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1.
Biomed Mater ; 19(2)2024 Feb 27.
Artigo em Inglês | MEDLINE | ID: mdl-38364288

RESUMO

In this work, the semi solid extrusion 3D printing process was utilized to incorporate anti-HIV drug Dolutegravir and its nanoparticles into the buccal film (BF) that was fabricated using the developed polymer ink. The composite made of polyvinyl alcohol (PVA) and sodium alginate was processed into a 3D printing polymer ink with optimum viscosity (9587 ± 219 cP) needed for the seamless extrusion through the nozzle of the 3D printer. The formulated BFs were assessed for its physical properties like weight (0.414 ± 0.3 g), thickness (1.54 ± 0.02 mm), swelling index (18.5 ± 0.91%), and mucoadhesiveness strength (0.165 ± 0.09 N) etc, The structural integrity and the surface morphology of the developed BFs were investigated by scanning electron microscopy analysis. The chemical stability and the solid-state nature of the drug in the BFs were assessed by Fourier transform infrared and x-ray diffraction analysis respectively. Further the BFs were assessed for drug dissolutionin-vitroandex-vivo, to study the effect of polymer composition and printing condition on the dissolution profile of the drug in the simulated salivary fluid. The results demonstrated that the developed PVA based polymer ink for 3D printing utilizing pressure is a versatile approach in the context of manufacturing mucoadhesive BFs customized in terms of shape and the amount of drug loaded.


Assuntos
Quitosana , Compostos Heterocíclicos com 3 Anéis , Nanopartículas , Oxazinas , Piperazinas , Piridonas , Humanos , Criança , Quitosana/química , Polímeros/química , Álcool de Polivinil/química , Impressão Tridimensional
2.
Sci Rep ; 13(1): 11373, 2023 07 14.
Artigo em Inglês | MEDLINE | ID: mdl-37452106

RESUMO

The present study attempts to treat S. aureus-induced soft skin infections using a combinatorial therapy with an antibiotic, Ciprofloxacin (CIP), and an efflux pump inhibitor 5-Nitro-2-(3-phenylpropoxy) pyridine (5-NPPP) through a smart hydrogel delivery system. The study aims to reduce the increasing rates of infections and antimicrobial resistance; therefore, an efflux pump inhibitor molecule is synthesized and delivered along with an antibiotic to re-sensitize the pathogen towards antibiotics and treat the infections. CIP-loaded polyvinyl alcohol (PVA) hydrogels at varying concentrations were fabricated and optimized by a chemical cross-linking process, which exhibited sustained drug release for 5 days. The compound 5-NPPP loaded hydrogels provided linear drug release for 2 days, necessitating the need for the development of polymeric nanoparticles to alter the release drug pattern. 5-NPPP loaded Eudragit RSPO nanoparticles were prepared by modified nanoprecipitation-solvent evaporation method, which showed optimum average particle size of 230-280 nm with > 90% drug entrapment efficiency. The 5-NPPP polymeric nanoparticles loaded PVA hydrogels were fabricated to provide a predetermined sustained release of the compound to provide a synergistic effect. The selected 7% PVA hydrogels loaded with the dual drugs were evaluated using Balb/c mice models induced with S. aureus soft skin infections. The results of in vivo studies were evidence that the dual drugs loaded hydrogels were non-toxic and reduced the bacterial load causing re-sensitization towards antibiotics, which could initiate re-epithelization. The research concluded that the PVA hydrogels loaded with CIP and 5-NPPP nanoparticles could be an ideal and promising drug delivery system for treating S. aureus-induced skin infections.


Assuntos
Staphylococcus aureus Resistente à Meticilina , Infecções Estafilocócicas , Camundongos , Animais , Polímeros/química , Fluoroquinolonas/farmacologia , Staphylococcus aureus , Antibacterianos/farmacologia , Antibacterianos/química , Sistemas de Liberação de Medicamentos , Ciprofloxacina/farmacologia , Ciprofloxacina/química , Hidrogéis/química , Infecções Estafilocócicas/tratamento farmacológico , Liberação Controlada de Fármacos
3.
Assay Drug Dev Technol ; 19(2): 139-152, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33646014

RESUMO

The objective of the present study is to formulate the bilayer hydrogel of Aceclofenac and Itraconazole followed by surface spray coating with citric acid to treat inflammation, oral candidiasis, and xerostomia conditions in HIV patients. The hydrogel was prepared by the chemical cross-linking method using polyvinyl alcohol as polymer at the concentrations of 3%, 5%, 7%, and 9% w/v, for both the individual drugs and the combination bilayer. The amount of cross-linking agent (glutaraldehyde 1% v/v) and the catalyst (concentrated hydrochloric acid [HCl], dilute HCl, and acetic acid) was optimized at the level of 0.1 mL each in every hydrogel system, based on the required physical properties. The hydrogels were subjected for various evaluation parameters like weight variation (0.054-0.300 g), diameter (9.5-12.5 mm), thickness (2.5-4.0 mm), drug content (2.5-2.8 mg/mL), and swelling study. The increase in the polymer composition had led to a significant increase in the thickness and weight of the hydrogel and a corresponding decrease in the swelling index. Other characterization techniques like Fourier Transform Infra-Red Spectroscopy, X-Ray Diffraction, ThermoGravimetry-Differential Scanning Calorimetry, and optical microscopy analysis were carried out to study physicochemical interactions, crystallinity, thermal, and surface properties of the optimized hydrogel, respectively. The in vitro drug release studies by United States Pharmacopeia dissolution basket model and ex vivo permeation studies using Franz diffusion cell with goat buccal skin were carried out for 6 h, in different media such as distilled water, phosphate buffer pH 6.8, and simulated salivary fluid.


Assuntos
Ácido Cítrico/química , Diclofenaco/análogos & derivados , Hidrogéis/química , Itraconazol/uso terapêutico , Xerostomia/tratamento farmacológico , Diclofenaco/química , Diclofenaco/uso terapêutico , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Humanos , Itraconazol/química
4.
Pharmaceutics ; 12(9)2020 Aug 28.
Artigo em Inglês | MEDLINE | ID: mdl-32872234

RESUMO

Silver nanoparticles (AgNPs) have recently become very attractive for the scientific community due to their broad spectrum of applications in the biomedical field. The main advantages of AgNPs include a simple method of synthesis, a simple way to change their morphology and high surface area to volume ratio. Much research has been carried out over the years to evaluate their possible effectivity against microbial organisms. The most important factors which influence the effectivity of AgNPs against microorganisms are the method of their preparation and the type of application. When incorporated into fabric wound dressings and other textiles, AgNPs have shown significant antibacterial activity against both Gram-positive and Gram-negative bacteria and inhibited biofilm formation. In this review, the different routes of synthesizing AgNPs with controlled size and geometry including chemical, green, irradiation and thermal synthesis, as well as the different types of application of AgNPs for wound dressings such as membrane immobilization, topical application, preparation of nanofibers and hydrogels, and the mechanism behind their antimicrobial activity, have been discussed elaborately.

5.
J Antimicrob Chemother ; 74(6): 1618-1626, 2019 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-30863862

RESUMO

BACKGROUND: MDR Staphylococcus aureus is a major aetiological agent of catheter-associated infections. A quorum sensing targeted drug development approach proves to be an effective alternative strategy to combat such infections. METHODS: Intravenous catheters were coated with polymethacrylate copolymers loaded with the antivirulent compound 2-[(methylamino)methyl]phenol (2MAMP). The in vitro drug release profile and kinetics were established. The anti-biofilm effect of the coated catheters was tested against clinical isolates of MDR S. aureus. The in vivo studies were carried out using adult male Wistar rats by implanting coated catheters in subcutaneous pockets. Histopathological analysis was done to understand the immunological reactions induced by 2MAMP. RESULTS: A uniform catheter coating of thickness 0.1 mm was achieved with linear sustained release of 2MAMP for 6 h. The coating formulation was cytocompatible. The in vitro and in vivo anti-adherence studies showed reduced bacterial accumulation in coated catheters after 48 h. The histopathological results confirmed that the coated catheter did not bring about any adverse inflammatory response. CONCLUSIONS: The developed anti-quorum-coated catheter that is non-toxic and biocompatible has the potential to be used in other medical devices, thereby preventing catheter-associated infections.


Assuntos
Infecções Relacionadas a Cateter/microbiologia , Catéteres , Materiais Revestidos Biocompatíveis , Polímeros , Percepção de Quorum/efeitos dos fármacos , Infecções Estafilocócicas/microbiologia , Staphylococcus aureus/efeitos dos fármacos , Animais , Biofilmes/efeitos dos fármacos , Infecções Relacionadas a Cateter/tratamento farmacológico , Catéteres/microbiologia , Materiais Revestidos Biocompatíveis/farmacologia , Modelos Animais de Doenças , Testes de Sensibilidade Microbiana , Polímeros/química , Ratos , Análise Espectral , Infecções Estafilocócicas/tratamento farmacológico , Infecções Estafilocócicas/patologia
6.
Drug Deliv Transl Res ; 7(5): 750-760, 2017 10.
Artigo em Inglês | MEDLINE | ID: mdl-28597122

RESUMO

Hyperpigmentation is a dermal condition of melanocyte proliferation, induced by various factors like ultraviolet radiation producing reactive oxygen species, DNA damage, and apoptosis. The application of topical antioxidants through the different type of formulations can help to prevent oxidative damage to the skin. L-ascorbic acid (vitamin C) is a water-soluble compound and the most abundant antioxidant in human skin, but this vitamin is unstable and loses its potency with poor formulation strategies. Nanotechnology has been effectively used to promote stability and therapeutic activity of various drug molecules. With this context, the objective of the work was set to formulate a topical delivery system of vitamin C nanoparticles incorporated into the polymeric gel. Vitamin C (50 mg) was loaded into ethyl cellulose nanoparticles, of varying concentrations (50-250 mg), by the solvent evaporation method and subsequently incorporated into hydroxypropyl methyl cellulose gels (3, 5, and 7%). The formulations were characterized for various physico-chemical properties such as particle size, drug content, entrapment efficiency, and drug-polymer interactions. In vitro, drug release studies were conducted by using dialysis bag method and Franz diffusion cell for the nanoparticles and gel formulations, respectively. The optimized formulation exhibited sustained release over 8 h. The ex vivo skin permeation studies were performed and the amount of drug retained and released through the skin were determined. The results obtained from the study proved the potentiality and suitability of this novel system to treat hyperpigmentation.


Assuntos
Antioxidantes/administração & dosagem , Ácido Ascórbico/administração & dosagem , Administração Cutânea , Animais , Antioxidantes/química , Antioxidantes/farmacocinética , Ácido Ascórbico/química , Ácido Ascórbico/farmacocinética , Química Farmacêutica , Géis , Nanopartículas , Tamanho da Partícula , Absorção Cutânea
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