Lecithin vesicles for topical delivery of diclofenac

Boinpally, Ramesh; Zhou, Sasha; Poondru, Srinivasu; Devraj, Gopinath; Jasti, Bhaskara

doi:10.1016/s0939-6411(03)00143-7

Cited by 83 publications

(36 citation statements)

References 8 publications

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“…They have been shown to be interesting as drug delivery systems for topical delivery. Due to their similarity to biological membranes since the lipid bilayer contains natural phospholipids and cholesterol liposomes theoretically do not have any risk of antigencity (Boinpally et al, 2003). Micro-emulsions, which are optically isotropic and thermodynamically stable systems of water, oil, surfactant and co-surfactant, have been studied as drug delivery systems because of their capacity to enhance the solubility of poorly water-soluble drugs as well as their enhancement of topical and systemic availability (Cooney et al, 1998).…”

Section: Introductionmentioning

confidence: 99%

Comparative topical delivery of antifungal drug croconazole using liposome and micro-emulsion-based gel formulations

2013

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Section: Introductionmentioning

confidence: 99%

Comparative topical delivery of antifungal drug croconazole using liposome and micro-emulsion-based gel formulations

2013

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“…These carriers are particularly interesting because they can be used as solvents and enhancers, and they can also increase the time of residence of the drug in the stratum corneum and epidermis, while reducing the systemic absorption of the drug. [19][20][21] In the field of vesicle preparation, catanionic surfactants have attracted considerable attention in the last two decades. Indeed, this surfactant family, obtained by mixing two oppositely charged surfactants, exhibits a unique ability to form stable vesicles spontaneously in an aqueous solution.…”

Section: Introductionmentioning

confidence: 99%

Design of Original Bioactive Formulations Based on Sugar–Surfactant/Non‐steroidal Anti‐inflammatory Catanionic Self‐Assemblies: A New Way of Dermal Drug Delivery

Consola

Blanzat

Pérez

et al. 2007

Chemistry A European J

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A new kind of catanionic assembly was developed that associates a sugar-based surfactant with a non-steroidal anti-inflammatory drug (NSAID). Three different assemblies using indomethacin, ibuprofen and ketoprofen as NSAIDs were easily obtained in water by an acid-base reaction. These assemblies formed new amphiphilic entities because of electrostatic and hydrophobic effects in water and led to the spontaneous formation of vesicles. These catanionic vesicles were then tested as potential NSAID delivery systems for dermatological application. The anti-inflammatory activity was evaluated in vivo, and this study clearly showed an improved therapeutic effect for NSAIDs that were formulated as catanionic vesicles. These vesicles ensured a slower diffusion of the NSAID through the skin. This release probably increased the time of retention of the NSAID in the targeted strata of the skin. Thus, the present study suggests that this catanionic bioactive formulation could be a promising dermal delivery system for NSAIDs in the course of skin inflammation treatment.

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“…Diclofenac is widely prescribed as an oral medication, but due to its gastrointestinal side effects such as gastric ulcers and gastrointestinal bleeding, extensive first pass metabolism (~ 50%), and short biological halflife, an alternative delivery approach is desirable. One such approach, iontophoretic delivery, can potentially provide deeper tissue penetration without compromising target tissue concentrations (4). Diclofenac potassium (pKa 4.0) has partition coefficient (5) of 13.4 at pH 7.4.…”

Section: Introductionmentioning

confidence: 99%

Subcutaneous concentrations following topical iontophoretic delivery of diclofenac

et al. 2012

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A self-contained Wearable Electronic Disposable Drug Delivery (WEDD ® ) patch was used to demonstrate that diclofenac levels delivered by iontophoresis are greater than estimated minimal effective concentrations in local subcutaneous tissue and are also greater than either passive transdermal or intravenous delivery using hairless rats. In vitro iontophoretic delivery was evaluated to optimize donor cell formulation using Franz diffusion cells and 1000 NMWL Millipore ultrafiltration membrane. In vivo animal studies were done using patches powered with a 4-volt system, consisting of a 1-volt Zn anode and Ag/AgCl cathode with built in 3-volt lithium battery. Blood and microdialysis samples were collected at different time points after patch application. Current levels increased to 1.0 mA at 30 min, then fell to a steady state of ~ 0.4 mA. Both WEDD ® and passive patches produced measurable levels of diclofenac in the subcutaneous tissue below the application site (C max ± SE = 113.3 ± 61.7 ng/mL and 36.3 ± 15.9 ng/mL, respectively). The dose delivered in six hours was calculated to be 0.226 ± 0.072 mg and 0.430 ± 0.048 mg in passive and iontophoretic delivery, respectively. Diclofenac was not detected in the subcutaneous tissue after intravenous administration of 1.5 mg/kg diclofenac solution. The trend indicates that WEDD ® can be used to successfully deliver diclofenac to subcutaneous tissue to concentrations higher when compared to either passive delivery or intravenous dosing of 1.5 mg/kg.

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Lecithin vesicles for topical delivery of diclofenac

Cited by 83 publications

References 8 publications

Comparative topical delivery of antifungal drug croconazole using liposome and micro-emulsion-based gel formulations

Comparative topical delivery of antifungal drug croconazole using liposome and micro-emulsion-based gel formulations

Design of Original Bioactive Formulations Based on Sugar–Surfactant/Non‐steroidal Anti‐inflammatory Catanionic Self‐Assemblies: A New Way of Dermal Drug Delivery

Subcutaneous concentrations following topical iontophoretic delivery of diclofenac

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