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1.
Sci Rep ; 12(1): 13907, 2022 08 16.
Artigo em Inglês | MEDLINE | ID: mdl-35974065

RESUMO

Dolutegravir (DTG) is an antiretroviral drug approved in the year 2013, and being categorized as a BCS-II molecule, it possesses solubility issues. In order to enhance the solubility and improve its bioavailability, DTG-loaded Chitosan nanoparticles (NPs) were synthesized utilizing spray drying technology. The developed nanoformulation was characterized for its physicochemical properties and investigated for the feasibility of its administration through an oral route along with milk/food as an admixture for paediatric antiretroviral therapy. The in vivo oral bioavailability studies were conducted in Balb-C mice, where the animals were treated with the selected formulation of DTG-loaded Chitosan NPs and compared to pure DTG. The NPs exhibited 2.5-fold increase in the Cmax (77.54 ± 7.93 µg/mL) when compared to the pure DTG (30.15 ± 8.06 µg/mL). This phenomenon was further reflected by the improved bioavailability of DTG (AUC: 678.3 ± 10.07 µg/h/mL) in the NPs administered to mice when compared to the AUC of animals administered with pure DTG (405.29 ± 7 µg/h/mL). Altogether, the research findings showed that Chitosan-based NPs were ideal carriers for oral administration of DTG along with milk and exhibited great potential to enhance the bioavailability of the drug and treatment adherence for paediatric HIV patients.


Assuntos
Quitosana , Infecções por HIV , Nanopartículas , Administração Oral , Animais , Disponibilidade Biológica , Quitosana/química , Portadores de Fármacos/química , Infecções por HIV/tratamento farmacológico , Compostos Heterocíclicos com 3 Anéis , Humanos , Camundongos , Leite , Nanopartículas/química , Oxazinas , Piperazinas , Piridonas
2.
Sci Rep ; 9(1): 17803, 2019 Nov 28.
Artigo em Inglês | MEDLINE | ID: mdl-31780736

RESUMO

The newer methodology to improve the performance of cutting tool is by the constructive method of micro-texturing and green synthesized nanoparticles into the texture gaps for self-lubrication. Cross-chevron textures were made on the rake face of the cemented carbide tool using Neodymium Doped Yttrium Aluminium Garne (Nd-YAG) laser texturing machine. The environmentally friendly, non-hazardous and rapid method of producing nanoparticles was followed to produce Al2O3 nanoparticles. Various techniques used for characterizing the synthesized Al2O3 nanoparticles are Potential of Hydrogen (pH), Fourier Transform Infra-Red Spectroscopy Analysis (FTIR), Dynamic light scattering (DLS) and X-Ray Diffraction (XRD). The XRD shows the presence of required functional groups and the size of nanoparticles in the range of 500-550 nm. This article discusses the effect of textures, with and without nanoparticles filled on the texture gaps of the cemented carbide tool on the main cutting force, thrust force and co-efficient of friction while machining austenitic stainless steel 304. The combined effect of surface texturing and lubrication of Al2O3 nanoparticles enhanced the performance of the cutting tool compared with the conventional and textured tool.

3.
Eur J Pharm Sci ; 112: 38-51, 2018 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-29111151

RESUMO

The purpose of the present investigation is to formulate liposomes of Lornoxicam for topical delivery using Central Composite Design, to provide a sustained release of the drug and thereby extend its elimination half-life. Liposomes were prepared by thin film hydration method with pH induced vesiculation. The liposomes were assessed for their particle size, charge, morphology and drug entrapment and characterized using TGA-DSC and FTIR analysis, to assess the interaction between the drug and excipients. The in vitro release study was performed using modified USP dissolution apparatus-I using three different dissolution media and the ex vivo release study was performed using goat skin. The cytotoxicity of Lornoxicam liposomes were studied on NIH 3T3 cells by MTT assay. The optimized formulation with particle size ranging from 100-200nm provided sustained release for 8h. The characterization studies proved very less interactions between the drug and the excipients. The ex vivo studies showed flux value of 23.29µg/cm2/h and Kp 0.011645cm/h. The cytotoxicity study showed increase in toxicity with increase in concentration more than 0.5µg/mL. The in vivo skin toxicity studies and histopathology analysis showed absence of toxic lesions, which confirmed the suitability of the formulation for topical application. Lornoxicam liposomes with good skin permeation and sustained release of drug were finally optimized by the experimental design.


Assuntos
Anti-Inflamatórios não Esteroides/administração & dosagem , Piroxicam/análogos & derivados , Administração Cutânea , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/toxicidade , Sobrevivência Celular/efeitos dos fármacos , Preparações de Ação Retardada/administração & dosagem , Preparações de Ação Retardada/química , Preparações de Ação Retardada/toxicidade , Liberação Controlada de Fármacos , Cabras , Lipossomos , Camundongos , Modelos Químicos , Células NIH 3T3 , Piroxicam/administração & dosagem , Piroxicam/química , Piroxicam/toxicidade , Ratos Wistar , Pele/metabolismo , Absorção Cutânea
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