A Novel Solid-in-oil Nanosuspension for Transdermal Delivery of Diclofenac Sodium

Piao, Hongyu; Kamiya, Noriho; Hirata, Akihiko; Fujii, Takeru; Goto, Masahiro

doi:10.1007/s11095-007-9445-7

Cited by 77 publications

(30 citation statements)

References 17 publications

(17 reference statements)

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“…The particle size seems to play an important role in the permeation of the encapsulated active ingredient. Smaller particles seem to enhance the permeation to a greater extent than larger particles [130,131,132]. However, this conclusion is contradictory since it has already been shown that for the same kind of nanoemulsion there was no influence of the emulsion droplet size on the skin penetration of the encapsulated substance when applied to dermatomed human skin [133].…”

Section: Lipid Systemsmentioning

confidence: 96%

Transport of Substances and Nanoparticles across the Skin and in Vitro Models to Evaluate Skin Permeation and/or Penetration

Contri

Fiel

Pohlmann

et al. 2011

Nanocosmetics and Nanomedicines

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Abstract. Nanotechnology can be used to modify the drug permeation/penetration of encapsulated substances, through the manipulation of many different factors, including direct contact with the skin surface and controlled release. In general, nanoparticles cannot cross the skin barrier, which can be explained by the cell cohesion and lipids of the stratum corneum, the outermost skin layer. The device most commonly used to study the transport of substances and nanoparticles across the skin is the Franz vertical diffusion cell, followed by the substance quantification in the receptor fluid or determination of the amount retained in the skin. Microscopy techniques have also been applied in skin penetration or permeation experiments. This chapter will present the fundamental considerations regarding the transport of encapsulated substances and/or nanoparticles across the skin, the experimental models applied in these studies and a review of the main studies reported in the literature in order to allow the reader to gain insight into the current knowledge available in this area.

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Section: Lipid Systemsmentioning

confidence: 96%

Transport of Substances and Nanoparticles across the Skin and in Vitro Models to Evaluate Skin Permeation and/or Penetration

Contri

Fiel

Pohlmann

et al. 2011

Nanocosmetics and Nanomedicines

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“…The drug carvedilol is neutral in character but exhibits high negative potential due to the medium (PVA) in which it is suspended. Zeta potential value turned out to be À17.10, yet the stability of formulated nanosuspension was quite high because of the presence of interfacial film of polymers on the drug particles which generally exhibit irreversible adsorption (Piao et al, 2008).…”

Section: Surface Charge On Particlementioning

confidence: 99%

Formulation and evaluation of mucoadhesive buccal films impregnated with carvedilol nanosuspension: a potential approach for delivery of drugs having high first-pass metabolism

Rana¹,

Murthy²

2013

Drug Delivery

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Context: Mucoadhesive buccal films containing three layers (mucoadhesive layer, nanosuspension containing layer and backing membrane) were incorporated with carvedilol nanosuspension. Objective: Formulation and evaluation of nanosuspension incorporated mucoadhesive buccal films of carvedilol for bioavailability enhancement by avoiding first-pass metabolism. Methods: Carvedilol-loaded nanosuspension was prepared by a precipitation-ultrasonication method with varying concentrations of the polymer. The formulation was analyzed for size, size distribution, surface charge and morphology. Optimized nanosuspension was incorporated into drug gel layer which was sandwiched between a mucoadhesive layer and a backing layer to form tri-layered buccal films. They were evaluated for their physical, mechanical and bioadhesive parameters followed by in vitro and in vivo studies. Results and discussion: Nanosuspension showed a negative zeta potential (À17.21 mV) with a diameter of around 495 nm and a polydispersity index of 0.203. Nanosuspension incorporated drug gel layer (62.4% drug loading) was optimized to contain 3% HPMC and 50 mg Carbopol 934P. The mucoadhesive layer and the backing layer were optimized to contain 3% HPMC and 1% ethyl cellulose, respectively. In vitro drug release was 69% and 62.4% in 9 h across synthetic membrane and porcine buccal mucosa, respectively. In vivo studies conducted in rabbit model showed 916% increase in the relative bioavailability in comparison to marketed oral tablet formulation. The C max and T max of the prepared formulation increased due to increased surface area of drug and also by-passing hepatic metabolism. Conclusion: The drug delivery system has been designed as a novel platform for potential buccal delivery of drugs having high first-pass metabolism.

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“…[15][16][17] Recently, the use of drug nanoparticles has been shown to improve drug delivery to the skin. [18][19][20][21][22][23][24] Surface area enhancement due to the size reduction of drug crystals or their amorphous formation may affect skin permeation behavior. Nano-sized drug may also contribute to the enhanced retention, which is applicable for the topical administration.…”

Section: )mentioning

confidence: 99%

Effect of Particle Size on Skin Permeation and Retention of Piroxicam in Aqueous Suspension

et al. 2010

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Reduction in particle size of hydrophobic drugs has attracted interest as a way to improve their dissolution and absorption properties.1-4) Grinding is one of the methods used to reduce the size of drug crystals. Cogrinding of a hydrophobic drug with a hydrophilic polymer and surfactant appears to be an effective method for the preparation of drug nanoparticles and stable nanosuspensions.5-8) Using a drug/ polyvinylpyrrolidone K17 (PVP K17)/sodium dodecyl sulfate (SDS) ternary ground mixture (GM) at a weight ratio of 1/3/1, more than 20 kinds of drugs have been effectively reduced to nano-order particle size.6) When a probucol/PVP K12/SDS GM suspension was orally administered to rats, plasma concentration increased as particle size decreased.

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A Novel Solid-in-oil Nanosuspension for Transdermal Delivery of Diclofenac Sodium

Abstract: The SONS formulation can enhance the percutaneous absorption of DFNa.

Cited by 77 publications

References 17 publications

Transport of Substances and Nanoparticles across the Skin and in Vitro Models to Evaluate Skin Permeation and/or Penetration

Transport of Substances and Nanoparticles across the Skin and in Vitro Models to Evaluate Skin Permeation and/or Penetration

Formulation and evaluation of mucoadhesive buccal films impregnated with carvedilol nanosuspension: a potential approach for delivery of drugs having high first-pass metabolism

Effect of Particle Size on Skin Permeation and Retention of Piroxicam in Aqueous Suspension

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