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1.
Int J Biol Macromol ; 275(Pt 1): 133588, 2024 Jul 02.
Article in English | MEDLINE | ID: mdl-38960246

ABSTRACT

The understanding of cancer immunity and antitumor factors generated by natural polysaccharides is not yet fully comprehended. Polysaccharides, like cashew gum (CG), can exhibit immunomodulatory action and may assist in the antitumor process and side effects relieve. This study aimed to determine the antitumor effect of CG alone or in combination with cyclophosphamide (CTX), and its interactions with immune cells, in a murine melanoma model, using the B16-F10 cell line. Tumor growth inhibition, hematological, histopathological, ELISA, flow cytometry, immunofluorescence, and qRT-PCR analyses were performed to elucidate the antitumor potential, involvement of immune cells, and potential toxic effects. CG showed significant tumor growth inhibition, reaching up to 42.9 % alone and 51.4 % in combination with CTX, with mild toxicity to organs. CG enhanced leukocyte count, even in the presence of CTX. Furthermore, CG influenced the activation of tumor-associated macrophages (TAM), characterized by an increase in Il4, as well as a reduction in Ifng, Il1b, Tgfb, and Il6 gene expression. Nevertheless, these effects did not compromise the antitumor activity of CG. In summary, the combination of CG with CTX is a promising approach for leukopenia, one of the most important side effects of cancer treatment and deserves further investigation.

2.
Carbohydr Polym ; 342: 122356, 2024 Oct 15.
Article in English | MEDLINE | ID: mdl-39048219

ABSTRACT

In this study, we report the synthesis and characterization of pH-responsive nanoconjugates for targeted drug delivery. Galactomannan extracted from D. regia seeds was oxidized to form aldehyde groups, achieving a percentage of oxidation of 25.6 %. The resulting oxidized galactomannan (GMOX) was then copolymerized with PINIPAm-NH2, yielding a copolymer. The copolymer exhibited signals from both GMOX and PNIPAm-NH2 in its NMR spectrum, confirming successful copolymerization. Critical association concentration (CAC) studies revealed the formation of nanostructures, with lower CAC values observed at higher temperatures. The copolymer and GMOX reacted with doxorubicin (DOX), resulting in nanoconjugates with controlled drug release profiles, especially under acidic conditions similar to tumor microenvironments. Cytotoxicity assays demonstrated significant efficacy of the nanoconjugates against melanoma cells with reduced toxicity towards healthy cells. These findings underscore the potential of the pH-responsive nanoconjugates as promising candidates for targeted cancer therapy, offering improved therapeutic efficacy and reduced systemic side effects.


Subject(s)
Doxorubicin , Galactose , Mannans , Nanoconjugates , Doxorubicin/pharmacology , Doxorubicin/chemistry , Mannans/chemistry , Mannans/pharmacology , Galactose/chemistry , Galactose/analogs & derivatives , Humans , Nanoconjugates/chemistry , Hydrogen-Ion Concentration , Drug Liberation , Cell Line, Tumor , Drug Carriers/chemistry , Cell Survival/drug effects , Antibiotics, Antineoplastic/pharmacology , Antibiotics, Antineoplastic/chemistry , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology
3.
Int J Biol Macromol ; 274(Pt 2): 133048, 2024 Jun 08.
Article in English | MEDLINE | ID: mdl-38857734

ABSTRACT

Epiisopiloturine (EPI) is a compound found in jaborandi leaves with antiparasitic activity, which can be enhanced when incorporated into nanoparticles (NP). Cashew Gum (CG), modified by carboxymethylation, is used to produce polymeric nanomaterials with biological activity. In this study, we investigated the antimicrobial potential of carboxymethylated CG (CCG) NP containing EPI (NPCCGE) and without the alkaloid (NPCCG) against bacteria and parasites of the genus Leishmania. We conducted theoretical studies, carboxymethylated CG, synthesized NP by nanoprecipitation, characterized them, and tested them in vitro. Theoretical studies confirmed the stability of modified carbohydrates and showed that the EPI-4A30 complex had the best interaction energy (-8.47 kcal/mol). CCG was confirmed by FT-IR and presented DSabs of 0.23. NPCCG and NPCCGE had average sizes of 221.94 ± 144.086 nm and 247.36 ± 3.827 nm, respectively, with homogeneous distribution and uniform surfaces. No NP showed antibacterial activity or cytotoxicity to macrophages. NPCCGE demonstrated antileishmanial activity against L. amazonensis, both in promastigote forms (IC50 = 9.52 µg/mL, SI = 42.01) and axenic amastigote forms (EC50 = 6.6 µg/mL, SI = 60.60). The results suggest that nanostructuring EPI in CCG enhances its antileishmanial activity.

4.
Chem Biol Interact ; 398: 111115, 2024 Aug 01.
Article in English | MEDLINE | ID: mdl-38908811

ABSTRACT

In the present study, the effect of sulfonamide-chalcone 185 (SSC185) was investigated against B16-F10 metastatic melanoma cells aggressive actions, besides migration and adhesion processes, by in silico and in vitro assays. In silico studies were used to characterize the pharmacokinetic profile and possible targets of SSC185, using the pkCSM web server, and docking simulations with AutoDock Tools. Furthermore, the antimetastatic effect of SSC185 was investigated by in vitro experiments using MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide), colony, scratch, and cell adhesion assays, and atomic force microscopy (AFM). The molecular docking results show better affinity of SSC185 with the metalloproteinases-2 (MMP-2) and α5ß1 integrin. SSC185 effectively restricts the formation of colonies, migration, and adhesion of B16-F10 metastatic melanoma cells. Through the AFM images changes in cells morphology was identified, with a decrease in the filopodia and increase in the average cellular roughness. The results obtained demonstrate the potential of this molecule in inhibit the primordial steps for metastasis, which is responsible for a worse prognosis of late stage cancer, being the main cause of morbidity among cancer patients.


Subject(s)
Cell Adhesion , Cell Movement , Chalcone , Molecular Docking Simulation , Sulfonamides , Cell Movement/drug effects , Cell Adhesion/drug effects , Sulfonamides/pharmacology , Sulfonamides/chemistry , Mice , Animals , Cell Line, Tumor , Chalcone/pharmacology , Chalcone/chemistry , Chalcone/analogs & derivatives , Matrix Metalloproteinase 2/metabolism , Melanoma, Experimental/pathology , Melanoma, Experimental/drug therapy , Melanoma, Experimental/metabolism , Microscopy, Atomic Force , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry , Chalcones/pharmacology , Chalcones/chemistry , Humans
5.
Int J Biol Macromol ; 268(Pt 1): 131661, 2024 May.
Article in English | MEDLINE | ID: mdl-38641286

ABSTRACT

In this study, two nanoemulsions were formulated with essential oil (EO) of Ocimum gratissimum with (EON) or without (EOE) cashew gum (CG). Subsequently, inhibition of melanosis and preservation of the quality of shrimp stored for 16 days at 4 ± 0.5 °C were evaluated. A computational approach was performed to predict the system interactions. Dynamic light scattering (DLS) and atomic force microscopy (AFM) were used for nanoparticle analysis. Gas chromatography and flame ionization detector (GC-FID) determined the chemical composition of the EO constituents. Shrimps were evaluated according to melanosis's appearance, psychrotrophic bacteria's count, pH, total volatile basic nitrogen, and thiobarbituric acid reactive substances. EON exhibited a particle size three times smaller than EOE. The shrimp treated with EON showed a more pronounced sensory inhibition of melanosis, which was considered mild by the 16th day. Meanwhile, in the other groups, melanosis was moderate (EOE) or severe (untreated group). Both EON and EOE treatments exhibited inhibition of psychrotrophic bacteria and demonstrated the potential to prevent lipid oxidation, thus extending the shelf life compared to untreated fresh shrimp. EON with cashew gum, seems more promising due to its physicochemical characteristics and superior sensory performance in inhibiting melanosis during shrimp preservation.


Subject(s)
Anacardium , Ocimum , Oils, Volatile , Animals , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Ocimum/chemistry , Anacardium/chemistry , Penaeidae/chemistry , Plant Gums/chemistry , Food Preservation/methods
6.
J Pharm Pharmacol ; 76(6): 732-742, 2024 Jun 06.
Article in English | MEDLINE | ID: mdl-38546507

ABSTRACT

OBJECTIVES: Angico gum (AG) (Anadenanthera colubrina var. Cebil [Griseb.] Altschul) is utilized by some Brazilian communities to alleviate symptoms from gastroesophageal reflux disease. Here, we aimed to investigate the "in vitro" topical protective capacity of AG on human esophageal mucosa. METHODS: Biopsies of the distal esophageal mucosa were collected from 35 patients with heartburn (24 non-erosive and 11 with erosive oesophagitis (EE)) and mounted in Üssing chambers. AG was applied topically, followed by exposure with acid solution (pH 2.0 or pH 1.0), where transepithelial electrical resistance (TER) and The transepithelial permeability for fluorescein was assessed. The incubation of the AG labeled with FITC in the esophageal mucosa was localized by fluorescence microscopy. KEY FINDINGS: Pretreatment with AG prevented the drop in TER induced by acid solution, as well as significantly decreases the fluorescein permeability in non-erosive patients. The protective effect of AG was sustained for up to 120 min both in biopsies of non-erosive and erosive esophagitis. Confocal microscope images showed mucosal luminal adherence of FITC-labeled AG. CONCLUSION: AG had a prolonged topical protective effect against acid solution in mucosal biopsies of patients with non-erosive and erosive esophagitis.


Subject(s)
Esophageal Mucosa , Gastroesophageal Reflux , Humans , Gastroesophageal Reflux/drug therapy , Gastroesophageal Reflux/prevention & control , Esophageal Mucosa/drug effects , Esophageal Mucosa/pathology , Esophageal Mucosa/metabolism , Male , Female , Middle Aged , Adult , Permeability , Electric Impedance , Administration, Topical , Biopolymers , Aged , Fluorescein/administration & dosage , Esophagus/drug effects , Esophagus/pathology , Esophagus/metabolism , Heartburn/drug therapy , Heartburn/prevention & control , Clinical Relevance
7.
Int J Biol Macromol ; 260(Pt 1): 129397, 2024 Mar.
Article in English | MEDLINE | ID: mdl-38219933

ABSTRACT

Biotechnological advancements require the physicochemical alteration of molecules to enhance their biological efficacy for the effective treatment of gastric ulcers. The study aimed to produce a polyelectrolytic compound from red angico gum (AG) by carboxymethylation, evaluate its physicochemical characteristics and investigate gastric protection against ethanol-induced ulcers. AG and carboxymethylated angico gum (CAG) were characterized by Fourier transform infrared spectroscopy, determination of the degree of substitution and gel permeation chromatography (GPC) and 13C NMR techniques. The results demonstrated that the modification of the polymer was satisfactory, presenting conformational changes e improving the interaction with the gastric mucosa. AG and CAG reduced macroscopic and microscopic damage such as edema, hemorrhage and cell loss caused by exposure of the mucosa to alcohol. Both demonstrated antioxidant activity in vitro, and in vivo, pretreatment with gums led to the restoration of superoxide dismutase and glutathione levels compared to the injured group. Concurrently, the levels of malondialdehyde and nitrite decreased. Atomic force microscopy showed that CAG presented better conformational properties of affinity and protection with the gastric mucosa compared to AG in the acidic pH. Based on our findings, it is suggested that this compound holds promise as a prospective product for future biotechnological applications.


Subject(s)
Colubrina , Fabaceae , Stomach Ulcer , Prospective Studies , Stomach , Antioxidants/adverse effects , Gastric Mucosa , Stomach Ulcer/chemically induced , Stomach Ulcer/drug therapy , Plant Extracts/chemistry
8.
Int J Biol Macromol ; 253(Pt 6): 127281, 2023 Dec 31.
Article in English | MEDLINE | ID: mdl-37806422

ABSTRACT

Hydrogels made with depolymerized guar gum, oxidized with theoretical oxidation degrees of 20, 35 and 50 %, were obtained via Schiff's base reaction with N-succinyl chitosan. The materials obtained were subjected to characterization by FT-IR, rheology, swelling, degradation, and morphology. Additionally, their gelation time categorized all three hydrogels as injectable. The materials' swelling degrees in Phosphate-Buffered Saline (PBS) were in the range of 26-35 g of fluid/g gel and their pore size distribution was heterogeneous, with pores varying from 67 to 93 µm. All hydrogels degraded in PBS solution, but maintained around 40 % of their initial mass after 28 days, which was more than enough time for wound healing. The biomaterials were also flexible, self-repairing, adhesive and cytocompatible and presented intrinsic actions, regardless of the presence of additives or antibiotics, against gram-positive (Staphylococcus aureus, Staphylococcus epidermidis) and gram-negative bacteria (Escherichia coli). However, the most pronounced bactericidal effect was against resistant Staphylococcus aureus - MRSA. In vivo assays, performed with 50 % oxidized gum gel, demonstrated that this material exerted anti-inflammatory effects, accelerating the healing process and restoring tissues by approximately 99 % within 14 days. In conclusion, these hydrogels have unique characteristics, making them excellent candidates for wound-healing dressings.


Subject(s)
Chitosan , Methicillin-Resistant Staphylococcus aureus , Hydrogels/pharmacology , Chitosan/pharmacology , Spectroscopy, Fourier Transform Infrared , Bandages , Bacteria , Anti-Bacterial Agents/pharmacology , Staphylococcus aureus
9.
Polymers (Basel) ; 15(13)2023 Jun 28.
Article in English | MEDLINE | ID: mdl-37447501

ABSTRACT

Tree-exuded gums are natural polymers that represent an abundant raw material in the food and pharmaceutical industries. The cashew gum can be obtained by exudation of trees of the genus Anacardium, a native species of the Brazilian northeast; its polymer consists of monosaccharide units propitious to the action of chemical reactions that tend to improve their intrinsic characteristics among them, as the degree of hydro-solubility. The objective of this work was to modify the exudate gum of Anacardium occidentale (cashew gum (CG)) through an amine reaction. The modification was confirmed by Nuclear Magnetic Resonance (1H NMR), infrared spectroscopy (FTIR), gel permeation chromatography (GPC), zeta potential, and thermogravimetric analysis (TG). In addition, the chemical modification altered the molar mass and surface charge of the CG, and the amino group binding to the CG polymers was confirmed by FTIR spectra. In addition, cytotoxicity tests were performed where cell viability was estimated by an MTT assay on RAW 264.7 macrophages. Through these tests, it was found that the amine caused an increase in the thermal stability of the amino compounds and did not present cytotoxic potential at concentrations below 50.0 mg/L.

10.
Int J Biol Macromol ; 243: 125254, 2023 Jul 15.
Article in English | MEDLINE | ID: mdl-37295699

ABSTRACT

The present work explores the esterification reaction in the polysaccharide extracted from the seaweed Gracilaria birdiae and investigates its antioxidant potential. The reaction process was conducted with phthalic anhydride at different reaction times (10, 20 and 30 min), using a molar ratio of 1:2 (polymer: phthalic anhydride). Derivatives were characterized by FTIR, TGA, DSC and XRD. The biological properties of derivatives were investigated by assays of cytotoxicity and antioxidant activity (2,2-diphenyl-1-picrylhydroxyl - DPPH and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt - ABTS). The results obtained by FT-IR confirmed the chemical modification, there was a reduction related to the presence of carbonyl and hydroxyl groups when compared to the in nature polysaccharide spectrum. TGA analysis showed a change in the thermal behavior of the modified materials. X-ray diffraction, it was shown that the in nature polysaccharide appeared as an amorphous material, while the material obtained after the chemical modification process had increased crystallinity, due to the introduction of phthalate groups. For the biological assays, it was observed that the phthalate derivative was more selective than the unmodified material for the murine metastatic melanoma tumor cell line (B16F10), revealing a good antioxidant profile for DPPH and ABTS radicals.


Subject(s)
Antineoplastic Agents , Gracilaria , Animals , Mice , Antioxidants/chemistry , Phthalic Anhydrides , Galactans , Spectroscopy, Fourier Transform Infrared , Antineoplastic Agents/chemistry , Polysaccharides/chemistry
11.
Pharmaceuticals (Basel) ; 16(2)2023 Feb 10.
Article in English | MEDLINE | ID: mdl-37259411

ABSTRACT

Hydrogels are structures that have value for application in the area of tissue engineering because they mimic the extracellular matrix. Naturally obtained polysaccharides, such as chitosan (CH) and cashew gum, are materials with the ability to form polymeric networks due to their physicochemical properties. This research aimed to develop a scaffold based on chitosan and phthalated cashew tree gum and test it as a support for the growth of human mesenchymal stem cells. In this study, phthalation in cashew gum (PCG) was performed by using a solvent-free route. PCG-CH scaffold was developed by polyelectrolyte complexation, and its ability to support adherent stem cell growth was evaluated. The scaffold showed a high swelling rate. The pore sizes of the scaffold were analyzed by scanning electron microscopy. Human dental pulp stem cells (hDPSCs) were isolated, expanded, and characterized for their potential to differentiate into mesenchymal lineages and for their immunophenotypic profile. Isolated mesenchymal stem cells presented fibroblastoid morphology, plastic adhesion capacity, and differentiation in osteogenic, adipogenic, and chondrogenic lineages. Mesenchymal stem cells were cultured in scaffolds to assess cell adhesion and growth. The cells seeded on the scaffold showed typical morphology, attachment, and adequate distribution inside the matrix pores. Thus, cells seeded in the scaffold may improve the osteoinductive and osteoconductive properties of these biomaterials.

12.
Polymers (Basel) ; 15(11)2023 May 23.
Article in English | MEDLINE | ID: mdl-37299211

ABSTRACT

The incorporation of polymeric components into aerogels based on clay produces a significant improvement in the physical and thermal properties of the aerogels. In this study, clay-based aerogels were produced from a ball clay by incorporation of angico gum and sodium alginate using a simple, ecologically acceptable mixing method and freeze-drying. The compression test showed a low density of spongy material. In addition, both the compressive strength and the Young's modulus of elasticity of the aerogels showed a progression associated to the decrease in pH. The microstructural characteristics of the aerogels were investigated by X-ray diffraction (XRD) and scanning electron microscopy (SEM). The chemical structure was studied by infrared spectroscopy with Fourier transform (FTIR). The TGA curves from a non-oxidizing atmosphere indicated that the clay had a mass loss of 9% above 500 °C and that due to the presence of polysaccharides, the aerogels presented a decomposition of 20% at temperatures above 260 °C. The DSC curves of the aerogels demonstrated a displacement in higher temperatures. In conclusion, the results showed that aerogels of ball clay with the incorporation of polysaccharides, which are still minimally studied, have potential application as thermal insulation considering the mechanical and thermal results obtained.

13.
Int J Biol Macromol ; 232: 123058, 2023 Mar 31.
Article in English | MEDLINE | ID: mdl-36669633

ABSTRACT

Lemon gum (LG) obtained from Citrus × latifolia in Brazil was isolated and characterized. In addition, gum biocompatibility was evaluated in vitro and in vivo by Galleria mellonella and mice model. The cytotoxicity against tumor cells was also evaluated. The ratio of arabinose:galactose: rhamnose:4-OMe-glucuronic acid was 1:0.65:0.06:0.15. Small traces of protein were detected, emphasizing the isolate purity. Molar mass was 8.08 × 105 g/mol, with three different degradation events. LG showed antiproliferative activity against human prostate adenocarcinoma cancer cells, with percentage superior to 50 %. In vivo toxicity models demonstrated that LG is biocompatible polymer, with little difference in the parameters compared to control group. These results demonstrate advance in the study of LG composition and toxicity, indicating a potential for several biomedical and biotechnological future applications.


Subject(s)
Adenocarcinoma , Citrus , Male , Animals , Mice , Humans , Prostate , Galactans , Adenocarcinoma/drug therapy
14.
Int J Biol Macromol ; 230: 123272, 2023 Mar 01.
Article in English | MEDLINE | ID: mdl-36649864

ABSTRACT

Nanotechnology is a crucial technology in recent years has resulted in new and creative applications of nanomedicine. Polymeric nanoparticles have increasing demands in pharmaceutical applications and require high reproducibility, homogeneity, and control over their properties. Work explores the use of cashew phthalate gum (PCG) as a particle-forming polymer. PCG exhibited a pH-sensitive behavior due to the of acid groups on its chains, and control drug release. We report the development of nanoparticles carrying benznidazole. Formulations were characterized by DLS, encapsulation efficiency, drug loading, FTIR, pH-responsive behavior, release, and in vitro kinetics. Interaction between polymer and drug was an evaluated by molecular dynamics. Morphology was observed by SEM, and in vitro cytotoxicity by MTT assay. Trypanocidal effect for epimastigote and trypomastigote forms was also evaluated. NPs responded to the slightly basic pH, triggering the release of BNZ. In acidic medium, they presented small size, spherical shape, and good stability. It was indicated NP with enhanced biological activity, reduced cytotoxicity, high anti T. cruzi performance, and pH-sensitive release. This work investigated properties related to the development and enhancement of nanoparticles. PCG has specific physicochemical properties that make it a promising alternative to drug delivery, however, there are still challenges to be overcome.


Subject(s)
Anacardium , Nanoparticles , Trypanosoma cruzi , Reproducibility of Results , Nanoparticles/chemistry , Drug Liberation , Polymers/pharmacology , Hydrogen-Ion Concentration , Drug Carriers/pharmacology
15.
Laryngoscope ; 133(1): 162-168, 2023 01.
Article in English | MEDLINE | ID: mdl-35258096

ABSTRACT

OBJECTIVE: This study aimed to evaluate the in vivo protective effect of the angico gum biopolymer in reducing the inflammatory response and preserving the integrity of the laryngeal and esophageal mucosa. STUDY DESIGN: Animal study. METHODS: A murine surgical model of gastroesophageal reflux disease was accomplished and subsequently treated with angico gum or omeprazole. On days 3 and 7 post surgery, samples of the larynx and esophagus, respectively, were collected to measure the level of inflammation (wet weight and myeloperoxidase activity) and mucosal integrity (transepithelial electrical resistance and mucosal permeability to fluorescein). RESULTS: Angico gum and omeprazole decreased laryngeal inflammation (wet weight and myeloperoxidase activity) and dramatically improved the integrity of the laryngeal mucosa. It also reduced inflammation (decreased wet weight and myeloperoxidase activity) of the esophagus and preserved the barrier function (inferred by assessing the integrity of the mucosa). CONCLUSION: This study demonstrates the protective effect of angico gum in an experimental gastroesophageal reflux disease model. Angico gum attenuates inflammation and impairment of the mucosal barrier function not only in the larynx but also in the esophagus. LEVEL OF EVIDENCE: NA Laryngoscope, 133:162-168, 2023.


Subject(s)
Esophageal Mucosa , Gastroesophageal Reflux , Mice , Animals , Gastroesophageal Reflux/drug therapy , Electric Impedance , Mucous Membrane , Disease Models, Animal
16.
Polymers (Basel) ; 14(18)2022 Sep 09.
Article in English | MEDLINE | ID: mdl-36145923

ABSTRACT

Rigid polyurethane foams were prepared by the one-step expandable foam method using casting molding followed by forming clay-based composites. Polyurethane/vermiculite foam composites (PU/VMT) were controlled based on adding the percentage of clay in the formulation. The effects of composite modifications were evaluated by X-ray diffraction (XRD), thermogravimetric analysis (TG/DTG), and scanning electron microscopy (SEM/EDS) applied to the flame retardancy explored by the vertical burn test. The results indicated that adding clay controlled the particle size concerning polyurethane (PU) foams. However, they exhibited spherical structures with closed cells with relatively uniform distribution. XRD analysis showed the peaks defined at 2θ = 18° and 2θ = 73° relative to the crystallinity in formation and interaction of rigid segments were identified, as well as the influence of crystallinity reduction in composites. In the flame test, the flame retardant surface was successful in all composites, given the success of the dispersibility and planar orientation of the clay layers and the existence of an ideal content of vermiculite (VMT) incorporated in the foam matrix.

17.
AAPS PharmSciTech ; 23(6): 212, 2022 Aug 02.
Article in English | MEDLINE | ID: mdl-35918472

ABSTRACT

Squamous cell carcinoma (SCC) represents 20% of cases of non-melanoma skin cancer, and the most common treatment is the removal of the tumor, which can leave large scars. 5-Fluorouracil (5FU) is a drug used in the treatment of SCC, but it is highly hydrophilic, resulting in poor skin penetration in topical treatment. Some strategies can be used to increase the cutaneous penetration of the drug, such as the combination of liposomes containing penetration enhancers, for instance, surfactants, associated with the use of microneedling. Thus, the present work addresses the development of liposomes with penetration enhancers, such as sorbtitan monolaurate, span 20, for topical application of 5-FU and associated or not with the use of microneedling for skin delivery. Liposomes were developed using the lipid film hydration, resulting in particle size, polydispersity index, zeta potential, and 5-FU encapsulation efficiency of 88.08 nm, 0.169, -12.3 mV, and 50.20%, respectively. The presence of span 20 in liposomes potentiated the in vitro release of 5-FU. MTT assay was employed for cytotoxicity evaluation and the IC50 values were 0.62, 30.52, and 24.65 µM for liposomes with and without span 20 and 5-FU solution, respectively after 72-h treatment. Flow cytometry and confocal microscopy analysis evidenced high cell uptake for the formulations. In skin penetration studies, a higher concentration of 5-FU was observed in the epidermis + dermis, corresponding to 1997.71, 1842.20, and 2585.49 ng/cm2 in the passive penetration and 3214.07, 2342.84, and 5018.05 ng/cm2 after pretreatment with microneedles, for solution, liposome without and with span 20, respectively. Therefore, herein, we developed a nanoformulation for 5-FU delivery, with suitable physicochemical characteristics, potent skin cancer cytotoxicity, and cellular uptake. Span 20-based liposomes increased the skin penetration of 5-FU in association of microneedling. Altogether, the results shown herein evidenced the potential of the liposome containing span 20 for topical delivery of 5-FU.


Subject(s)
Fluorouracil , Skin Neoplasms , Hexoses , Humans , Liposomes/metabolism , Particle Size , Skin/metabolism , Skin Absorption , Skin Neoplasms/drug therapy , Skin Neoplasms/metabolism
18.
Biosens Bioelectron ; 210: 114211, 2022 Aug 15.
Article in English | MEDLINE | ID: mdl-35468419

ABSTRACT

Composite materials have gained significant attention owing to the synergistic effects of their constituent materials, thereby facilitating their utilization in new applications or in improving the existing ones. In this study, a composite based on nickel phthalocyanine (NiTsPc), zinc oxide nanoparticles (ZnONPs), and carbon nanotubes (CNT) was developed and subsequently immobilized on a pyrolytic graphite electrode (PGE). The PGE/NiTsPc-ZnONPs-CNT was identified as a selective catalytic hybrid system for detection of neurotransmitter dopamine (DA). The electrochemical and morphological characterizations were conducted using atomic force microscopy (AFM). Chronoamperometry and differential pulse voltammetry (DPV) were used to detect DA and detection limits of 24 nM and 7.0 nM was found, respectively. In addition, the effects of some possible DA interferents, such as ascorbic acid, uric acid, and serotonin, on DA response were evaluated. Their presence did not show significant variations in the DA electrochemical response. The high specificity and sensitivity of PGE/NiTsPc-ZnONPs-CNT for DA enabled its direct detection in human serum without sample pretreatment as well as in DA-enriched serum samples, whose recovery levels were close to 100%, thereby confirming the effectiveness of the proposed method. In general, PGE/NiTsPc-ZnONPs-CNT is a promising candidate for future applications in clinical diagnosis.


Subject(s)
Biosensing Techniques , Graphite , Nanoparticles , Nanotubes, Carbon , Zinc Oxide , Humans , Ascorbic Acid/chemistry , Dopamine/chemistry , Electrochemical Techniques/methods , Electrodes , Graphite/chemistry , Indoles , Isoindoles , Nanoparticles/chemistry , Nanotubes, Carbon/chemistry , Nickel
19.
Int J Biol Macromol ; 193(Pt A): 450-456, 2021 Dec 15.
Article in English | MEDLINE | ID: mdl-34688680

ABSTRACT

Enoxaparin is an effective biological molecule for prevention and treatment of coagulation disorders. However, it is poorly absorbed in the gastrointestinal tract. In this study, we developed an Eudragit® L100 coated chitosan core shell nanoparticles for enoxaparin oral delivery (Eud/CS/Enox NPs) through a completely eco-friendly method without employing any high-energy homogenizer technique and any organic solvents. Spherical nanocarriers were successfully prepared with particle size lower than 300 nm, polydispersity index about 0.12 and zeta potential higher than +25 mV, entrapment efficiency greater than 95% and the in vitro release behavior confirms the good colloidal stability and the successful Eudragit® L100 coating process demonstrated by negligible cumulative enoxaparin release (<10%) when the particles are submitted to simulated gastric fluid conditions. Finally, we demonstrated that the core-shell structure of the particle influenced the drug release mechanism of the formulations, indicating the presence of the Eudragit® L100 on the surface of the particles. These results suggested that enteric-coating approach and drug delivery nanotechnology can be successfully explored as potential tools for oral delivery of enoxaparin.


Subject(s)
Chitosan/chemistry , Drug Carriers/chemistry , Enoxaparin/chemistry , Nanoparticles/chemistry , Drug Liberation , Particle Size
20.
Int J Biol Macromol ; 193(Pt A): 100-108, 2021 Dec 15.
Article in English | MEDLINE | ID: mdl-34627848

ABSTRACT

In this study, nanoemulsions of essential oil from Ocimumgratissimum (Linn) (EO) were produced using low and high energy techniques using cashew gum (CG) as a co-surfactant. The main constituents of the EO were determined by Gas Chromatography coupled with Mass Spectrometry (GC-MS), and their presence in the EO and in the formulations verified by Fourier Transform Infrared Spectroscopy (FTIR) and UV-visible spectrophotometry was observed the encapsulation efficiency (EE%), with colloidal stability. Nuclear magnetic resonance (NMR) was used to study cashew gum. Dynamic light scattering analysis (DLS) determined the nanoemulsion Z means, polydispersity index and the Zeta potential value, nanoparticle tracking analysis (NTA) were determined. The nanostructured EO showed better antibacterial action against the pathogenic gastroenteritis species Staphylococcus aureus, Escherichia coli and Salmonella enterica when compared to free EO. Atomic Force Microscopy (AFM) was used for morphological analysis of the nanoparticle and study of the action of the nanoemulsion through images of the cellular morphology of S. enterica. The antioxidant activity was evaluated against the ABTS radical (2,2'-azino-bis diazonium salt (3-ethylbenzothiazoline-6-sulfonic acid)). The encapsulation of EO in a nanostructured system improved its antibacterial and antioxidant activity, the low energy synthesis showed greater storage stability, remaining stable for 37 days.


Subject(s)
Anti-Bacterial Agents/chemistry , Emulsions/chemistry , Ocimum/metabolism , Oils, Volatile/chemistry , Plant Gums/chemistry , Plant Leaves/metabolism
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