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1.
Int J Biol Macromol ; 254(Pt 2): 127916, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37944740

RESUMO

Mucilage of C. pareira leaves was utilized, being manufactured for use in pharmaceutical products. Carrageenan and Eudragit® NE30D were used to combined. Glycerin was used as a plasticizer at a concentration of 20 % w/w based on the amount of polymer used. Computer software optimized its characteristics, including tensile properties, moisture uptake, and erosion; the optimal formulation was 1.4:1.2:2.8. The percentages of optimization error ranged from 8.48 to 13.80 %. Propranolol HCl was mixed to an optimal formulation. The film layer was tight, homogeneous, and smooth, with no holes. DSC thermogram showed no interaction peaks at 101.33 °C and 170.50 °C. Propranolol HCl concentration in the film ranged from 2.18 to 2.20 mg/cm2. Propranolol HCl was quickly released from the film. The kinetic model for the release profile was first-order kinetic. Although propranolol HCl had a high-release profile, its skin permeation was limited. The permeation lag time, Jss, and Kp were 1.60-2.65 h, 0.0182-0.0338 µg/cm2/h, and 9.10-15.35 cm/h, respectively. A significant amount of propranolol HCl residue was found on the skin's surface. Glycerin appeared to influence propranolol HCl permeability. Therefore, the plant leaf mucilage/carrageenan/Eudragit® NE30D blended film can be utilized in pharmaceutical applications to control drug release from its film layer.


Assuntos
Mucilagem Vegetal , Carragenina , Propranolol/química , Química Farmacêutica , Glicerol , Preparações Farmacêuticas
2.
Pharmaceutics ; 15(11)2023 Nov 08.
Artigo em Inglês | MEDLINE | ID: mdl-38004581

RESUMO

The work demonstrated the use of natural rubber for topical drug delivery. The first objective was to fabricate a porous deproteinized natural rubber film loaded with silver nanoparticles. Characterizing and assessing its formulation was the second objective. Surface pH, mechanical properties, swelling ratio, erosion, moisture vapor transmission rate, scanning electron microscopy/energy dispersive X-ray analysis, and X-ray diffraction were evaluated. In vitro studies and antibacterial activity were assessed. It was discovered that silver nanoparticles could enter the film and that their concentrations ranged between 7.25 and 21.03 µg/cm2. The pH of the film's surface was 7.00. The mechanical properties of the film with silver nanoparticle loading differed from the blank film. After adding silver nanoparticles, the film eroded faster than before, but the swelling ratio was not affected significantly. Increased time utilization had an impact on the moisture vapor transmission rate of the film. Silver nanoparticles released easily from the film while there was less permeability. The dead pig-ear skin had significant silver nanoparticle accumulation. Potent antibacterial activity was seen in the film containing silver nanoparticles. The silver nanoparticle-loaded film may be used as a wound dressing for a topical film that promotes wound healing while also protecting the area from infection.

3.
AAPS PharmSciTech ; 24(5): 105, 2023 Apr 20.
Artigo em Inglês | MEDLINE | ID: mdl-37081249

RESUMO

Traditional Asian remedies have mainly employed the macrofungus Ganoderma applanatum, which belongs to the family Ganodermataceae, as a medicinal mushroom due to its high antibacterial and antioxidant activity. Extracts of the fungus can be synthesized into nanoparticles, which are subsequently produced as plaster gels. Synthesized silver nanoparticle-mediated G. applanatum was discovered to have the greatest ability to inhibit bacterial growth in S. epidermidis. When applied to the skin, the prepared plaster gel converted from a gel to a film; thus, both gel and film generation are characteristic of its formulation. The plaster gel that was made was found to be consistent and attractive, and the yellow color had darkened. Its viscosity and pH were appropriate for the application and allowed it to remain on the skin without dripping or reacting with the skin until it dried. A shorter duration for film formation is possible. The film's tensile was slightly reduced, and it exhibited excellent thermal stability. Decomposition of the generated film occurred at a slower rate, which constrained the polymer chain's ability to move. The semi-crystalline structure was characteristic of the film. It was found that particles were distributed in the film. Rapid release from plaster gel within 4 h was seen, and this was followed by a period of a slowly declining release rate over 12 h. The accurate first-order kinetic used to estimate the release rate of the formulation. The plaster gel demonstrated greater antibacterial activity than the MIC value indicated. The in vivo evaluation was positive and showed no skin irritation. The formulation showed good stability. Therefore, this indicated that the prepared plaster gel is appropriate for topical pharmaceutical delivery and safe for skin application.


Assuntos
Ganoderma , Nanopartículas Metálicas , Nanopartículas Metálicas/química , Prata , Antibacterianos , Géis/química
4.
Pharmaceutics ; 15(4)2023 Mar 29.
Artigo em Inglês | MEDLINE | ID: mdl-37111583

RESUMO

Imidazolium-based ionic liquids have been widely utilized as versatile solvents for metal nanoparticle preparation. Silver nanoparticles and Ganoderma applanatum have displayed potent antimicrobial activities. This work aimed to study the effect of 1-butyl-3-methylimidazolium bromide-based ionic liquid on the silver-nanoparticle-complexed G. applanatum and its topical film. The ratio and conditions for preparation were optimized by the design of the experiments. The optimal ratio was silver nanoparticles: G. applanatum extract: ionic liquid at 97:1:2, and the conditions were 80 °C for 1 h. The prediction was corrected with a low percentage error. The optimized formula was loaded into a topical film made of polyvinyl alcohol and Eudragit®, and its properties were evaluated. The topical film was uniform, smooth, and compact and had other desired characteristics. The topical film was able to control the release of silver-nanoparticle-complexed G. applanatum from the matrix layer. Higuchi's model was used to fit the kinetic of the release. The skin permeability of the silver-nanoparticle-complexed G. applanatum was improved by about 1.7 times by the ionic liquid, which might increase solubility. The produced film is suitable for topical applications and may be utilized in the development of potential future therapeutic agents for the treatment of diseases.

5.
An Acad Bras Cienc ; 92(2): e20191073, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32696844

RESUMO

The objectives of this study are to prepare a 5 wt% lidocaine/aspirin ionic liquid drug-loaded gelatin/polyvinyl alcohol composite film using a freeze-thaw procedure and to evaluate their physicochemical characteristics, in vitro drug release, and stability. Lidocaine/aspirin ionic liquid drugs can be prepared by an ion-pair reaction between the hydrochloride salts of lidocaine and the sodium salts of aspirin, which showed a significant change in their thermal properties when compared to those pure drugs. The results showed that a transdermal patch could feasibly be used in pharmaceutical transdermal patches with good physicochemical properties. A chemical interaction between the drug and polymer base was not found. Decomposition of the lidocaine/aspirin ionic liquid drug was found in the patch; however, the properties of the patch were not changed after drug loading. The patch controlled the drug release and showed good stability during the studied period of three months when kept at 4°C more than at ambient temperature and 45°C.


Assuntos
Líquidos Iônicos , Adesivo Transdérmico , Administração Cutânea , Aspirina , Gelatina , Lidocaína , Álcool de Polivinil
6.
AAPS PharmSciTech ; 20(8): 322, 2019 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-31650263

RESUMO

The objectives of this work were to prepare a 5 wt% lidocaine-diclofenac ionic liquid drug-loaded gelatin/poly(vinyl alcohol) transdermal patch using a freeze/thaw method and to evaluate its physicochemical properties, in vitro release of lidocaine and diclofenac, and stability test. The lidocaine-diclofenac ionic liquid drug was produced by the ion pair reaction between the hydrochloride salts of lidocaine and the sodium salts of diclofenac. The thermal properties of the final drug product were significantly changed from the primary drugs. The ionic liquid drug could be dissolved in water and mixed in a polymer solution. The resulting transdermal patch was then exposed to 10 cycles of freezing and thawing preparation at - 20°C for 8 h and at 25°C for 4 h, respectively. As a result, it was found that the lidocaine-diclofenac ionic liquid drug-loaded transdermal patch showed good physicochemical properties and could feasibly be used in pharmaceutical applications. The lidocaine-diclofenac ionic liquid drug was not affected by the properties of the transdermal patch due to the lack of chemical interaction between polymer base and drug. The high drug release values of both lidocaine and diclofenac were controlled by the gelatin/poly(vinyl alcohol) transdermal patch. The patch showed good stability over the study period of 3 months when kept at 4°C or under ambient temperature.


Assuntos
Diclofenaco/farmacocinética , Gelatina/farmacocinética , Líquidos Iônicos/farmacocinética , Lidocaína/farmacocinética , Álcool de Polivinil/farmacocinética , Adesivo Transdérmico , Administração Cutânea , Anestésicos Locais/química , Anestésicos Locais/farmacocinética , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacocinética , Preparações de Ação Retardada/química , Preparações de Ação Retardada/farmacocinética , Diclofenaco/química , Combinação de Medicamentos , Liberação Controlada de Fármacos , Congelamento , Gelatina/química , Líquidos Iônicos/química , Lidocaína/química , Álcool de Polivinil/química
7.
J Environ Pathol Toxicol Oncol ; 33(1): 59-68, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24579810

RESUMO

To study the acute and subacute pulmonary toxicity of colloidal silver nanoparticles (Ag-NPs), 0 or 100 ppm of Ag-NPs were instilled intratracheally in mice. Cellular and biochemical parameters in bronchoalveolar lavage fluid (BALF) and histological alterations were determined 1, 3, 7, 15, and 30 days after instillation. Ag-NPs induced moderate pulmonary inflammation and injury on BALF indices during the acute period; however, these changes gradually regressed in a time-dependent manner. Concomitant histopathological and laminin immunohistochemical findings generally correlated to BALF data. Superoxide dismutase and metallothionein expression occurred in particle-laden macrophages and alveolar epithelial cells, which correlated to lung lesions in mice treated with Ag-NPs. These findings suggest that instillation of Ag-NPs causes transient moderate acute lung inflammation and tissue damage. Oxidative stress may underlie the induction of injury to lung tissue. Moreover, the expression of metallothionein in tissues indicated the protective response to exposure to Ag-NPs.


Assuntos
Pneumopatias/induzido quimicamente , Pneumopatias/patologia , Nanopartículas Metálicas/toxicidade , Metalotioneína/metabolismo , Prata/toxicidade , Doença Aguda , Administração por Inalação , Animais , Coloides , Modelos Animais de Doenças , Células Epiteliais/efeitos dos fármacos , Células Epiteliais/metabolismo , Células Epiteliais/patologia , Pulmão/efeitos dos fármacos , Pulmão/metabolismo , Pulmão/patologia , Pneumopatias/metabolismo , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Macrófagos/patologia , Masculino , Nanopartículas Metálicas/administração & dosagem , Camundongos , Camundongos Endogâmicos ICR , Prata/administração & dosagem , Fatores de Tempo
8.
J Vet Med Sci ; 73(11): 1417-23, 2011 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-21712637

RESUMO

Tests for acute oral toxicity, eye irritation, corrosion and dermal toxicity of colloidal silver nanoparticles (AgNPs) were conducted in laboratory animals following OECD guidelines. Oral administration of AgNPs at a limited dose of 5,000 mg/kg produced neither mortality nor acute toxic signs throughout the observation period. Percentage of body weight gain of the mice showed no significant difference between control and treatment groups. In the hematological analysis, there was no significant difference between mice treated with AgNPs and controls. Blood chemistry analysis also showed no differences in any of the parameter examined. There was neither any gross lesion nor histopathological change observed in various organs. The results indicated that the LD(50) of colloidal AgNPs is greater than 5,000 mg/kg body weight. In acute eye irritation and corrosion study, no mortality and toxic signs were observed when various doses of colloidal AgNPs were instilled in guinea pig eyes during 72 hr observation period. However, the instillation of AgNPs at 5,000 ppm produced transient eye irritation during early 24 hr observation time. No any gross abnormality was noted in the skins of the guinea pigs exposed to various doses of colloidal AgNPs. In addition, no significant AgNPs exposure relating to dermal tissue changes was observed microscopically. In summary, these findings of all toxicity tests in this study suggest that colloidal AgNPs could be relatively safe when administered to oral, eye and skin of the animal models for short periods of time.


Assuntos
Nanopartículas Metálicas/toxicidade , Prata/toxicidade , Testes de Toxicidade Aguda , Animais , Peso Corporal/efeitos dos fármacos , Coloides , Olho/efeitos dos fármacos , Feminino , Cobaias , Dose Letal Mediana , Masculino , Camundongos , Camundongos Endogâmicos ICR , Distribuição Aleatória , Pele/efeitos dos fármacos , Testes de Irritação da Pele
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