Dermal and Transdermal Drug Delivery Systems: Current and Future Prospects

Brown, Marc; Martin, Gary P.; Jones, Stuart A.; Akomeah, Franklin K.

doi:10.1080/10717540500455975

Cited by 569 publications

(357 citation statements)

References 96 publications

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“…The systemic drug administration through the skin holds several advantages such as the maintenance of constant drug levels in the blood, decrease of side effects, improvement of bioavailability by circumvention of hepatic first pass metabolism and increased patient compliance [1].…”

Section: Introductionmentioning

confidence: 99%

Films based on chitosan polyelectrolyte complexes for skin drug delivery: Development and characterization

Silva

Pereira

Ramalho

et al. 2008

Journal of Membrane Science

117

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a b s t r a c tNovel chitosan based polyelectrolyte complexes (PEC) were developed and optimized in order to obtain films possessing the optimal functional properties (flexibility, resistance, water vapour transmission rate and bioadhesion) to be applied on skin. The development was based on the combination of chitosan and two polyacrylic acid (PAA) polymers with different crosslinkers and crosslinking densities. The interaction between the polymers was maximized controlling the pH, and by forming the films at a pH value close to the pK a of the respective components as identified by potentiometric and turbidimetric titrations. The action of glycerol, PEG200, Hydrovance and trehalose upon the functional properties of the films was also evaluated. Glycerol was found to improve the film properties in terms of flexibility, resistance and water vapour transmission rate (WVTR) with a maximum effect at 30%. The application of a pressure sensitive adhesive (PSA) significantly improved bioadhesion with a negligible influence in the resistance and flexibility of the films.The optimized film, including adhesive, has shown very good properties for application in the skin and represents a very promising formulation for further incorporation of drugs for topical and transdermal administration.

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Section: Introductionmentioning

confidence: 99%

Films based on chitosan polyelectrolyte complexes for skin drug delivery: Development and characterization

Silva

Pereira

Ramalho

et al. 2008

Journal of Membrane Science

117

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“…These results are in agreement with the findings reported earlier (21,22). Upon statistical evaluation (two-way ANOVA), a significant difference was observed between the test products (p < 0.01) but not within the test products for AUC (0)(1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12) , AUC (0-24) , AUC (0-∞) , t 1/2, K el and MRT values. Spearman rank correlation, a non-parametric statistical test, demonstrated a high degree of positive correlation, showing complete agreement in the order of ranks between the percentage of drug absorbed from patches and C max (p < 0.02; two tails), AUC (0-24) (p < 0.02; two tails) and AUC (0-∞) (p < 0.02; two tails).…”

Section: In Vivo Studies In Rabbitsmentioning

confidence: 99%

“…and anti-arthritic drugs, are being investigated and developed for the transdermal therapeutic system either for academic research or for commercial purposes (3,4). The present work is aimed at developing a matrix-dispersion type transdermal drug delivery of pentazocine.…”

mentioning

confidence: 99%

Development of matrix controlled transdermal delivery systems of pentazocine: In vitro/in vivo performance

Verma

Chandak²

2009

Acta Pharmaceutica

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Transdermal drug delivery system is being extensively investigated as a viable alternative to drug delivery with improved bioavailability. It offers many advantages over conventional administration such as enhanced efficacy, increased safety, and greater convenience and improved patient compliance. Transdermal route permits the use of a relatively potent drug with minimal risk of systemic toxicity and avoids gastrointestinal degradation and hepatic first-pass metabolism (1-3). A number of therapeutic agents, including antihypertensive, antianginal, antihistaminic, anti-inflammatory, analgesic, The present study aimed to develop hydroxypropyl methylcellulose based transdermal delivery of pentazocine.In formulations containing lower proportions of polymer, the drug released followed the Higuchi kinetics while, with an increase in polymer content, it followed the zero-order release kinetics. Release exponent (n) values imply that the release of pentazocine from matrices was non-Fickian. FT-IR, DSC and XRD studies indicated no interaction between drug and polymer. The in vitro dissolution rate constant, dissolution half-life and pharmacokinetic parameters (C max , t max , AUC (s) , t 1/2, K el , and MRT) were evaluated statistically by two-way ANOVA. A significant difference was observed between but not within the tested products. Statistically, a good correlation was found between per cent of drug absorbed from patches vs. C max and AUC (s) . A good correlation was also observed when per cent drug released was correlated with the blood drug concentration obtained at the same time point. The results of this study indicate that the polymeric matrix films of pentazocine hold potential for transdermal drug delivery.Keywords: pentazocine, transdermal drug delivery, Cygnus' sandwich patch holder, in vitro characterization, in vivo evaluation * Correspondence; e-mail: prpverma275730@yahoo.com Unauthenticated Download Date | 8/28/18 7:56 PM and anti-arthritic drugs, are being investigated and developed for the transdermal therapeutic system either for academic research or for commercial purposes (3, 4). The present work is aimed at developing a matrix-dispersion type transdermal drug delivery of pentazocine.Pentazocine (PTZ), a benzomorphan derivative, is an opioid analgesic that has mixed opioid agonist and antagonist actions. It is considered to be a partial agonist or weak antagonist at the m-receptor and a k-receptor agonist. Pentazocine is used for relief of moderate to severe pain. Oral administration of PTZ has the disadvantage of low bioavailability (about 18-22 %) due to extensive first-pass metabolism (5-7). In addition, PTZ has a short half-life of 2-4 h and requires frequent dosing in order to maintain the optimal therapeutic concentration. Repeated injections over long periods may cause fibrotic changes in the skin and muscular tissue. Low molecular mass (285.4), suitable pK a values of 8.5 and 10, log P (octanol/phosphate buffer pH 7.4) of 2.0 and low oral bioavailability provide a rationale for developing a...

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“…Since a drug molecule that is larger than 500 Da cannot pass through the 408 SC layer passively [36], we define that the diffusion coefficient for insulin (MW: 5808 Da) in the 409 SC layer is negligible. The histological images also indicate that the MNs partially break the SC 410 layer and mass transfer distance between the drug solution and the receptor compartment in a 411 FDC is reduced.…”

Section: Calculation Of Mn Insertion Depths Based On Histological Imamentioning

confidence: 99%

A New Paradigm for Numerical Simulation of Microneedle-Based Drug Delivery Aided by Histology of Microneedle-Pierced Skin

Han

Das

2015

Journal of Pharmaceutical Sciences

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Microneedle (MN) is a relatively recent invention and an efficient technology for transdermal 8 drug delivery (TDD). Conventionally, the mathematical models of MNs drug delivery define the 9 shape of the holes created by the MNs in the skin as the same as their actual geometry. 10 Furthermore, the size of the MN holes in the skin is considered to be either the same or a 11 certain fraction of the lengths of the MNs. However, the histological images of the MN treated 12 skin indicate that the real insertion depth is much shorter than the length of the MNs and the 13 shapes may vary significantly from one case to another. In addressing these points, we propose 14 a new approach for modelling MN based drug delivery, which incorporate the histology of MN 15 pierced skin using a number of concepts borrowed from image processing tools. It is expected 16 that the developed approach will provide better accuracy of the drug diffusion profile. A new 17 computer program is developed to automatically obtain the outline of the MNs treated holes and 18 import these images into computer software for simulation of drug diffusion from MN systems. 19This method can provide a simple and fast way to test the quality of MNs design and modelling, 20 as well as simulate experimental studies, e.g., permeation experiments on MN pierced skin 21 using diffusion cell. The developed methodology is demonstrated using two dimensional (2D) 22 numerical modelling of flat MNs (2D). However, the methodology is general and can be 23 implemented for 3D MNs if there is sufficient number of images for reconstructing a 3D image 24 for numerical simulation. Numerical modelling for 3D geometry is demonstrated by using 25 images of an ideal 3D MN. The methodology is not demonstrated for real 3D MN as there are 26 not sufficient numbers of images for the purpose of this paper. 27

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Dermal and Transdermal Drug Delivery Systems: Current and Future Prospects

Cited by 569 publications

References 96 publications

Films based on chitosan polyelectrolyte complexes for skin drug delivery: Development and characterization

Films based on chitosan polyelectrolyte complexes for skin drug delivery: Development and characterization

Development of matrix controlled transdermal delivery systems of pentazocine: In vitro/in vivo performance

A New Paradigm for Numerical Simulation of Microneedle-Based Drug Delivery Aided by Histology of Microneedle-Pierced Skin

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