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Transdermal Delivery (transdermal + delivery)

Distribution by Scientific Domains
Medical Sciences57%
Chemistry21%

Terms modified by Transdermal Delivery

  • transdermal delivery system
    		•

    Selected Abstracts

    Transdermal Delivery of the Potent Analgesic Dihydroetorphine: Kinetic Analysis of Skin Permeation and Analgesic Effect in the Hairless Rat

    JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 12 2000
    SATOSHI OHMORI
    Dihydroetorphine is an extraordinarily strong opioid analgesic. To assess its effectiveness after topical application in hairless rats we have examined the kinetic analysis of skin permeation through excised skin and the in-vitro reservoir effect of skin, and have investigated the predictability of plasma concentration and analgesic effect following in-vivo transdermal application. Dihydroetorphine was moderately permeable from an aqueous suspension through excised hairless rat skin. Dihydroetorphine flux from drug-dispersed pressure-sensitive adhesive tape was threefold that from the applied aqueous suspension. The fluxes through the abdominal and the dorsal skin during tape application fitted the Fickian diffusion equation well after the tape was removed peeling off the outer layer of the stratum corneum. The relationship between the plasma concentration and the analgesic effect was examined for four different rates of infusion of dihydroetorphine. A non-linear pharmacokinetic disposition was observed. Following abdominal (0.28 cm2, 20,g) and dorsal (0.50 cm2, 35,g) applications of the dihydroetorphine tape, plasma concentration (0.2-0.8 ng mL,1) and analgesic effect were maintained at a suitable level, for more than 8h, until removal of the tape. These profiles were predictable using the combined equation for percutaneous absorption, disposition and the analgesic effect, but the analgesic effect was slightly lower than the predicted value. The results show that it was possible to control the plasma concentration and the analgesic effect of dihydroetorphine by topical application of the analgesic using pressure-sensitive adhesive tape in the hairless rat. It was possible to predict the result using mathematical modelling. [source]

    Controlled Transdermal Delivery of Propranolol Using HPMC Matrices: Design and In-vitro and In-vivo Evaluation

    JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 2 2000
    P. R. P. VERMA
    To improve bioavailability and achieve a smoother plasma-concentration profile as compared with oral administration, a matrix-dispersion-type transdermal delivery system was designed and developed for propranolol using different ratios of hydroxypropyl-methylcellulose (HPMC) K4M, K15M and K100M. Formulations were evaluated for in-vitro dissolution characteristics using a Cygnus' sandwich-patch holder. Drug release followed Higuchi rather than zero-order or first-order kinetics. In-vivo evaluation was carried out on healthy volunteers (21 ± 1.41 years; 60.89 ± 5.35 kg) following the balanced incomplete block design. The dissolution rate constant (k) and data generated from plasma and urine (Cmax, maximum plasma concentration; tmax, time to reach peak plasma concentration; AUC, area under the curve; ke, elimination rate constant; t½e, elimination half-life; ka, absorption rate constant; t½a, absorption half-life) were evaluated statistically by two-way analysis of variance. Statistically excellent correlation was found between the percentage of drug absorbed and Cmax, AUC0,24 and AUC0-,. A highly significant difference (P < 0.001) was observed when Cmax and AUC0-, generated from plasma and urine were compared, but ke, t½e, ka and t½a did not differ significantly (P > 0.1). We conclude that urinary excretion data may be used as a simpler alternative to blood level data in studying the kinetics of absorption and deriving the absorption parameters. [source]

    Transdermal delivery of two antioxidants from different cosmetic formulations

    INTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 1-2 2003
    S. Richert
    Synopsis The efficacy of any cosmetic product containing a functional ingredient is determined by the skin delivery of the active molecule, which is influenced by the type of the vehicle and the molecule itself. This study was designed to compare the percutaneous absorption habits of the antioxidants carcinine and lipoic acid out of various formulations by means of the porcine skin model. Initial evaluation of the in vitro porcine skin model has demonstrated its feasibility for various substances and formulations [1, 2]. Increasing legal requirements for risk assessment in the cosmetic industry have led to the development of this alternative test method. The penetration properties are determined by the OECD Guideline TG 428: Skin Absorption: in vitro Method [3, 4], which allows the use of porcine skin for penetration studies. Porcine skin is used because of its similarity to human skin in terms of its morphology and the essential permeation characteristics [5]. The mass balances for each tested formulation type of the antioxidants show individual penetration behaviours with significant differences. The presented data plainly demonstrate that the lipophilic lipoic acid has a distinct higher penetration potential than the hydrophilic carcinine. The chosen vehicle can enhance or reduce the transdermal delivery of both tested antioxidants. Modern effective cosmetic formulations will work only, if the active ingredients penetrate into the epidermis. In conclusion, the correct selection of a suitable formulation plays an important role during product development. Résumé L'efficacité d'un produit cosmétique ou de son principe actif est définie par l'absorption du principe actif par la peau. Cette action est influencée par la structure moléculaire du principe actif ainsi que par la galénique du produit. Dans cette étude, les taux d'absorption percutanée des agents anti-oxydants Carcinine et Acide Lipoïque intégrés dans différentes formulations cosmétiques ont été comparés avec le modèle de peau porcine. La phase de validation sur plusieurs années du modèle peau porcine in vitro a prouvé qu'il se prête très bien à la détermination de la pénétration percutanée de différentes substances et formulations. Des exigences légales de plus en plus sévères concernant la pratique des tests de sécurité pour les produits cosmétiques ont mené au développement de cette méthode qui remplace les essais sur animaux. La définition des qualités de pénétration se fait selon la directive OECD TG 428 : Skin Absorption : in vitro Method [3, 4] qui permet l'utilisation de la peau porcine provenant des abattoirs pour l'exécution des études de pénétration. Les bilans quantitatifs des formulations testées montrent que les agents anti-oxydants ont des comportements de pénétration différant de manière significative. Les données présentées démontrent très clairement que l'acide Lipoïque, lipophile, possède un potentiel de pénétration bien plus élevé que la Carcinine, hydrophile. La base cosmétique peut aussi réduire ou augmenter le potentiel de pénétration des agents anti-oxydant testés. En résumé, le choix correct d'un type de formulation joue un rôle très important dans le développement d'un produit cosmétique. [source]

    Two Photon Polymerization-Micromolding of Polyethylene Glycol-Gentamicin Sulfate Microneedles

    ADVANCED ENGINEERING MATERIALS, Issue 4 2010
    Shaun D. Gittard
    The use of microneedles for transdermal drug delivery is limited due to the risk of infection associated with formation of channels through the stratum corneum layer of the epidermis. The risk of infection associated with use of microneedles may be reduced by imparting these devices with antimicrobial properties. In this study, a photopolymerization-micromolding technique was used to fabricate microneedle arrays from a photosensitive material containing polyethylene glycol 600 diacrylate, gentamicin sulfate, and a photoinitiator. Scanning electron microscopy indicated that the photopolymerization-micromolding process produced microneedle arrays that exhibited good microneedle-to-microneedle uniformity. An agar plating assay revealed that microneedles fabricated with polyethylene glycol 600 diacrylate containing 2,mg mL,1 gentamicin sulfate inhibited growth of Staphylococcus aureus bacteria. Scanning electron microscopy revealed no platelet aggregation on the surfaces of platelet rich plasma-exposed undoped polyethylene glycol 600 diacrylate microneedles and gentamicin-doped polyethylene glycol 600 diacrylate microneedles. These efforts will enable wider adoption of microneedles for transdermal delivery of pharmacologic agents. [source]

    Electrode design for skin electroporation with minimal nerve stimulation

    EXPERIMENTAL DERMATOLOGY, Issue 9 2004
    U. Pliquett
    Electroporation is an efficient tool for transdermal delivery of water-soluble molecules sizing up to several kDa. The main barrier to these agents is the stratum corneum, a 15 mm thin layer of dead keratinized cells. Once this layer is charged (approximately 50 V) by an outer electric field, structural rearrangements of the lipids create aqueous pathways (electroporation). Due to the high electric field within the stratum corneum, (E = 50 V/15 µm = 33 kV/cm) electrophoresis can drive charged molecules into the deeper skin layers. A major concern is the high electric field required, because nerve stimulation is inconvenient for the patient. Taking advantage of the fact that up to a depth of 50 µm no nervous receptors appear, a confinement of the field within the upper 15 µm would circumvent sensation. Field confinement within the stratum corneum is arranged by a special electrode geometry, an array of 300 µm holes within a 0.5 mm thick dielectric. The bottom, facing the stratum corneum, is metalized with a gap to the holes. The size of this gap (3,10 µm) is critical for the penetration depth of the electric field between the metalized bottom and a distant electrode at the other side of the holes. A drug reservoir is implemented below the distant electrode and the dielectric. [source]

    Transdermal delivery of two antioxidants from different cosmetic formulations

    INTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 1-2 2003
    S. Richert
    Synopsis The efficacy of any cosmetic product containing a functional ingredient is determined by the skin delivery of the active molecule, which is influenced by the type of the vehicle and the molecule itself. This study was designed to compare the percutaneous absorption habits of the antioxidants carcinine and lipoic acid out of various formulations by means of the porcine skin model. Initial evaluation of the in vitro porcine skin model has demonstrated its feasibility for various substances and formulations [1, 2]. Increasing legal requirements for risk assessment in the cosmetic industry have led to the development of this alternative test method. The penetration properties are determined by the OECD Guideline TG 428: Skin Absorption: in vitro Method [3, 4], which allows the use of porcine skin for penetration studies. Porcine skin is used because of its similarity to human skin in terms of its morphology and the essential permeation characteristics [5]. The mass balances for each tested formulation type of the antioxidants show individual penetration behaviours with significant differences. The presented data plainly demonstrate that the lipophilic lipoic acid has a distinct higher penetration potential than the hydrophilic carcinine. The chosen vehicle can enhance or reduce the transdermal delivery of both tested antioxidants. Modern effective cosmetic formulations will work only, if the active ingredients penetrate into the epidermis. In conclusion, the correct selection of a suitable formulation plays an important role during product development. Résumé L'efficacité d'un produit cosmétique ou de son principe actif est définie par l'absorption du principe actif par la peau. Cette action est influencée par la structure moléculaire du principe actif ainsi que par la galénique du produit. Dans cette étude, les taux d'absorption percutanée des agents anti-oxydants Carcinine et Acide Lipoïque intégrés dans différentes formulations cosmétiques ont été comparés avec le modèle de peau porcine. La phase de validation sur plusieurs années du modèle peau porcine in vitro a prouvé qu'il se prête très bien à la détermination de la pénétration percutanée de différentes substances et formulations. Des exigences légales de plus en plus sévères concernant la pratique des tests de sécurité pour les produits cosmétiques ont mené au développement de cette méthode qui remplace les essais sur animaux. La définition des qualités de pénétration se fait selon la directive OECD TG 428 : Skin Absorption : in vitro Method [3, 4] qui permet l'utilisation de la peau porcine provenant des abattoirs pour l'exécution des études de pénétration. Les bilans quantitatifs des formulations testées montrent que les agents anti-oxydants ont des comportements de pénétration différant de manière significative. Les données présentées démontrent très clairement que l'acide Lipoïque, lipophile, possède un potentiel de pénétration bien plus élevé que la Carcinine, hydrophile. La base cosmétique peut aussi réduire ou augmenter le potentiel de pénétration des agents anti-oxydant testés. En résumé, le choix correct d'un type de formulation joue un rôle très important dans le développement d'un produit cosmétique. [source]

    Transdermal Clonidine Skin Reactions

    JOURNAL OF CLINICAL HYPERTENSION, Issue 2 2002
    L. Michael Prisant MD
    The clonidine transdermal therapeutic system is being used as a therapy for blood pressure treatment. Systemic side effects seem to be fewer than with oral clonidine. However, localized skin reactions occur frequently and the incidence increases with the dose and duration of use. Common signs include erythema, scaling, vesiculation, excoriation, and induration. Allergic contact dermatitis is less frequent but common. Hyperpigmentation and depigmentation also occur. Pretreatment with 0.5% hydrocortisone is associated with less skin irritation and higher blood levels. Although oral clonidine is no longer widely used in the management of hypertension, awareness of these reactions to the transdermal delivery of this agent is important. [source]

    Elastic liposomes mediated transdermal delivery of an anti-hypertensive agent: Propranolol hydrochloride

    JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 1 2007
    Dinesh Mishra
    Abstract One major problem encountered in transdermal drug delivery is the low permeability of drugs through the skin barrier. In the present investigation ultradeformable lipid vesicles, that is, elastic liposomes were prepared incorporating propranolol hydrochloride for enhanced transdermal delivery. Elastic liposomes bearing propranolol hydrochloride were prepared by conventional rotary evaporation method and characterized for various parameters including vesicles shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, turbidity, and in vitro drug release. In vitro flux, enhancement ratio (ER), and release pattern of propranolol hydrochloride were calculated for transdermal delivery. In vivo study conducted on male albino rats (Sprague Dawley) was also taken as a measure of performance of elastic liposomal, liposomal, and plain drug solution. The better permeation through the skin was confirmed by confocal laser scanning microscopy (CLSM). Results indicate that the elastic liposomal formulation for transdermal delivery of propranolol hydrochloride provides better transdermal flux, higher entrapment efficiency, ability as a self-penetration enhancer and effectiveness for transdermal delivery as compared to liposomes. © 2006 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 96:145,155, 2007 [source]

    Effect of lipid bilayer alteration on transdermal delivery of a high-molecular-weight and lipophilic drug: Studies with paclitaxel

    JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 9 2004
    Ramesh Panchagnula
    Abstract Skin forms an excellent barrier against drug permeation, due to the rigid lamellar structure of the stratum corneum (SC) lipids. Poor permeability of drugs can be enhanced through alteration in partition and diffusion coefficients, or concentration gradient of drug with an appropriate choice of solvent system, along with penetration enhancers. The aim of the current investigation was to assess applicability of lipid bilayer alteration by fatty acids and terpenes toward the permeation enhancement of a high-molecular-weight, lipophilic drug, paclitaxel (PCL) through rat skin. From among the fatty acids studied using ethanol/isopropyl myristate (1:1) vehicle, no significant enhancement in flux of PCL was observed (p,>,0.05). In the case of cis mono and polyunsaturated fatty acids lag time was found to be similar to control (p,>,0.05). This suggests that the permeation of a high-molecular-weight, lipophilic drug may not be enhanced by the alteration of the lipid bilayer, or the main barrier to permeation could lie in lower hydrophilic layers of skin. A significant increase in lag time was observed with trans unsaturated fatty acids unlike the cis isomers, and this was explained on the basis of conformation and preferential partitioning of fatty acids into skin. From among the terpenes, flux of PCL with cineole was significantly different from other studied terpenes and controls, and after treatment with menthol and menthone permeability was found to be reduced. Menthol and menthone cause loosening of the SC lipid bilayer due to breaking of hydrogen bonding between ceramides, resulting in penetration of water into the lipids of the SC lipid bilayer that leads to creation of new aqueous channels and is responsible for increased hydrophilicity of SC. This increased hydrophilicity of the SC bilayer might have resulted in unfavorable conditions for ethanol/isopropyl myristate (1:1) along with PCL to penetrate into skin, therefore permeability was reduced. The findings of this study suggest that the permeation of a high-molecular-weight and lipophilic drug cannot be enhanced through bilayer alteration by penetration enhancers, and alteration in partitioning of drug into skin could be a feasible mode to enhance the permeation of drug. © 2004 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 93:2177,2183, 2004 [source]

    Combined strategies for enhancing the transdermal absorption of midazolam through human skin

    JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 9 2010
    Cristina Balaguer-Fernández
    Abstract Objectives, Midazolam administration by intravenous or intramuscular injection produces pain and stress. For this reason, alternative methods of administration have been proposed. The transdermal administration of midazolam could improve patient comfort, which is especially important for children in the pre-operative period. We aimed to assess the effect of iontophoresis and chemical percutaneous enhancers applied individually and together, to determine if a synergistic effect is achieved when both enhancement techniques are simultaneously employed. Methods, This work reports the characterization of the passive diffusion of midazolam hydrochloride through human skin in vitro and evaluates the effect of iontophoresis application and chemical percutaneous enhancers on said diffusion when employed both individually and in combination. Key findings, Percutaneous absorption assays demonstrated that the physical technique of iontophoresis, when applied alone, moderately increased midazolam hydrochloride permeation flux through human skin, producing a similar effect to that obtained with R -(+)-limonene chemical enhancer. Among the strategies assayed, it was observed that Azone produced the most pronounced enhancement effect when applied separately. The combination of pre-treatment with Azone and iontophoresis exhibited a higher capacity for enhancing the transdermal flux of midazolam through human skin than Azone alone. Conclusions, In conclusion, when applied individually, Azone exhibited the greatest enhancement effect on the transdermal diffusion of midazolam of the various strategies assayed. The combination of Azone and iontophoresis produce the highest transdermal steady-state flux of midazolam but no synergic effect was achieved when the two enhancement strategies were applied in combination, showing that although selecting the best conditions for iontophoresis application, it is less effective for augmenting the transdermal delivery of midazolam than the chemical enhancer Azone. [source]

    Ester prodrugs of morphine improve transdermal drug delivery: a mechanistic study

    JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 7 2007
    Jhi-Joung Wang
    Two alkyl esters of morphine, morphine propionate (MPR) and morphine enanthate (MEN), were synthesized as potential prodrugs for transdermal delivery. The ester prodrugs could enhance transdermal morphine delivery. The mechanisms of this enhancing effect were elucidated in this study. Both prodrugs were more lipophilic than their parent drug as evaluated by the skin/vehicle partition coefficient (log P) and capacity factor (log K,). The in-vitro skin permeation of morphine and its prodrugs from pH 6 buffer was in the order of MEN > MPR > morphine. MPR and MEN respectively enhanced the transdermal delivery of morphine by 2- and 5-fold. A contrary result was observed when using sesame oil as the vehicle. The prodrugs were stable against chemical hydrolysis in an aqueous solution, but were readily hydrolysed to the parent drug when exposed to skin homogenate and esterase. Approximately 98% MPR and ,75% MEN were converted to morphine in an in-vitro permeation experiment. The viable epidermis/dermis contributed to a significant resistance to the permeation of ester prodrugs. According to the data of skin permeation across ethanol-, ,-terpineol-, and oleic acid-pretreated skin, MEN was predominantly transported via lipid bilayer lamellae in the stratum corneum. The intercellular pathway was not important for either morphine or MPR permeation. [source]

    Ion-pair Formation as a Strategy to Enhance Topical Delivery of Salicylic Acid

    JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 8 2000
    STELLA A. MEGWA
    An in-vitro study was carried out to determine the possibility of improving the efficiency of transdermal delivery of salicylate through human epidermis by ion-pair formers (alkylamines and quaternary ammonium ions). Further, the relationship between the physico-chemical properties of the counter-ions and salicylate flux was examined. It was found that flux can be related to the conductivity associated with the penetrant solution, molecular size of the counter-ion and lipophilicity expressed as either octanol/water partition coefficient of the ion pairs or the carbon chain-length of the counter-ions. Equations have been developed to predict salicylate flux from these physicochemical parameters. [source]

    Skin Permeation of Testosterone and its Ester Derivatives in Rats

    JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 4 2000
    MI-KYEONG KIM
    To establish the optimum conditions for improving the transdermal delivery of testosterone, we studied the relationship between the lipophilicity of testosterone ester derivatives and the rat skin permeation rate of testosterone. We performed a rat skin permeation study of testosterone and its commercially available ester derivatives, testosterone hemisuccinate, testosterone propionate and testosterone-17,-cypionate, using an ethanol/water co-solvent system. The aqueous solubility and rat skin permeation rate of each drug, saturated in various compositions of an ethanol/water system, was determined at 37°C. The aqueous solubility of testosterone and its ester derivatives increased exponentially as the volume fraction of ethanol increased up to 100% (v/v). The stability of testosterone propionate in both the skin homogenate and the extract was investigated to observe the enzymatic degradation during the skin permeation process. Testosterone propionate was found to be stable in the isotonic buffer solution and in the epidermis-side extract for 10 h at 37°C. However, in the skin homogenate and the dermis-side extract testosterone propionate rapidly degraded producing testosterone, implying that testosterone propionate rapidly degraded to testosterone during the skin permeation process. The steady-state permeation rates of testosterone in the ethanol/water systems increased exponentially as the volume fraction of ethanol increased, reaching the maximum value (2.69 ± 0.69 ,g cm,2 h,1) at 70% (v/v) ethanol in water, and then decreasing with further increases in the ethanol volume fraction. However, in the skin permeation study with testosterone esters saturated in 70% (v/v) ethanol in water system, testosterone esters were hardly detected in the receptor solution, probably due to the rapid degradation to testosterone during the skin permeation process. Moreover, a parabolic relationship was observed between the permeation rate of testosterone and the log P values of ester derivatives. Maximum flux was achieved at a log P value of around 3 which corresponded to that of testosterone (log P = 3.4). The results showed that the skin permeation rate of testosterone and its ester derivatives was maximized when these compounds were saturated in a 70% ethanolic solution. It was also found that a log P value of around 3 is suitable for the skin permeation of testosterone related compounds. [source]

    Photomechanical transdermal delivery of insulin in vivo

    LASERS IN SURGERY AND MEDICINE, Issue 3 2001
    Shun Lee PhD
    Abstract Background and Objective Previous studies have shown that photomechanical waves transiently permeabilize the stratum corneum in vivo. The aim of the present work was to investigate the potential of photomechanical waves for systemic drug delivery. Study Design/Materials and Methods Photomechanical waves were generated by ablation of a polystyrene target by a Q-switched ruby laser. Systemic insulin delivery in a streptozotocin-diabetic rat model was monitored by measuring the blood glucose level. Results After photomechanical insulin delivery, the blood glucose decreased 80 ,±, 3% and remained below 200 mg/dl for more than 3 hours. Whereas in control experiments (for which insulin was applied without photomechanical waves), there was no dramatic change in the blood glucose (standard deviation of measurements over 4 hours was 7%). Conclusion The application of the photomechanical waves allowed ,6-kDa protein molecules (insulin) to pass through the stratum corneum and into the systemic circulation. Lasers Surg. Med. 28:282,285, 2001. © 2001 Wiley-Liss, Inc. [source]

    Gene therapy for psoriasis in the K14-VEGF transgenic mouse model by topical transdermal delivery of interleukin-4 using ultradeformable cationic liposome

    THE JOURNAL OF GENE MEDICINE, Issue 6 2010
    Jiong Li
    Abstract Background Topical transdermal gene delivery to the skin shows great potential for painless, non-invasive administration of vaccines and therapeutic agents. Interleukin (IL)-4 strategies have shown a good antipsoriatic effect in clinic trials. To date, no information has been acquired on the effectiveness of gene therapy for psoriasis in the K14-VEGF transgenic mouse model by topical transdermal penetration of murine IL-4 (mIL-4) using ultradeformable cationic liposome (UCL). Methods In the present study, we synthesized an UCL and determined a suitable formula for transdermally delivering plasmid DNA to mouse skin. We then tested the antipsoriatic efficacy in the K14-VEGF transgenic mouse model by transdermal delivery of mIL-4 using UCL. Results We found that plasmid DNA was transdermally delivered to vicinal sites of epidermis and hair follicles using this optimized formula. Plasmid DNA expression was detected in ear skin. Twenty-four hours after topical application, plasmid DNA was not detected in blood serum and liver, which may decrease the risk of insertion of promoter from plasmid to genomic DNA. Mice treated with UCL/mIL-4 displayed a mild psoriasis phenotype. Histological analysis of pathological score using the Baker scoring system revealed an antipsoriatic effect. Immunohistochemical analysis revealed that hyperplastic and inflamed vessels were suppressed. Conclusions These observations provide evidence of antipsoriatic efficacy by topical transdermal delivery of mIL-4. Therefore, topical transdermal gene transfer is attractive and offers future potential for application in human patients with other dermatogic diseases. Copyright © 2010 John Wiley & Sons, Ltd. [source]

    Transdermal drug delivery by coated microneedles: geometry effects on drug concentration in blood

    ASIA-PACIFIC JOURNAL OF CHEMICAL ENGINEERING, Issue 6 2009
    Barrak Al-Qallaf
    Abstract Drug administration through transdermal delivery is restricted by the top layer of skin, the stratum corneum. One possible solution to overcome the barrier function of the stratum corneum is to employ microneedle arrays. However, detailed theoretical models relating drug-coated microneedles and their geometry to the drug concentration in the blood are limited. This article aims to address this issue by examining the blood concentration profiles for a model drug, insulin, that has been administered via coated microneedles. A mathematical model is introduced and applied to predict theoretical blood concentrations. Furthermore, the insulin concentration in blood is calculated for a range of different microneedle shapes and dimensions to identify the most effective geometry. The results indicate that the optimum microneedle geometry in terms of maximizing insulin concentration was a rocket-shaped needle with a constant tip angle of 90°. Also, it has been found that the number of microneedles in an array is the most significant factor in determining maximum insulin concentration in the blood (Cb, max). Penetration depth of the microneedle, centre-to-centre spacing and microneedle thickness had a less significant effect on the maximum insulin concentration in the blood. It is envisaged that the current study will help in designing microneedles of optimum size and shape for transdermal drug delivery. Copyright © 2009 Curtin University of Technology and John Wiley & Sons, Ltd. [source]