In vitro based index of topical anti-inflammatory activity to compare a series of NSAIDs

Cordero, José Antonio; Camacho, Mercedes; Obach, R.; Domènech, Josep Mestres i; Vila, L.

doi:10.1016/s0939-6411(00)00149-1

Cited by 68 publications

(39 citation statements)

References 25 publications

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“…On the one hand, cortisone with its cytostatic features interferes with the cell proliferation of fibroblasts and keratinocytes [4, 5], but on the other hand, it is responsible for the inhibition of the physiological inflammatory phase during wound healing [6]. NSAIDs show a similar but weaker effect on the well-orchestrated processes of wound healing, by disturbing the inflammatory phase [7]. …”

Section: Introductionmentioning

confidence: 99%

Side Effects of Frequently Used Antihypertensive Drugs on Wound Healing in vitro

Besser

Terberger

Bachmann

et al. 2019

Skin Pharmacol Physiol

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Background: The number of patients who has a daily intake of antihypertensive drugs is rising, due to an also rising prevalence of lifestyle diseases. Interestingly, knowledge about effects of these drugs in terms of wound healing is low. Objective: Based on a few differing studies, the idea arose that antihypertensives may have side effects on wound healing. Methods: Five antihypertensive drugs from different substance classes (metoprolol, amlodipine, ramipril, hydrochlorothiazide, candesartan) were investigated, in terms of possible impacts on cell metabolism and migration of human skin fibroblasts and keratinocytes. Additionally, histological and immunohistochemical analyses were performed in a 3-dimensional (3D) wound model addressing the influence on regeneration processes, such as cell migration, metabolic activity, apoptosis and epidermal thickness. Results: Hydrochlorothiazide and ramipril exerted inhibiting effects in nearly all analyses, interestingly, in serum equivalent doses. In contrast, candesartan and amlodipine induced slight positive effects in 2D as well as in 3D models. The previously described positive effects of β-blockers could only partially be confirmed by metoprolol. Antihypertensive drugs affected fibroblasts more than keratinocytes – whether positively or negatively. Conclusion: Antihypertensive drugs have an influence on keratinocytes and fibroblasts; they are not neutral. Candesartan has the most positive effects on skin cells. For angiotensin-converting enzyme inhibitors and thiazide diuretics, wound healing in a 3D model is delayed. β-Receptor blockers seem to improve wound healing to a small extent just like calcium channel blockers. These results should be evaluated in a clinical trial to verify their clinical relevance.

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Section: Introductionmentioning

confidence: 99%

Side Effects of Frequently Used Antihypertensive Drugs on Wound Healing in vitro

Besser

Terberger

Bachmann

et al. 2019

Skin Pharmacol Physiol

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“…[4][5][6] It is generally recognized that NSAIDs are characterized by a low water solubility, which is associated with their hydrophobicity, and these features are responsible for their low intrinsic dermal bioavailability.…”

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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“…site-specific delivery). But studies on topical administration of Tenoxicam have shown that its penetration is very poor by this route compared to other NSAIDs [4]. Probably due to unfavourable physico-chemical characters of the molecule, such as its melting point range from 205 C to 213 C and log P (octanol/water) of 2.40, Tenoxicam is mostly marketed as oral formulations.…”

Section: Introductionmentioning

confidence: 99%

Nano-appended transdermal gel of Tenoxicam via ultradeformable drug carrier system

Negi

Chauhan

Garg

2013

Journal of Experimental Nanoscience

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Tenoxicam is one of the potent non-steroidal anti-inflammatory drugs (NSAIDs), which is used clinically in the treatment of rheumatoid arthritis. Like other NSAIDs, Tenoxicam also suffers from the drawback of being associated with gastrointestinal side effects. Further, transdermal penetration of this drug is very poor, which circumvents the use of transdermal route. The main objective of this study is to exploit the concept of ultradeformable vesicles to increase the transport of Tenoxicam through transdermal route, and also to present it as a possible replacement for the oral NSAID therapy for rheumatoid arthritis. Three concentrations (5%, 15% and 25%) of three different surfactants (Tween-80, Span-80 and sodium desoxycholate) were used along with soya lecithin to prepare the ultradeformable vesicles. Among nine different types of vesicles, T3 vesicles (with 25% Tween-80) were found to have shown the smallest size (82.80 AE 0.74 nm), highest release in 24 h (98.01 AE 0.33%) and highest deformability (31.27 AE 0.28) and hence chosen for formulating into the gel. Among three different Carbopol Õ 934 concentrations (1%, 1.5% and 2%), G-2 with 1.5% carbopol was chosen as the final formulation. The formulation has shown almost twice the transdermal flux as compared to the gel with free Tenoxicam. The in vivo performance was also found to be significantly better than the oral Tenoxicam and marketed aceclofenac gel (Hifenac Õ ). This study concluded that the gel containing Tenoxicam encapsulated in ultradeformable vesicles has a better prospective for the transdermal use to treat rheumatoid arthritis.

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In vitro based index of topical anti-inflammatory activity to compare a series of NSAIDs

Cited by 68 publications

References 25 publications

Side Effects of Frequently Used Antihypertensive Drugs on Wound Healing in vitro

Side Effects of Frequently Used Antihypertensive Drugs on Wound Healing in vitro

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

Nano-appended transdermal gel of Tenoxicam via ultradeformable drug carrier system

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