4.7 Article

Nanospray technology for an in situ gelling nanoparticulate powder as a wound dressing

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INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 473, 期 1-2, 页码 30-37

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ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2014.06.049

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Nanoparticles by spray-drying; In situ gelling dry powder; Topical antibiotic controlled release; Wound dressing; Antimicrobial activity

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In the current study the feasibility of the novel nano spray drying technique for the production of stable nanoparticulate dry powder, able to gel when administered locally on a wound, is explored. Gentamicin sulphate (GS) was loaded into alginate/pectin nanoparticles as highly soluble (hygroscopic) model drug with wide range antibacterial agent for wound dressing. The influence of process variables, mainly spray mesh size and feed concentration, on particle size and morphology, powder wound fluid uptake ability and gelling rate, as well as hydrogel water vapour transmission at wound site were studied. Particles morphology was spherical with few exceptions as slightly corrugated particles when the larger nozzle was used. Production of spherical nanoparticles (d(50) similar to 350 nm) in good yield (82-92%) required 4 mu m spray mesh whereas 7 mu m mesh produced larger wrinkled particles. Nano spray-dried particles showed high encapsulation efficiency (similar to 80%), good flowability, high fluid uptake, fast gel formation (15 min) and proper adhesiveness to fill the wound site and to remove easily the formulation after use. Moreover, moisture transmission of the in situ formed hydrogel was between 95 and 90 g/m(2)/h, an optimum range to avoid wound dehydration or occlusion phenomena. Release of the encapsulated GS, monitored as permeation rate using Franz cells in simulated wound fluid (SWF) was related to particle size and gelling rate. Sustained permeation profiles were obtained achieving total permeation of the drug between 3 and 6 days. However, all nano spray-dried formulations presented a burst effect, suitable to prevent infection spreading at the beginning of the therapy. Antimicrobial tests against Staphylococcus aureus and Pseudomonas aeruginosa showed stronger and prolonged antimicrobial effect of the nanoparticles compared to pure GS both shortly after administration and over time (till 12 days). (C) 2014 Elsevier B.V. All rights reserved.

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