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1.
Molecules ; 28(17)2023 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-37687262

RESUMO

Curcumin (CUR) is a natural compound extracted from turmeric (Curcuma longa L.) used to cure acne, wound healing, etc. Its disadvantages, such as poor solubility and permeability, limit its efficacy. Nanoemulsion (NE)-based drug delivery systems have gained popularity due to their advantages. This study aimed to optimize a CUR-NE-based gel and evaluate its physicochemical and biological properties. A NE was prepared using the catastrophic phase inversion method and optimized using the Design Expert 12.0 software. The CUR-NE gel was characterized in terms of visual appearance, pH, drug release, antibacterial and wound healing effects. The optimal formulation contained CUR, Capryol 90 (oil), Labrasol:Cremophor RH40 (1:1) (surfactants), propylene glycol (co-surfactant), and water. The NE had a droplet size of 22.87 nm and a polydispersity index of 0.348. The obtained CUR-NE gel had a soft, smooth texture and a pH of 5.34 ± 0.05. The in vitro release of CUR from the NE-based gel was higher than that from a commercial gel with nanosized CUR (21.68 ± 1.25 µg/cm2, 13.62 ± 1.63 µg/cm2 after 10 h, respectively). The CUR-NE gel accelerated in vitro antibacterial and in vivo wound healing activities as compared to other CUR-loaded gels. The CUR-NE gel has potential for transdermal applications.


Assuntos
Curcumina , Curcumina/farmacologia , Hidrogéis , Inibidores de Ciclo-Oxigenase , Sistemas de Liberação de Medicamentos , Antibacterianos/farmacologia
2.
Int J Biol Macromol ; 194: 1010-1018, 2022 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-34843817

RESUMO

Local delivery of drug is a promising strategy to manage periodontitis characterized by chronic inflammation of the soft tissue surrounding the teeth. An optimized system should prolong the drug retention time and exhibit controlled drug permeation through the buccal mucosal layer. This study was aimed to develop hydroxyethyl cellulose (HEC)-based gel containing metronidazole (MTZ) loaded in solid lipid nanoparticles (SLNs), and to enhance the antimicrobial activity of MTZ. SLNs were prepared using a combination method of solvent evaporation and hot homogenization. The results showed that the fabricated SLNs, comprising of Precirol (2.93%, w/v), Tween 80 (1.8%, w/v), and the drug:lipid ratio of 19.3% (w/w), were approximately 200 nm in size, with a narrow distribution. The HEC (3%, w/w)-based gel formed a smooth, homogeneous structure and had preferable mechanical and rheological properties. Moreover, the MTZ-loaded SLNs-based HEC gel (equivalent to 1% of MTZ, w/w) exhibited a sustained in vitro drug release pattern, optimal ex vivo permeability, and enhanced in vitro antimicrobial activity after 24 h of treatment. These findings indicate the potential of the MTZ-loaded SLNs-based HEC formulation for local drug delivery at the buccal mucosa in managing periodontal disease.


Assuntos
Celulose/análogos & derivados , Portadores de Fármacos/química , Composição de Medicamentos , Géis/química , Lipossomos/química , Metronidazol/administração & dosagem , Mucosa Bucal , Nanopartículas/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Celulose/química , Fenômenos Químicos , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Fenômenos Mecânicos , Metronidazol/química , Metronidazol/farmacologia , Testes de Sensibilidade Microbiana , Mucosa Bucal/efeitos dos fármacos , Permeabilidade , Análise Espectral
3.
Drug Dev Ind Pharm ; 43(7): 1134-1142, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-28277847

RESUMO

OBJECTIVE: Artesunate (ART) is proven to have potential anti-proliferative activities, but its instability and poor aqueous solubility limit its application as an anti-cancer drug. The present study was undertaken to develop coaxial electrospraying as a novel technique for fabricating nanoscale drug delivery systems of ART as the core-shell nanostructures. METHODS: The core-shell nanoparticles (NPs) were fabricated with coaxial electrospraying and the formation mechanisms of NPs were examined. The physical solid state and drug-polymer interactions of NPs were characterized by X-ray powder diffraction (XRPD) and Fourier transform infrared (FTIR) spectroscopy. The effects of materials and electrospraying process on the particle size and surface morphology of NPs were investigated by scanning electron microscopy (SEM). The drug release from NPs was determined in vitro by a dialysis method. RESULTS: The ART/poly(lactic-co-glycolic) acid (PLGA) chitosan (CS) NPs exhibited the mean particle size of 303 ± 93 nm and relatively high entrapment efficiency (80.5%). The release pattern showed an initial rapid release within two hours followed by very slow extended release. The release pattern approached the Korsmeyer-Peppas model. CONCLUSIONS: The present results suggest that the core-shell NPs containing PLGA and CS have a potential as carriers in the anticancer drug therapy of ART.


Assuntos
Antineoplásicos/administração & dosagem , Artemisininas/administração & dosagem , Quitosana/química , Sistemas de Liberação de Medicamentos/métodos , Nanopartículas/química , Ácido Poliglicólico/química , Antineoplásicos/química , Artemisininas/química , Artesunato , Liberação Controlada de Fármacos , Microscopia Eletrônica de Varredura , Tamanho da Partícula , Difração de Raios X
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