectins , beta Carotene
4.
J Food Sci Technol ; 56(3): 1165-1173, 2019 Mar.
Article in English | MEDLINE | ID: mdl-30956296

ABSTRACT

This study evaluated the total phenolic content (TPC) and the antioxidant activity (AA) of cow's milk enriched with phenolic compounds extracted from jaboticaba peel, either by adding jaboticaba crude extract or a jaboticaba-loaded nanoemulsion. Three nanoemulsions with 5, 10 and 15% of jaboticaba extract were prepared. Average particle diameter (166.7-181.7 nm), polydispersity index (0.138-0.156) and zeta potential (ranging from - 35.30 to - 38.60 mV) were measured for the three different colloidal systems. The nanoemulsion with 15% of jaboticaba extract (J15-NE) was chosen for milk enrichment. J15-NE showed an encapsulation efficiency of 85.6% and remained stable for 60 days at 8 °C. Transmission electron microscopy of J15-NE displayed nanoparticles with a well-defined spherical shape. Reference milk, milk enriched with jaboticaba extract and milk enriched with J15-NE were characterised by a TPC of 93, 171 and 161 µg/ml GAE (gallic acid equivalent), respectively, and an AA of 0.04, 0.17 and 0.14 µg/ml TEAC (trolox equivalent antioxidant capacity), respectively. Thus, this study showed that nanoemulsion with jaboticaba peel extract could be exploited as an ingredient to enrich the properties of milk.

5.
Int J Nanomedicine ; 13: 5823-5836, 2018.
Article in English | MEDLINE | ID: mdl-30319253

ABSTRACT

BACKGROUND: Posttransplant cell tracking, via stem cell labeling, is a crucial strategy for monitoring and maximizing benefits of cell-based therapies. The structures and functionalities of polysaccharides, proteins, and lipids allow their utilization in nanotechnology systems. MATERIALS AND METHODS: In the present study, we analyzed the potential benefit of curcumin-loaded nanoparticles (NPC) using Vero cells (in vitro) and NPC-labeled adipose-derived mesenchymal stem cells (NPC-ADMSCs) (in vivo) in myocardial infarction and sciatic nerve crush preclinical models. Thereafter, transplantation, histological examination, real time imaging, and assessment of tissue regeneration were done. RESULTS: Transplanted NPC-ADMSCs were clearly identified and revealed potential benefit when used in cell tracking. CONCLUSION: This approach may have broad applications in modeling labeled transplanted cells and in developing improved stem cell therapeutic strategies.


Subject(s)
Cell Tracking/methods , Curcumin/pharmacology , Nanoparticles/chemistry , Animals , Cell Differentiation , Chlorocebus aethiops , Fluorescence , Green Fluorescent Proteins/metabolism , Immunophenotyping , Mesenchymal Stem Cell Transplantation , Mesenchymal Stem Cells/metabolism , Myocardial Infarction/pathology , Myocardial Infarction/therapy , Nanoparticles/ultrastructure , Nerve Crush , Rats, Wistar , Sciatic Nerve/pathology , Vero Cells
6.
Drug Dev Ind Pharm ; 44(4): 643-651, 2018 Apr.
Article in English | MEDLINE | ID: mdl-29139323

ABSTRACT

OBJECTIVE: The aim of this work is to develop and characterize nanoemulsions containing jaboticaba extract (Plinia peruviana) aiming pharmaceutical and cosmetic applications. METHODS: Nanoemulsions were prepared by high-pressure homogenization method using different concentrations of components (oil, surfactant, and extract) and homogenization pressures, in order to optimize the preparation conditions. Both unloaded and extract-loaded nanoemulsions were characterized according to their size, polydispersity, zeta potential, pH, morphology, and physical stability. Total phenolic and flavonoid contents in free jaboticaba extract and jaboticaba-loaded nanoemulsions were determined spectrophotometrically, while ellagic acid content was determined by high-performance liquid chromatography (HPLC) analysis. In vitro antioxidant activity was investigated by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) methods. RESULTS: Colloidal dispersions exhibited a mean particle size around 200 nm, with monodisperse size distribution (PdI <0.3), and spherical shape. Stability studies showed that nanoemulsions were stable over 120 d of storage at room temperature. Jaboticaba nanoemulsions showed significant concentrations of phenolics, flavonoids, and ellagic acid, with encapsulation efficiency values higher than 90%. Antioxidant properties of jaboticaba nanoemulsions were demonstrated by its remarkable ability to scavenge DPPH free radicals and to reduce ferric-tripyridyltriazine complex, which can be attributed to their phenolic and flavonoid contents. CONCLUSIONS: The results suggest that nanoemulsions containing jaboticaba extract can be considered a promising candidate as a new antioxidant agent.


Subject(s)
Antioxidants/chemistry , Antioxidants/pharmacology , Myrtaceae/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Antioxidants/administration & dosage , Biphenyl Compounds , Drug Compounding , Drug Stability , Ellagic Acid/chemistry , Emulsions , Flavonoids/analysis , Hydrogen-Ion Concentration , Nanoparticles , Particle Size , Phenols/analysis , Picrates , Plant Extracts/administration & dosage
7.
Curr Pharm Des ; 23(24): 3515-3528, 2017.
Article in English | MEDLINE | ID: mdl-28472915

ABSTRACT

Nanotechnology is an exciting emerging field with multiple applications in skin regeneration. Nanofibers have gained special attention in skin regeneration based on their structural similarity to the extracellular matrix. A wide variety of polymeric nanofibers with distinct properties have been developed and tested as scaffolds for skin regeneration. Besides providing support for tissue repair, nanofibrous materials can act as delivery systems for drugs, proteins, growth factors, and other molecules. Moreover, the morphology, biodegradability, and other functionalities of nanofibrous materials can be controlled towards specific conditions of wound healing. Other nanostructured drug delivery systems, such as nanoparticles, micelles, nanoemulsions, and liposomes, have been used to improve wound healing at different stages. These nanoscale delivery systems have demonstrated several benefits for the wound healing process, including reduced cytotoxicity of drugs, administration of poorly water-soluble drugs, improved skin penetration, controlled release properties, antimicrobial activity, and protection of drugs against light, temperature, enzymes or pH degradation, as well as stimulation of fibroblast proliferation and reduced inflammation.


Subject(s)
Biocompatible Materials/administration & dosage , Nanoparticles/administration & dosage , Nanotechnology/trends , Tissue Scaffolds/trends , Wound Healing/physiology , Animals , Biocompatible Materials/metabolism , Humans , Liposomes , Micelles , Nanofibers/administration & dosage , Nanoparticles/metabolism , Nanostructures/administration & dosage , Nanotechnology/methods , Wound Healing/drug effects
8.
AAPS PharmSciTech ; 18(3): 920-925, 2017 Apr.
Article in English | MEDLINE | ID: mdl-27230504

ABSTRACT

It is well-known that nanoencapsulation may overcome biopharmaceutical limitations of curcumin (CUR), but studies regarding the contribution of the vesicular nature of CUR-loaded nanoparticles on skin permeation are still scarce. Therefore, the effect of three colloidal systems (solid lipid nanoparticles (SLN), nanoemulsion (NE), and polymeric nanoparticles (NP)) on the control of cutaneous permeation of CUR was investigated in porcine ear skin/Franz diffusion cells. Colloidal suspensions were designed to present a similar particle size (±170 nm), narrow size distribution (PdI < 0.2), and high entrapment efficiency (>99%). Zeta potential values were -0.13, -9.68 and -36.7 mV for the CUR-loaded NP, SLN and NE, respectively. Nanoencapsulation resulted in a cumulative amount of CUR in the more superficial layers of the skin. NP significantly enhanced the compound retention in the epidermis, which was approximately 2.49- and 3.32-fold more than SLN and NE, respectively. The CUR levels into the dermis were significantly increased after treatment with NE, which may be associated with repulsion phenomena in surface skin. Therefore, a more superficial or deeper action of CUR on the skin may be obtained depending on nanostructure type. While NPs are more effective in upper skin layers, NE should be prioritized when a dermal action for the CUR is required.


Subject(s)
Curcumin/chemistry , Lipids/chemistry , Nanostructures/chemistry , Polymers/chemistry , Skin/metabolism , Administration, Cutaneous , Animals , Curcumin/administration & dosage , Drug Delivery Systems/methods , Emulsions/administration & dosage , Emulsions/chemistry , Nanoparticles/chemistry , Particle Size , Permeability , Swine
9.
J Nanosci Nanotechnol ; 16(2): 1275-81, 2016 Feb.
Article in English | MEDLINE | ID: mdl-27433577

ABSTRACT

Quercetin is a natural compound that has several biological activities including anticancer activity. However, the use of this drug has been limited mostly because of its poor water solubility and low bioavailability. Therefore, the development of quercetin-loaded nanocarrier systems may be considered a promising advance to exploit its therapeutic properties in clinical setting including cancer treatment. This study evaluates the effect of orally administered nanosized emulsion containing quercetin (QU-NE) on the cytotoxicity activity against B16-F10 cells in vitro, and on subcutaneous melanoma in mice inoculated with B16-F1O cells. In vivo experiments, also evaluate the co-administration of quercetin with cisplatin in order to predict synergic effects and the renal and hepatic toxicity. The nanocarriers were prepared through the hot solvent diffusion associated with the phase inversion temperature methods. In vitro study showed reduction of cell viability in a concentration-depend manner for free quercetin and QU-NE. In vivo study, quercetin either as a free drug or colloidal dispersion was administrated at a dose of 5 mg kg(-1) twice a week for 17 days via oral route. Cisplatin was administrated at dose of 1 mg kg(-1) once a week intraperitoneally. Free quercetin and QU-NE reduced tumor growth, however, the reduction observed for QU-NE (P < 0.001 vs. control) was significantly higher than free quercetin (P < 0.05 vs. control). The association of both drugs did not show synergic effect. Besides, no renal or hepatic toxicities were observed after administration of free quercetin and QU-NE. These results suggest that an improvement in the oral bioavailability of quercetin occurred when this compound was dissolved in the oily phase of a nanosized emulsion, indicating that it might have a potential application in the treatment of melanoma.


Subject(s)
Antineoplastic Agents , Drug Carriers , Melanoma/drug therapy , Nanoparticles/chemistry , Quercetin , Administration, Oral , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Cisplatin/chemistry , Cisplatin/pharmacology , Drug Carriers/chemistry , Drug Carriers/pharmacology , Drug Screening Assays, Antitumor , Emulsions , Male , Melanoma/metabolism , Melanoma/pathology , Mice , Quercetin/chemistry , Quercetin/pharmacology
10.
Methods Mol Biol ; 1391: 65-80, 2016.
Article in English | MEDLINE | ID: mdl-27108310

ABSTRACT

Plinia cauliflora (jaboticaba) is a native fruit tree from Brazilian rainforest widely used in popular medicine to prevent diarrhea, asthma, and infections. Studies have shown that the major therapeutic potential of jaboticaba fruits is on its peel, a rich source of anthocyanins. These secondary metabolites have well-known antioxidant and anti-inflammatory activities and have been claimed to be effective to treat diabetes, cancer, cardiovascular diseases, and stroke. This chapter describes a series of methodologies to evaluate important in vitro biological activities like cytotoxicity, proliferation, and migration of a hydroalcoholic extract of jaboticaba peel on mouse fibroblast L929 line. Assays to assess total phenolic, flavonoid, and anthocyanin contents and antioxidant activities are described as well.


Subject(s)
Anthocyanins/chemistry , Anthocyanins/pharmacology , Drug Evaluation, Preclinical/methods , Myrtaceae/chemistry , Animals , Anthocyanins/isolation & purification , Antioxidants/chemistry , Antioxidants/isolation & purification , Antioxidants/pharmacology , Cell Line , Cell Movement/drug effects , Cell Proliferation/drug effects , Cell Survival/drug effects , Fibroblasts/cytology , Fibroblasts/drug effects , Flavonoids/chemistry , Flavonoids/isolation & purification , Flavonoids/pharmacology , Mice , Phenols/chemistry , Phenols/isolation & purification , Phenols/pharmacology , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Wound Healing/drug effects
11.
J Nanosci Nanotechnol ; 15(1): 781-91, 2015 Jan.
Article in English | MEDLINE | ID: mdl-26328442

ABSTRACT

Mucoadhesive nanoparticles loaded with curcumin were developed as a new approach to deliver curcumin for the local treatment of oral cancer. PCL nanoparticles coated with chitosan displaying different molar masses were prepared by using the nanoprecipitation technique. The mucoadhesive properties of nanoparticle suspensions were demonstrated by their strong ability to interact with the glycoprotein mucin through electrostatic interactions. Similar permeation profiles of curcumin loaded in uncoated and chitosan-coated nanoparticles across porcine esophageal mucosa were verified. Curcumin concentrations retained in the mucosa suggest the possibility of a local effect of the drug. In vitro studies demonstrated that free curcumin.and curcumin loaded into nanoparticles coated with chitosan caused significant reduction of SCC-9 human oral cancer cell viability in a concentration and time-dependent manner. However, no significant cell death was observed after 24 h of treatment with unloaded nanoparticles coated with chitosan. In addition, curcumin-loaded nanoparticles showed reduced cytotoxicity, when compared with the free drug. Therefore, chitosan-coated PCL nanoparticles may be considered a promising strategy to deliver curcumin directly into the oral cavity for the treatment of oral cancer.


Subject(s)
Antineoplastic Agents/pharmacokinetics , Chitosan/pharmacokinetics , Curcumin/pharmacokinetics , Mouth Neoplasms/metabolism , Nanoparticles/chemistry , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Cell Survival/drug effects , Chitosan/chemistry , Chitosan/pharmacology , Curcumin/chemistry , Curcumin/pharmacology , Esophagus/chemistry , Esophagus/metabolism , Humans , Mucins/metabolism , Nanoparticles/toxicity , Swine
12.
J Pharm Sci ; 104(10): 3524-34, 2015 Oct.
Article in English | MEDLINE | ID: mdl-26085173

ABSTRACT

The study was aimed to evaluate the effect of orally administered chitosan-coated nanoparticles containing curcumin on metastatic melanoma. Chitosan-coated nanoparticles containing curcumin were prepared, and their antimetastatic activity was investigated both in vitro and in vivo. Curcumin decreased cell viability and induced apoptosis of B16F10 melanoma cells. We observed that curcumin significantly decreased the expression of metalloproteinases, which are known to be associated with migration and proliferation of cancer cells. Importantly, treatment with chitosan-coated nanoparticles containing curcumin decreased pulmonary tumor formation in a murine model of experimental metastasis. Histological analyses confirmed the macroscopic results in which lungs of mice treated with curcumin-loaded chitosan-coated polycaprolactone nanoparticles had only a few small nodules and most of them were free of melanoma. Our findings indicate that nanoparticles coated with the mucoadhesive polymer chitosan containing curcumin may be a promising approach and/or intervention for the treatment of malignant melanoma.


Subject(s)
Antineoplastic Agents, Phytogenic/administration & dosage , Antineoplastic Agents, Phytogenic/therapeutic use , Curcumin/administration & dosage , Curcumin/therapeutic use , Melanoma, Experimental/drug therapy , Melanoma/drug therapy , Animals , Apoptosis/drug effects , Cell Line, Tumor , Cell Movement/drug effects , Chitosan , Female , Intestinal Absorption , Matrix Metalloproteinase 2/biosynthesis , Melanoma/pathology , Melanoma, Experimental/pathology , Mice , Mice, Inbred C57BL , Nanoparticles , Neoplasm Metastasis , Polyesters , Skin Neoplasms , Melanoma, Cutaneous Malignant
13.
Toxicol Sci ; 147(1): 104-15, 2015 Sep.
Article in English | MEDLINE | ID: mdl-26048652

ABSTRACT

Xyloglucan-block-polycaprolactone (XGO-PCL) copolymer nanoparticles have been proposed as nanocarriers for drug delivery. However, the possible harmful effects of exposure to nanoparticles still remain a concern. Therefore, the aim of this study is to evaluate the potential toxicity of XGO-PCL nanoparticles using in vitro and in vivo assays. Cytotoxicity and genotoxicity studies were conducted on MRC-5 human fetal lung fibroblast cells upon exposure to XGO-PCL nanoparticles. No significant reduction in the cell viability and no DNA damage were observed at the different concentrations tested. Erythrocyte toxicity was assessed by the incubation of nanoparticles with human blood. XGO-PCL nanoparticles induced a hemolytic ratio of less than 1%, indicating good blood compatibility. Finally, the subacute toxicity of XGO-PCL nanoparticles (10 mg/kg/day) was evaluated in BALB/c mice when administered orally or intraperitoneally for 14 days. Results of the in vivo toxicity study showed no clinical signs of toxicity, mortality, weight loss, or hematological and biochemical alterations after treatment with nanoparticles. Also, microscopic analysis of the major organs revealed no histopathological abnormalities, corroborating the previous results. Thus, it can be concluded that XGO-PCL nanoparticles induced no effect indicative of toxicity, indicating their potential use as drug delivery systems.


Subject(s)
Drug Delivery Systems/adverse effects , Glucans/toxicity , Nanoparticles/toxicity , Polyesters/toxicity , Xylans/toxicity , Animals , Apoptosis/drug effects , Blood Cell Count , Body Weight/drug effects , Cell Line , Cell Survival/drug effects , DNA Damage , Erythrocytes/drug effects , Female , Hemolysis/drug effects , Humans , Mice , Mice, Inbred BALB C , Mutagens/toxicity , Polymers
14.
Int J Pharm ; 486(1-2): 217-25, 2015.
Article in English | MEDLINE | ID: mdl-25840273

ABSTRACT

A combination of bacterial cellulose (BC) gel and amphiphilic block copolymer nanoparticles was investigated as a drug delivery system (DDS) for hydrophobic active ingredients. Poly(ethylene oxide)-b-poly(caprolactone) (PEO-b-PCL) and retinol were used as the block copolymer and hydrophobic active ingredient, respectively. The BC gel was capable of incorporating copolymer nanoparticles and releasing them in an acetic acid-sodium acetate buffer solution (pH 5.2) at 37 °C. The percentage of released copolymer reached a maximum value of approximately 60% after 6h and remained constant after 24h. The percentage of retinol released from the copolymer-containing BC gel reached a maximum value at 4h. These results show that the combination of BC gel and nanoparticles is a slow-release system that may be useful in the cosmetic and biomedical fields for skin treatment and preparation.


Subject(s)
Cellulose/chemistry , Drug Delivery Systems , Lactones/chemistry , Nanoparticles/chemistry , Polyethylene Glycols/chemistry , Vitamin A/chemistry , Cellulose/biosynthesis , Delayed-Action Preparations/chemistry , Drug Liberation , Gels , Gluconacetobacter xylinus/metabolism , Hydrophobic and Hydrophilic Interactions
15.
J Pharm Sci ; 103(11): 3764-3771, 2014 Nov.
Article in English | MEDLINE | ID: mdl-25187001

ABSTRACT

Mucoadhesive films containing curcumin-loaded nanoparticles were developed, aiming to prolong the residence time of the dosage form in the oral cavity and to increase drug absorption through the buccal mucosa. Films were prepared by the casting method after incorporation of curcumin-loaded chitosan-coated polycaprolactone nanoparticles into plasticized chitosan solutions. Different molar masses of mucoadhesive polysaccharide chitosan and concentrations of plasticizer glycerol were used to optimize the preparation conditions. Films obtained using medium and high molar mass chitosan were found to be homogeneous and flexible. Curcumin-loaded nanoparticles were uniformly distributed on the film surface, as evidenced by atomic force microscopy and high-resolution field-emission gun scanning electron microscopy (FEG-SEM) images. Analyses of film cross sections using FEG-SEM demonstrate the presence of nanoparticles inside the films. In addition, films proved to have a good rate of hydration in simulated saliva solution, displaying a maximum swelling of around 80% and in vitro prolonged-controlled delivery of curcumin. These results indicate that the mucoadhesive films containing nanoparticles offer a promising approach for buccal delivery of curcumin, which may be particularly useful in the treatment of periodontal diseases that require a sustained drug delivery.


Subject(s)
Chitosan/chemistry , Coated Materials, Biocompatible , Curcumin/chemistry , Drug Carriers , Mouth Mucosa/physiology , Nanoparticles , Adhesiveness , Administration, Buccal , Chemistry, Pharmaceutical , Curcumin/administration & dosage , Delayed-Action Preparations , Glycerol/chemistry , Kinetics , Microscopy, Atomic Force , Microscopy, Electron, Scanning , Nanotechnology , Plasticizers/chemistry , Polyesters/chemistry , Solubility , Surface Properties , Technology, Pharmaceutical/methods , Water/chemistry
16.
J Biomed Nanotechnol ; 10(5): 787-94, 2014 May.
Article in English | MEDLINE | ID: mdl-24734531

ABSTRACT

Quartz Crystal Microbalance with Dissipation Monitoring (QCM-D) was used to investigate the mucoadhesive properties of nanoparticles decorated with low, medium and high molar mass chitosan (CS). Uncoated and chitosan-coated polycaprolactone (PCL) nanoparticles loaded with curcumin were prepared by nanoprecipitation method and characterized in terms of size, surface charge and drug content. The interactions between nanoparticles and mucin layer were monitored after the treatment of SAM-functionalized gold-coated quartz crystals with bovine submaxillary gland mucin (BSM). The results show that all investigated chitosan-coated nanoparticles adsorb onto the BSM layer, and the mass uptake was found to be independent of the chitosan molar mass. Uncoated nanoparticles showed, however, no affinity with BSM layer, confirming that the adsorption of colloidal systems occurs due to their decoration with chitosan. The adhesion is mainly attributed to electrostatic interactions between protonated amino groups of mucoadhesive chitosan and negatively charged groups of mucin. The results suggest that chitosan-coated nanoparticles are promising carriers for hydrophobic drugs delivery in the buccal mucosa.


Subject(s)
Chitosan/chemistry , Curcumin/chemistry , Mouth Mucosa/chemistry , Mucins/chemistry , Nanocapsules/chemistry , Polyesters/chemistry , Adhesiveness , Animals , Antineoplastic Agents/chemistry , Cattle , Coated Materials, Biocompatible/chemistry , Energy Transfer , Materials Testing , Micro-Electrical-Mechanical Systems/methods , Nanocapsules/ultrastructure , Protein Binding , Protein Interaction Mapping/methods , Surface Properties , Tensile Strength
17.
Macromol Biosci ; 14(5): 709-19, 2014 May.
Article in English | MEDLINE | ID: mdl-24469965

ABSTRACT

The development of novel xyloglucan-block-poly(ϵ-caprolactone) (XGO-b-PCL) nanoparticles coated with the mucoadhesive polysaccharide chitosan is described. XGO-b-PCL nanoparticles show monodisperse size distribution (Rh = 50 nm). Curcumin is successfully encapsulated within the PCL core within drug to polymer ratio of 1:5 (w/w). The coating of nanoparticles with chitosan results in an increased particle size and positive surface charge due to the polycation nature of the chitosan. Mucoadhesive properties of chitosan-coated nanoparticles are demonstrated by its exceptional ability to interact with mucin through electrostatic forces. Finally, in vitro studies show that curcumin-loaded nanoparticles exhibit higher cytotoxic effects against B16F10 melanoma cells than L929 fibroblast cells.


Subject(s)
Adhesives/chemistry , Biocompatible Materials/chemical synthesis , Chitosan/chemistry , Drug Delivery Systems/methods , Glucans/chemistry , Nanoparticles/chemistry , Polyesters/chemistry , Xylans/chemistry , Apoptosis/drug effects , Biocompatible Materials/chemistry , Curcumin/administration & dosage , Curcumin/chemistry , Curcumin/pharmacology , Microscopy, Electron, Transmission , Microscopy, Fluorescence , Models, Molecular , Molecular Structure , Surface Plasmon Resonance
18.
J Colloid Interface Sci ; 370(1): 58-66, 2012 Mar 15.
Article in English | MEDLINE | ID: mdl-22284577

ABSTRACT

Polycaprolactone (PCL) nanoparticles decorated with a mucoadhesive polysaccharide chitosan (CS) containing curcumin were developed aiming the buccal delivery of this drug. These nanoparticles were prepared by the nanoprecipitation method using different molar masses and concentrations of chitosan and concentrations of triblock surfactant poloxamer (PEO-PPO-PEO), in order to optimize the preparation conditions. Chitosan-coated nanoparticles showed positive surface charge and a mean particle radius ranging between 114 and 125 nm, confirming the decoration of the nanoparticles with the mucoadhesive polymer, through hydrogen bonds between ether and amino groups from PEO and CS, respectively. Dynamic Light Scattering (DLS) studies at different scattering angles and concentrations have shown that the nanoparticles are monodisperse (polydispersity indices were lower than 0.3). The nanoparticle systems were also examined with Nanoparticle Tracking Analysis (NTA), and the results were in good agreement with those obtained by DLS. Colloidal systems showed mean drug content about 460 µg/mL and encapsulation efficiency higher than 99%. Finally, when coated with chitosan, these nanoparticles show a great ability to interact with mucin indicating also their suitability for mucoadhesive applications.


Subject(s)
Chitosan/chemistry , Curcumin/chemistry , Drug Carriers/chemistry , Nanoparticles/chemistry , Administration, Buccal , Curcumin/administration & dosage , Light , Mucins/chemistry , Mucoproteins/chemistry , Particle Size , Polyethylene Glycols/chemistry , Propylene Glycols/chemistry , Scattering, Radiation , Surface Properties
19.
J Biomed Nanotechnol ; 7(3): 406-14, 2011 Jun.
Article in English | MEDLINE | ID: mdl-21830481

ABSTRACT

Curcumin is a polyphenol obtained from the plant Curcuma longa (called turmeric) that displays several pharmacological activities, including anti-inflammatory, antioxidant, antimicrobial and antitumoral activity, but clinical use has been limited by its poor solubility in water and, consequently, minimal systemic bioavailability. We have therefore formulated the drug into nanocarrier systems in an attempt to improve its therapeutic properties. This study evaluates the effect of intraperitoneally administered nanocapsules containing curcumin on subcutaneous melanoma in mice inoculated with B16-F10 cells, and on the cytotoxicity activity against B16-F10 cells in vitro. Phagocytic uptake of formulations was also evaluated upon incubation with macrophage J774 cells by fluorescence microscopy. Lipid and polymeric nanocapsules were prepared by the phase inversion and nanoprecipitation methods, respectively. The uptake of the lipid nanocapsules prepared using Solutol HS15 was significantly reduced in J774 cells. Curcumin, as free drug or as drug-loaded nanocapsules, was administrated at a dose of 6 mg/kg twice a week for 21 days. Free drug and curcumin-loaded nanocapsules significantly reduced tumor volume (P < 0.05 vs. control), but no difference was found in the antitumor activity displayed by lipid and polymeric nanocapsules. This assumption was supported by the in vitro study, in which free curcumin as well as loaded into nanocapsules caused significant reduction of cell viability in a concentration- and time-dependent manner.


Subject(s)
Curcumin/pharmacology , Macrophages/drug effects , Macrophages/metabolism , Nanocapsules , Surface-Active Agents , Animals , Biological Transport/drug effects , Cell Line, Tumor , Curcumin/pharmacokinetics , Curcumin/therapeutic use , Drug Stability , Ions , Liposomes , Macrophages/immunology , Melanoma, Experimental/drug therapy , Mice , Mice, Inbred C57BL , Nanocapsules/chemistry , Particle Size , Surface-Active Agents/chemistry
20.
Braz. j. pharm. sci ; 46(2): 219-226, Apr.-June 2010. ilus, tab
Article in English | LILACS | ID: lil-564888

ABSTRACT

A simple, rapid, and sensitive fluorimetric method was developed and validated to quantify curcumin in lipid and polymeric nanocapsule suspensions, using acetonitrile as a solvent. The excitation and emission wavelengths were set at 397 nm and 508 nm, respectively. The calibration graph was linear from 0.1 to 0.6 µg/mL with a correlation coefficient of 0.9982. The detection and quantitation limits were 0.03 and 0.10 µg/mL, respectively. The validation results confirmed that the developed method is specific, linear, accurate, and precise for its intended use. The current method was successfully applied to the evaluation of curcumin content in lipid and polymeric nanocapsule suspensions during the early stage of formulation development.


Um método fluorimétrico simples, rápido e sensível foi desenvolvido e validado para quantificação da curcumina em suspensões de nanocápsulas lipídicas e poliméricas, usando acetonitrila como solvente. Os comprimentos de onda de excitação e emissão foram 397 nm e 508 nm, respectivamente. Nas condições testadas, a curva de calibração demonstrou-se linear na faixa de 0,1 a 0,6 µg/mL, exibindo coeficiente de correlação de 0,9982. Os limites de detecção e quantificação foram 0,03 e 0,10 µg/mL, respectivamente. Os resultados da validação confirmaram que o método desenvolvido é específico, linear, exato e preciso para o uso proposto. O presente método foi aplicado com sucesso para a avaliação do teor de curcumina nas suspensões de nanocápsulas lipídicas e poliméricas durante o estágio inicial do desenvolvimento da formulação.


Subject(s)
Curcumin , Diagnosis , Experimental Development , Fluorometry , Lipids , Methods , Nanocapsules , Evaluation Studies as Topic
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