Strategies for meloxicam delivery to and across the skin: a review

Chen, Jianmin; Gao, Yunhua

doi:10.3109/10717544.2016.1157839

Cited by 24 publications

(10 citation statements)

References 78 publications

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“…MLX (4-hydroxy-2-methyl-N-(5-methylthiazol-2-yl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide) is an effective non-steroidal anti-inflammatory drug (NSAID) which is used in the treatment of rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis. In the last decade, several studies have been published regarding preparation and testing TTSs containing MLX with encouraging results in skin permeability [10][11][12][13].…”

Section: Lvfmentioning

confidence: 99%

"Development of a rapid capillary zone electrophoresis method to quantify Levofloxacin and Meloxicam from transdermal therapeutic systems "

Rusu¹,

Antonoaea²,

Ciurba³

et al. 2019

Studia UBB Chemia

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Capillary zone electrophoresis (CZE) could be a useful technique for the quantification of active substances from transdermal therapeutic systems (TTSs). TTSs are pharmaceutical forms in development that may release one or more active substances with some significant advantages as increased compliance to treatment, avoidance of first hepatic passage and low manufacturing costs. A simple, reliable, efficient, and lowcost CZE method was developed and validated for the simultaneous determination of levofloxacin (fluoroquinolone) and meloxicam (non-steroidal anti-inflammatory) from TTSs. The selected experimental parameters were 50 mM borax (pH 9.3) as background electrolyte, +25 kV applied voltage, 50 mbar/5 seconds hydrodynamic injection and 40°C temperature, using an uncoated fused-silica capillary with (51 cm total length/43 cm effective length, 50 µm i.d.). CZE experiments were performed in less than four minutes with a resolution of 7.79 at a wavelength of 335 nm. Validation of the method presented good linearity data, precision (RDS% < 1 for migration times and RDS% < 2 for peaks area) and sensitivity (LOD 3.43 and 16.05 μg•mL-1 , LOQ 10.38 and 54.55 μg•mL-1 for levofloxacin and meloxicam, respectively). Recovery of the active substances ranged between 85.14% and 96.38%. Our developed CZE method proved its applicability for analysis of the two substances from TTSs.

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Section: Lvfmentioning

confidence: 99%

"Development of a rapid capillary zone electrophoresis method to quantify Levofloxacin and Meloxicam from transdermal therapeutic systems "

Rusu¹,

Antonoaea²,

Ciurba³

et al. 2019

Studia UBB Chemia

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“…Recently, in situ film-forming systems (on the skin, after spreading in a thin layer) -FFSs which form a film on the skin after spreading in a thin layer, have been developed as a new approach to be used as an alternative to both conventional and transdermal topical formulations [12]. In this paper, four pharmaceutical substances were selected as potential active ingredients ( Figure 1) that could be useful in the form of film-forming systems with dermal and/or transdermal delivery: adapalene (ADA) [23,84], levofloxacin (LEV) [36,69], meloxicam (MEL) [16], and miconazole nitrate (MIC) [10]. These therapeutic agents have some significant physicochemical properties (Table I) based on which they can be individually used to treat various skin diseases: skin candidiasis, acne vulgaris, other skin infections, etc.…”

Section: Introductionmentioning

confidence: 99%

“…It is already known that a low MP will result in better absorption of the compounds [17]. Also, the diffusivity in stratum corneum is correlated with the molecular weight (MW); thus, the compound should not have high molecular weight and size [16,62].…”

Section: Introductionmentioning

confidence: 99%

Compatibility Study of Four Binary Combinations of Active Ingredients for Dermal Film Forming Systems

Rusu¹

2020

FARMACIA

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Adapalene (ADA), levofloxacin (LEV), meloxicam (MEL) and miconazole nitrate (MIC) were selected as potential active ingredients for film systems with dermal or transdermal delivery. This study aimed to evaluate the compatibility of four binary mixtures-ADA and LEV (M1), ADA and MIC (M2), LEV and MEL (M3), and LEV and MIC (M4)combinations for new bioadhesive polymeric matrix dermal systems produced by the casting solvent evaporation technique. The Fouriertransform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and molecular modelling (MM) were used to characterise and evaluate the compatibility between the selected active substances. In the FTIR data, M1, M2, and M4 mixtures presented a good compatibility. DSC revealed different chemical interactions as the temperature rose above 160°C, especially for M3 and M4. Through MM technique, interactions were found on the M2 and M3 mixtures. Following the correlation of all obtained results, the best compatibility was found to be on M1 and M4 combinations. Rezumat Adapalenul (ADA), levofloxacina (LEV), meloxicamul (MEL) şi nitratul de miconazol (MIC) au fost selectate ca potenţiale ingrediente active în sistemele de tip film cu eliberare dermică sau transdermică. Scopul acestui studiu este de a evalua compatibilitatea a patru amestecuri binare-ADA şi LEV (M1), ADA şi MIC (M2), LEV şi MEL (M3), şi LEV şi MIC (M4)-combinaţii pentru noi sisteme dermice de tip matriţă polimerică bioadezivă produse prin tehnica de turnare şi evaporare a solventului. Pentru a caracteriza şi evalua compatibilitatea dintre substanţele active selectate au fost utilizate spectroscopia cu transformată Fourier (FTIR), calorimetria cu scanare diferenţială (DSC) şi modelarea moleculară (MM). Din datele FTIR, amestecurile M1, M2 şi M4 au fost compatibilite. DSC a arătat diferite interacţiuni chimice, în special pentru M3 şi M4, la temperaturi mai mari de 160°C. Prin metoda MM au fost semnalate interacţiuni în combinaţiile M2 şi M3. Ca urmare a corelării tuturor rezultatelor obţinute, cea mai bună compatibilitate a fost găsită în combinaţiile M1 şi M4.

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“…[3][4][5][6] Unfortunately, MX has an extremely low aqueous solubility at physiological pH, which reduces its bioavailability and hinders its clinical application. [7][8][9] Several attempts have been made to improve the bioavailability and therapeutic effect of MX. Nanonization strategies have been shown to be very promising approaches to improve the dissolution.…”

Section: Introductionmentioning

confidence: 99%

A novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects

Chen

Liu

et al. 2018

IJN

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BackgroundThe objective of this study was to develop a more bio-available and safe nanosuspension of meloxicam (MX), which could dramatically improve inflammation targeting.Methods and resultsMX-loaded bovine serum albumin (BSA) nanosuspensions were prepared using acid–base neutralization in aqueous solution and the prepared nanosuspensions were characterized. The results obtained showed that the prepared nanosuspensions had a narrow size distribution with a mean particle size of 78.67±0.22 nm, a polydispersity index of 0.133±0.01, and a zeta potential of −11.87±0.91 mV. The prepared MX nanosuspensions were spherically wrapped by BSA with a smooth surface as shown by transmission electron microscopy. Stability studies showed that the nanosuspensions were physically stable at 4°C with a shelf life of at least 6 months. In the in vitro dissolution test, the MX-loaded BSA nanosuspension (MX-BSA-NS) exhibited sustained release. In addition, an in vivo pharmacokinetic study in rats following intravenous injection showed that the half-life (t1/2), mean residence time (MRT), and area under the concentration–time curve (AUC0–∞) of MX-BSA-NS was increased by 169.83%, 150.13%, and 148.80%, respectively, in comparison with MX conventional solution (MX solution). Furthermore, results from inflammation targeting studies showed that the concentration of MX increased significantly in inflamed tissues but was reduced in normal tissues compared with the MX solution group after injection of MX-BSA-NS.ConclusionThe prepared MX-BSA-NS significantly increased the inflammation-targeting properties and bioavailability of MX, suggesting its potential as a promising formulation for the targeted drug delivery of MX in future clinical applications.

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Strategies for meloxicam delivery to and across the skin: a review

Cited by 24 publications

References 78 publications

"Development of a rapid capillary zone electrophoresis method to quantify Levofloxacin and Meloxicam from transdermal therapeutic systems "

"Development of a rapid capillary zone electrophoresis method to quantify Levofloxacin and Meloxicam from transdermal therapeutic systems "

Compatibility Study of Four Binary Combinations of Active Ingredients for Dermal Film Forming Systems

A novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects

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