Characterization of new topical ketoprofen formulations prepared by drug entrapment in solid lipid matrices

Argemí, Anna; Domingo, Concepción; Sousa, A.R. Sampaio de; Duarte, Catarina M.M.; García‐González, Carlos A.; Saurina, Javier

doi:10.1002/jps.22684

Cited by 12 publications

(3 citation statements)

References 37 publications

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“…The processing of SLMPs using the PGSS technique avoids the use of solvents or washing steps. High loading efficiencies of bioactive agents (insulin, recombinant human growth hormone, ibuprofen, ketoprofen) are commonly obtained using this technique [ 32 , 33 , 34 , 35 , 36 ]. The advantageous features of PGSS technique can be herein exploited for the processing of SLMPs loaded with LID.…”

Section: Introductionmentioning

confidence: 99%

Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications

et al. 2020

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The delivery of bioactive agents using active wound dressings for the management of pain and infections offers improved performances in the treatment of wound complications. In this work, solid lipid microparticles (SLMPs) loaded with lidocaine hydrochloride (LID) were processed and the formulation was evaluated regarding its ability to deliver the drug at the wound site and through the skin barrier. The SLMPs of glyceryl monostearate (GMS) were prepared with different LID contents (0, 1, 2, 4, and 10 wt.%) using the solvent-free and one-step PGSS (Particles from Gas-Saturated Solutions) technique. PGSS exploits the use of supercritical CO2 (scCO2) as a plasticizer for lipids and as pressurizing agent for the atomization of particles. The SLMPs were characterized in terms of shape, size, and morphology (SEM), physicochemical properties (ATR-IR, XRD), and drug content and release behavior. An in vitro test for the evaluation of the influence of the wound environment on the LID release rate from SLMPs was studied using different bioengineered human skin substitutes obtained by 3D-bioprinting. Finally, the antimicrobial activity of the SLMPs was evaluated against three relevant bacteria in wound infections (Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa). SLMPs processed with 10 wt.% of LID showed a remarkable performance to provide effective doses for pain relief and preventive infection effects.

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Section: Introductionmentioning

confidence: 99%

Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications

et al. 2020

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“…Partial-thickness samples, including tissue culturederived skin equivalents (ie, living skin-equivalent models) and a human reconstructed epidermis, have also been used as alternatives to animal skins in transdermal delivery studies. 41 Living skin-equivalent models have a dermis, an epidermis, and a partially differentiated stratum corneum, but are deficient in skin appendages (ie, pilosebaceous units, hair follicles, and sweat glands). As a result, an 800-to 900-fold higher flux was achieved by using living skin-equivalent models than full-thickness human skin because of the differences in structures and lipid compositions.…”

Section: Discussionmentioning

confidence: 99%

Quantitative Evaluation of Sonophoresis Efficiency and Its Dependence on Sonication Parameters and Particle Size

Lee

Zhou

2015

J of Ultrasound Medicine

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ral administration and hypodermic injection are routine approaches for drug delivery to the circulation. However, they are associated with some shortcomings, such as premature drug metabolization by the first-pass effect of the liver and gut wall, degradation of drugs by the digestive tract, unstable plasma levels, difficulty of immediate termination, pain, dangerous medical waste, and risk of disease transmission by needle reuse. 1 Transporting therapeutic agents through the wide epidermis, known as transdermal drug delivery, is an attractive alternative to conventional approaches. Transdermal drug delivery is noninvasive in nature, and the systems can be self-administered, released over a long period, and inexpensive. Three generations of development have been undergone in transdermal drug delivery, such as chemical enhancers, 2 iontophoresis, 3 biochemical enhancers, 4 electroporation, 5 and microneedles. 6 These techniques are mostly reversible except microneedles. The skin structure and elasticity can be altered to enable increased permeation of compounds temporarily and resumed a few hours after termination without permanent damage. Kun Loong Lee, BS, Yufeng Zhou, PhDReceived January 14, 2014, Transdermal drug delivery makes a critical contribution to medical practice and some advantages over conventional oral administration and hypodermic injection. Enhancement of percutaneous absorption or penetration of therapeutic agents (ie, drugs and macromolecules) by ultrasound, termed sonophoresis, has been applied and studied for decades. In this study, the penetration percentage through porcine ear skin specimens was determined quantitatively by measuring the fluorescence from nanoparticles of 60, 220, and 840 nm in size in a receptor chamber at different sonication parameters (ie, duty cycle, 20%-100%; acoustic intensity, 0.3-1.0 W/cm 2 ; duration, 7-30 minutes; and frequency, 1 MHz). In general, the sonophoresis efficiency increased with the acoustic intensity, duty cycle, and sonication duration but decreased with the particle size (mean ± SD, 62.6% ± 5.4% for 60-nm versus 11.9% ± 1.1% for 840-nm polystyrene nanospheres after 30 minutes of sonication at 0.5 W/cm 2 and a 100% duty cycle; P < .05). On scanning electron microscopy the pore size remained the same (≈100 μm), but more flakes were observed with the progress of sonication. In summary, sonophoresis efficiency is dependent on the ultrasound parameters and particle size. Sufficient sonication would lead to satisfactory penetration of even submicrometer objects through the pores.

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“…A more detailed exposition of the method was subsequently reported by these authors [119]. A solid lipid matrix consisting of a mixture of hydrogenated castor oil and glyceryl monostearate has been imprinted with ketoprofen in supercritical carbon dioxide solvent, permitting the controlled release of the drug [120].…”

Section: Preparation Of Nano-sized Particlesmentioning

confidence: 99%

Some Advances in Supercritical Fluid Extraction for Fuels, Bio-Materials and Purification

Marcus

2019

Processes

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Supercritical fluids are used for the extraction of desired ingredients from natural materials, but also for the removal of undesired and harmful ingredients. In this paper, the pertinent physical and chemical properties of supercritical water, methanol, ethanol, carbon dioxide, and their mixtures are provided. The methodologies used with supercritical fluid extraction are briefly dealt with. Advances in the application of supercritical extraction to fuels, the gaining of antioxidants and other useful items from biomass, the removal of undesired ingredients or contaminants, and the preparation of nanosized particles of drugs are described.

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Characterization of new topical ketoprofen formulations prepared by drug entrapment in solid lipid matrices

Cited by 12 publications

References 37 publications

Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications

Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications

Quantitative Evaluation of Sonophoresis Efficiency and Its Dependence on Sonication Parameters and Particle Size

Some Advances in Supercritical Fluid Extraction for Fuels, Bio-Materials and Purification

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