Pretreatment with Skin Permeability Enhancers: Importance of Duration and Composition on the Delivery of Diclofenac Sodium

Maurya, Abhijeet; Murthy, S. Narasimha

doi:10.1002/jps.23938

Cited by 21 publications

(3 citation statements)

References 44 publications

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“…Compared to rats treated with TMP-ME alone, a 1.25-fold increase in C max , a 0.93-fold decrease in T max , and a 0.88-fold increase in AUC 0–t were observed for TMP in rats treated with MN-assisted TMP-ME ( p < 0.05). These results suggest that the rate and extent of percutaneous TMP absorption can be enhanced significantly by the application of MN-assisted TMP-ME, which is consistent with previous reports [ 29 ].…”

Section: Resultssupporting

confidence: 93%

Microneedle-Assisted Percutaneous Delivery of a Tetramethylpyrazine-Loaded Microemulsion

Qiang

et al. 2017

Molecules

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This study examined the efficacy of the percutaneous delivery of a tetramethylpyrazine-loaded microemulsion (TMP-ME) on skin pretreated with microneedles (MN). The TMP-ME formulation was optimized in vitro with skin permeation experiments, using a uniform experimental design, guided by a pseudo-ternary phase diagram, in which the TMP skin permeation level and mean particle size were indices. The effects of MN pretreatment on skin permeation by TMP-ME were assessed using in vitro skin permeation, in vivo skin microdialysis, and pharmacokinetic studies in rats. The influence of MN pretreatment on the skin barrier function was evaluated by measuring the electrical resistance of rat skin before and after MN insertion. In the optimal formulation of TMP-ME, the weight percentages of Maisine® 35-1 (oil phase), Labrasol® (surfactant), and Transcutol® P (co-surfactant) were 7%, 30% and 10%, respectively, with 1.5% TMP loading. In the in vitro skin permeation study, MN-assisted TMP-ME exhibited a two-fold increase in a 24-h cumulative TMP permeation compared with TMP-ME alone (p < 0.05). In the skin microdialysis study, TMP in MN-assisted TMP-ME exhibited a 1.25-fold increase in Cmax, a 0.93-fold decrease in Tmax, and a 0.88-fold increase in AUC0–t (p < 0.05). Similarly, in the pharmacokinetic study, TMP in MN-assisted TMP-ME exhibited a 2.11-fold increase in Cmax, a 0.67-fold decrease in Tmax, and a 1.07-fold increase in AUC0–t (p < 0.05). The percutaneous electrical resistance of rat skin before and after MN insertion was 850 ± 50 Ω/cm2 and 283 ± 104 Ω/cm2 respectively, indicating that MN dramatically compromises the skin barrier. These results suggest that MN assistance increases the skin permeation rate and the extent of percutaneous absorption of TMP-ME, and that the mechanism may involve the reversible barrier perturbation effect. The rate and extent of percutaneous absorption of TMP-ME can be significantly enhanced by MN assistance, possibly because MN causes a reversible barrier perturbation effect on skin.

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Section: Resultssupporting

confidence: 93%

Microneedle-Assisted Percutaneous Delivery of a Tetramethylpyrazine-Loaded Microemulsion

Qiang

et al. 2017

Molecules

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“…Suitable dilutions were made with acetonitrile followed by vortexing and centrifuging the solutions. The supernatant was then analyzed for the drug content in the epidermis using HPLC (Maurya and Murthy, 2014).…”

Section: Methodsmentioning

confidence: 99%

Development of poloxamer gel formulations via hot-melt extrusion technology

Mendonsa

Murthy

Hashemnejad

et al. 2018

International Journal of Pharmaceutics

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Poloxamer gels are conventionally prepared by the "hot" or the "cold" process. But these techniques have some disadvantages such as high energy consumption, requires expensive equipment and often have scale up issues. Therefore, the objective of this work was to develop poloxamer gels by hot-melt extrusion technology. The model drug selected was ketoprofen. The formulations developed were 30% and 40% poloxamer gels. Of these formulations, the 30% poloxamer gels were selected as ideal gels. DSC and XRD studies showed an amorphous nature of the drug after extrusion. It was observed from the permeation studies that with increasing poloxamer concentration, a decrease in drug permeation was obtained. Other studies conducted for the formulations included in-vitro release studies, texture analysis, rheological studies and pH measurements. In conclusion, the hot-melt extrusion technology could be successfully employed to develop poloxamer gels by overcoming the drawbacks associated with the conventional techniques.

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“…Several studies have been conducted demonstrating the use of oleic acid as a permeation enhancer in transdermal drug delivery systems (9–13). A few studies have also been conducted using oleic acid as a buccal permeation enhancer.…”

Section: Introductionmentioning

confidence: 99%

Bioadhesive Drug Delivery System for Enhancing the Permeability of a BCS Class III Drug via Hot-Melt Extrusion Technology

et al. 2017

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As the buccal route of administration has the ability to avoid the GI tract and first pass effect by directing the absorption towards the cheek area, the bioavailability of BCS class III drugs can be increased through this route. Only a handful of studies have been conducted using oleic acid as a permeation enhancer in any transbuccal drug delivery system. Therefore the objective of this novel study was to develop a buccal tablet using two concentrations of oleic acid for a model BCS class III drug via hot-melt extrusion technology and to investigate the effects of oleic acid on the physicochemical properties of the tablet. The model drug selected was ondansetron hydrochloride. Formulations consisting of the polymers (hydroxypropyl methylcellulose and polyethylene oxide) and two concentrations of oleic acid were prepared by hot-melt extrusion techniques. A melting point depression of the drug was obtained in the extruded granules as seen by the DSC thermograms. The ex-vivo permeation studies showed a greater permeation of the drug in the formulation containing 10% oleic acid (F2) as compared to the formulation containing 20% oleic acid (F1), although not statistically significant. The in-vitro bioadhesion studies, swelling studies and surface pH measurements of the tablets were also conducted. In conclusion, permeation studies exhibited the potential of oleic acid as a buccal permeation enhancer as a significant permeation of the drug was obtained in the formulations. Hot-melt extrusion technology was successfully employed to formulate buccal tablets of ondansetron hydrochloride.

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Pretreatment with Skin Permeability Enhancers: Importance of Duration and Composition on the Delivery of Diclofenac Sodium

Cited by 21 publications

References 44 publications

Microneedle-Assisted Percutaneous Delivery of a Tetramethylpyrazine-Loaded Microemulsion

Microneedle-Assisted Percutaneous Delivery of a Tetramethylpyrazine-Loaded Microemulsion

Development of poloxamer gel formulations via hot-melt extrusion technology

Bioadhesive Drug Delivery System for Enhancing the Permeability of a BCS Class III Drug via Hot-Melt Extrusion Technology

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