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Biomedical subjects

G G Krueger

Publications and source records attributed to G G Krueger.

At least 19 recordsLinked to original sources

The safety and efficacy of tazarotene gel, a topical acetylenic retinoid, in the treatment of psoriasis.

OBJECTIVE: To determine the safety and efficacy of topically applied tazarotene gel in the treatment of mild to moderate psoriatic plaques. DESIGN: Two multicenter, double-blind, randomized studies of 6- and 8-week duration, with an 8-week follow-up in the second study. SETTING: Medical center outpatient dermatology services. PARTICIPANTS: One hundred fifty-three adults with 2 bilateral target plaques on the trunk, legs, or arms. INTERVENTIONS: Vehicle gel or 0.01% and 0.05% tazarotene gel administered twice daily to 45 patients (study A), or 0.05% and 0.1% tazarotene gel administered either once or twice daily to 108 patients (study B). MAIN OUTCOME MEASURES: Treatment success and plaque elevation, scaling, and erythema vs time. RESULTS: The 0.01% tazarotene gel showed minimal efficacy. Applications of 0.05% and 0.1% tazarotene gels administered once or twice daily, resulted in significant improvements in plaque elevation, scaling, erythema, and overall clinical severity as early as 1 week. Treatment success rates (defined as > 75% improvement from baseline) were 45% with 0.05% tazarotene gel vs 13% with vehicle gel after 6 weeks of treatment (P < .05; study A) and ranged from 48% to 63% with the various tazarotene treatment regimens after 8 weeks of treatment (study B). These improvements were evident at the 8-week follow-up. Treatment-related adverse effects were generally limited to mild or moderate local irritation and were less frequent with the treatment regimen administered once daily. CONCLUSION: The 0.05% and 0.1% tazarotene gels demonstrated significant efficacy in the treatment of mild to moderate psoriatic plaques that persisted after cessation of treatment.

Administration, Cutaneous

Consensus workshop on the toxic effects of long-term PUVA therapy.

The possibility that there is an increased risk of melanoma in patients with psoriasis treated with psoralen-UV-A (PUVA) therapy has raised concern on the part of physicians and patients about the long-term safety of this treatment. In response to this concern, the National Psoriasis Foundation sponsored a workshop at which invited participants with expertise in PUVA therapy, psoriasis treatment, melanoma and nonmelanoma skin cancer, and epidemiological and clinical trials were asked to develop a consensus on the following 3 issues: the risk of long-term adverse effects of PUVA therapy with emphasis on nonmelanoma and melanoma skin cancer; the guidelines for physicians and patients for selection and use of PUVA therapy with consideration of the risk-benefit ratio of this treatment compared with the risk-benefit ratios of alternative treatments; and the directions for further evaluation of the long-term effects Of PUVA therapy.

Humans

Topical metronidazole maintains remissions of rosacea.

BACKGROUND: Rosacea is a chronic skin disease that requires long-term therapy. Oral antibiotics and topical metronidazole successfully treat rosacea. Because long-term use of systemic antibiotics carries risks for systemic complications and adverse reactions, topical treatments are preferred. OBJECTIVE: To determine if the use of topical metronidazole gel (Metrogel) could prevent relapse of moderate to severe rosacea. DESIGN: A combination of oral tetracycline and topical metronidazole gel was used to treat 113 subjects with rosacea (open portion of the study). Successfully treated subjects (n = 88) entered a randomized, double-blind, placebo-controlled study applying either 0.75% topical metronidazole gel (active agent) or topical metronidazole vehicle gel (placebo) twice daily (blinded portion of the study). SETTING: Subjects were enrolled at 6 separate sites in large cities at sites associated with major medical centers. SUBJECTS: One hundred thirteen subjects with at least 6 inflammatory papules and pustules, moderate to severe facial erythema and telangiectasia entered the open phase of the study. Eighty-eight subjects responded to treatment with systemic tetracycline and topical metronidazole gel as measured by at least a 70% reduction in the number of inflammatory lesions. These subjects were randomized to receive 1 of 2 treatments: either 0.75% metronidazole gel or placebo gel. INTERVENTIONS: Subjects were evaluated monthly for up to 6 months to determine relapse rates. MAIN OUTCOME MEASURES: Inflammatory papules and pustules were counted at each visit. Relapse was determined by the appearance of a clinically significant increase in the number of papules and pustules. Prominence of telangiectases and dryness (roughness and scaling) were also observed. RESULTS: In the open phase, treatment with tetracycline and metronidazole gel eliminated all papules and pustules in 67 subjects (59%). The faces of 104 subjects (92%) displayed fewer papules and pustules after treatment, and 82 subjects (73%) exhibited less erythema. In the randomized double-blind phase, the use of topical metronidazole significantly prolonged the disease-free interval and minimized recurrence compared with subjects treated with the vehicle. Eighteen (42%) of 43 subjects applying the vehicle experienced relapse, compared with 9 (23%) of 39 subjects applying metronidazole gel (P<.05). The metronidazole group had fewer papules and/or pustules after 6 months of treatment (P<.01). Relapse of erythema also occurred less often in subjects treated with metronidazole (74% vs 55%). CONCLUSION: In a majority of subjects studied, continued treatment with metronidazole gel alone maintains remission of moderate to severe rosacea induced by treatment with oral tetracycline and topical metronidazole gel.

Administration, Cutaneous

Comparative efficacy of once-daily flurandrenolide tape versus twice-daily diflorasone diacetate ointment in the treatment of psoriasis.

BACKGROUND: Flurandrenolide tape has recently been listed as a group I topical corticosteroid. There are no studies that compare this product to group I ointments in the treatment of steroid-responsive dermatoses. OBJECTIVE: Our purpose was to determine the relative efficacy of flurandrenolide (4 microg/cm2) tape versus 0.05% diflorasone diacetate ointment in plaque psoriasis. METHODS: Thirty patients participated in an investigator-blinded, randomized, bilateral paired-comparison study of flurandrenolide tape applied to lesions of one side of the body once daily for up to 16 hours versus diflorasone diacetate ointment applied contralaterally twice daily. Lesions were assessed at baseline, then reevaluated at 2 and 4 weeks. RESULTS: Flurandrenolide tape-treated plaques showed consistently greater clearing in terms of erythema, scaling, induration, and treatment success for all plaques, as well as the subset of knee and elbow plaques, when compared with the lesions receiving diflorasone diacetate ointment. CONCLUSION: The efficacy of flurandrenolide tape in the treatment of psoriatic plaques surpasses that of diflorasone diacetate ointment.

Administration, Topical

Use of cloned genetically modified human fibroblasts to assess long-term survival in vivo.

Because human fibroblasts are easily brought to tissue culture conditions and can be stably transduced with retroviral vectors encoding transgenes ex vivo, genetically modified fibroblasts are frequently considered in strategies to correct disease with gene therapy. This enthusiasm has been dampened by studies showing that transgene expression by genetically modified fibroblasts diminishes with time in vivo, but not in vitro, for reasons that are unclear. We elected to study this problem using cloned human fibroblasts that had been cloned by limiting dilution and stably transduced with a retroviral vector encoding lacZ ex vivo. These were seeded onto a nonbiodegradable nylon matrix that was transplanted to nude mice. Transgene expression was followed prospectively by histologic exam. Data show that human fibroblasts can withstand the pressure of cloning by limiting dilution. In addition, they can be passaged from 10 to > 20 times, and > 1 x 10(20) of genetically modified fibroblasts can be generated as progeny of one cell. Loss of transgene expression by the cloned genetically modified fibroblasts in vivo occurs in an orderly and progressive fashion, but is not complete by 4 months. Neither the loss nor the persistence of expression appear to be random. These observations are most compatible with the thesis that a major cause of the loss of transgene expression in vivo is secondary to apoptosis of the genetically modified fibroblast. Loss of expression of transgenes in senescent genetically modified fibroblasts occurs more rapidly than in their presenescent counterparts in the age-neutral, in vivo setting of the nude mouse.

Animals

Tazarotene gel, a new retinoid, for topical therapy of psoriasis: vehicle-controlled study of safety, efficacy, and duration of therapeutic effect.

BACKGROUND: Topical therapy providing initial improvement and maintenance of effect after treatment of the large majority of patients with limited, mild to moderate psoriasis is not presently available. Previous topical retinoids have generally been either ineffective or too irritating for therapy of psoriasis. OBJECTIVE: Our purpose was to evaluate a new topical retinoid, tazarotene, in the treatment of stable plaque psoriasis during treatment and posttreatment periods. METHODS: In a double-blind manner, 324 patients were randomly selected to receive tazarotene 0.1% or 0.05% gel, or vehicle control, once daily for 12 weeks and were then followed up for 12 weeks after treatment. RESULTS: Of the total, 318 patients could be evaluated. Tazarotene gels were superior (p < 0.05) to vehicle, often as early as treatment week 1, in all efficacy measures: plaque elevation, scaling, and erythema; treatment response; percentage treatment success (patients with > or = 50% improvement); and time to initial success. Efficacy was equivalent on target lesion sites (trunk or limbs and knees or elbows) and overall. A sustained therapeutic effect was observed for 12 weeks after treatment. Tazarotene gel was cosmetically acceptable. There was low systemic absorption, limiting toxicity to local irritation. CONCLUSION: Once-daily tazarotene was effective and safe as a topical monotherapy for plaque psoriasis, providing rapid reduction of signs and symptoms.

Administration, Topical

Cutaneous gene therapy.

Gene therapy efforts in a variety of tissues have foundered on fundamental technologic barriers, such as difficulties in achieving high-efficiency gene transfer to diseased tissues and in sustaining delivered transgene production. The skin offers an attractive tissue for development of approaches to therapeutic gene delivery by virtue of its accessibility for regulation by topical agents, the ease of gene transfer into cutaneous tissues, and the ready ability to monitor the impact of somatic gene transfer. With the ability of the skin to deliver therapeutic polypeptides to the systemic circulation and the recent molecular characterization of monogenic skin diseases, efforts to target genes to the skin are expected to accelerate. The current status of gene therapy efforts is reviewed, with a special focus on the skin.

Animals

Description of the intrafollicular delivery of large molecular weight molecules to follicles of human scalp skin in vitro.

The objective of this study was to ascertain the elements that govern the intrafollicular delivery of large molecules to follicles of human scalp skin in vitro. The experiments were designed to assess the intrafollicular disposition of drug as a function of size, charge, and formulation. First, fluorescein covalently linked to antisense oligonucleotides and rhodamine-conjugated dextrans were topically applied to fresh human scalp skin in vitro. The drug position in the follicle was qualitatively determined by examining histologic sections of hair-bearing skin taken parallel to the skin surface at various depths and dissected hair follicles via fluorescent microscopy. Using radiolabeled antisense oligonucleotides we demonstrated that these cross sections can also be used to quantitatively localize the intrafollicular delivery of large molecules to follicles of human scalp skin in vitro. Experimental results showed that cationic lipid-based formulations enhanced delivery of oligonucleotides within the follicle. The qualitative analysis also illustrated that cationic lipid-based formulations directed the intrafollicular permeation along the junction of the internal and external root sheath. The charged, lower molecular weight (MW) dextrans permeated into all components of the hair follicle, including the hair shaft. The higher MW dextrans were confined to the follicular structures immediately surrounding the hair shaft. The demonstration of quantitation showed that approximately 0.5% of the applied dose was delivered to the hair bulbs and the deeper skin strata within 24 h of a single application. We conclude that topically applied agents of relatively large MW, in properly formulated delivery vehicles; have the potential to reach pharmacologically active concentrations at the hair bulb. It also should be noted that delivery takes place via the junction of the internal and external root sheath.

Dextrans

Quantitative analysis of l-alpha-acetylmethadol, l-alpha-acetyl-N-normethadol, and l-alpha-acetyl-N,N-dinormethadol in human hair by positive ion chemical ionization mass spectrometry.

A sensitive and specific method was developed for the quantitative analysis of l-alpha-acetylmethadol (LAAM), l-alpha-acetyl-N-normethadol (norLAAM), and l-alpha-acetyl-N,N-dinormethadol (dinorLAAM) in hair. In the development of this method, it was determined that sample pretreatment methods performed by the laboratory greatly affect the measured concentrations of drug and metabolite in hair. Deuterated internal standards were added to 20-mg hair samples and the samples digested overnight in a buffered solution of Protease Type VIII enzyme. Digests were extracted by modification of a liquid-liquid extraction procedure developed previously in our laboratory for the analysis of plasma and tissues. Derivatized extracts were analyzed on a Finnigan MAT 4500 mass spectrometer in positive ion chemical ionization mode using methane and ammonia reagent gases, helium carrier gas, and a DB-5MS (30 m, 0.25-micron film thickness) capillary column. The assay was linear to 50 ng/mg hair (r = 0.99) for all three compounds with a limit of quantitation experimentally determined to be 0.5 ng/mg for LAAM and 0.3 ng/mg for norLAAM and dinorLAAM. Intra-assay precision ranged from 1.0 to 10.5% for the three analytes at concentrations of 0.5, 5.0, and 25.0 ng/mg of hair. Interassay precision ranged from 4.7 to 12.9%. The performance of the method was also evaluated for its utility in detecting and quantitating LAAM, norLAAM, and dinorLAAM in hair from rats (n = 6) that had been administered 3 mg/kg LAAM intraperitoneally once daily for five days. LAAM, norLAAM and dinorLAAM were detectable in pigmented hair at concentrations of 1.27 ng/mg (+/-0.04), 1.28 ng/mg (+/-0.014), and 2.89 ng/mg (+/-0.014), respectively. Five laboratory wash solvents were then evaluated for their effect on the measured concentration of LAAM and metabolites in the rat hair. Phosphate buffer and 1% SDS washes substantially reduced the measured LAAM, norLAAM, and dinorLAAM concentrations by at least 30%, which suggests that drug incorporated into hair is removed (extracted) during the laboratory wash procedures. Wash procedures using methanol, methylene chloride, or water reduced the measured concentrations by no more than 20%. Because measured concentrations of LAAM, norLAAM, and dinorLAAM in hair appear to depend on the specific wash procedures used by a laboratory, quantitative data must be interpreted cautiously based on the sample pretreatment conditions.

Animals

Codeine disposition in human hair after single and multiple doses.

OBJECTIVE: We studied the dose-proportion and time-course relationships for the incorporation of codeine into human hair after the administration of three different groups. SUBJECTS: Male volunteers, with dark hair, were given oral codeine either as a single dose of 60 mg (n = 7) or 120 mg (n = 12) or as multiple doses of 30 mg 3 times daily for 5 days (n = 7) (450 mg total dose). METHODS: Blood and urine were collected for various times for up to 72 h after dosing. Scalp hair was collected initially by plucking (up to 4 weeks) and later by cutting for up to 10 weeks. Plasma, urine, proximal 1 cm of hair and distal hair were each analyzed for codeine and its metabolites by positive-ion chemical ionization ion trap gas chromatography/mass spectrometry. RESULTS: Codeine was detected in the proximal 1 cm of hair within 30 min of an oral 120-mg dose. Codeine was not detected in the distal hair segment until 3 weeks after receiving a dose of codeine. Codeine was detected in distal hair segments for at least 10 weeks at 30 pg mg-1 hair following a single 120 mg codeine dose and at 90 pg mg-1 hair following 30 mg codeine 3 times a day for 5 days. Morphine or the glucuronides of codeine or morphine were not detected in the hair specimens of these subjects. CONCLUSION: Codeine is rapidly distributed into the germanitive elements of hair in a dose-proportional manner. A portion of the codeine remains bound as the hair grows and can be detected in distal hair for up to 10 weeks after a single dose.

Administration, Oral

Evaluation of human skin reconstituted from composite grafts of cultured keratinocytes and human acellular dermis transplanted to athymic mice.

This study evaluates the use of composite grafts of cultured human keratinocytes and de-epidermalized, acellular human dermis to close full-thickness wounds in athymic mice. Grafts were transplanted onto athymic mice and studied up to 8 wk. Graft take was excellent, with no instances of infection or graft loss. By 1 wk, the human keratinocytes had formed a stratified epidermis that was fused with mouse epithelium, and by 8 wk the grafts resembled human skin and could be freely moved over the mouse dorsum. Immunostaining for keratins 10 and 16 and for involucrin revealed an initial pattern of epithelial immaturity, which by 8 wk had normalized to that of mature unwounded epithelium. Mouse fibroblasts began to infiltrate the acellular dermis as early as 1 wk. By 8 wk fibroblasts had completely repopulated the dermis, and blood vessels were evident in the most superficial papillary projections. Dermal elements, such as rete ridges and elastin fibers, which were present in the starting dermis, persisted for the duration of the experiment. Grafts using keratinocytes from dark-skinned donors as opposed to light-skin donors had foci of pigmentation as early as 1 wk that progressed to homogenous pigmentation of the graft by 6 wk. These results indicate that melanocytes that persist in vitro are able to resume normal function in vivo. Our study demonstrates that composite grafts of cultured keratinocytes combined with acellular dermis are a useful approach for the closure of full-thickness wounds.

Animals

Disposition of codeine in female human hair after multiple-dose administration.

Studies of the disposition of codeine into the hair of female subjects (n = 7) were performed after a multiple-dose protocol. Caucasian female subjects with dark-brown-to-black hair were administered a total dose of 450 mg codeine over 5 days (30 mg was administered three times a day for 5 days). Analyses of codeine and metabolites in plasma, urine, and hair were performed by positive ion chemical ionization gas chromatography-mass spectrometry (GC-MS) on a Finnigan Magnum" mass spectrometer. Hair was plucked from the scalp for 5 weeks and subsequently cut from the scalp for up to 10 weeks. Prior to analysis, plucked hair specimens were cut into three segments: (a) a proximal, 1-cm segment, which contained the root, (b) the next distal, 3-cm segment, which was closest to the scalp, and (c) a segment containing all remaining hair to the natural hair tip. in female subjects, the mean (plus or minus standard error of the mean) hair concentration of codeine in the proximal, 1-cm segment from plucked hair was 2.7 ng/mg (+/- 0.55) at 12 h after the last codeine dose; 0.44 ng/mg (+/- 0.20) still remained in this segment at 5 weeks. Codeine was detected in the next 3-cm hair segment (above the scalp) at 1 week; the average codeine concentration for 10 weeks in the 3-cm, distal segment was 0.54 ng/mg (+/- O.05). No codeine was detected in the remaining hair segment (to the tip) at any time. In male subjects studied previously, the mean hair concentration of codeine in the proximal, 1-cm hair segment was 2.6 ng/mg (+/- 0.34) at 12 h after the last codeine dose, and no codeine was detected at 5 weeks. Codeine was not detected in the next 3-cm hair segment (above the scalp) until 3 weeks, and the average mean codeine concentration for 10 weeks was 0.09 ng/mg (+/- 0.01). Differences noted between male and female subjects in distal codeine hair concentrations were not explained by plasma pharmacokinetics.

Administration, Oral

Sustained production of human transferrin by transduced fibroblasts implanted into athymic mice: a model for somatic gene therapy.

Somatic gene therapy has been proposed as a means of treating inherited diseases involving defective or absent plasma proteins, viral diseases, and cancer. Introduction of the gene of interest into fibroblasts and implantation of these genetically modified fibroblasts using a skin equivalent system may be an attractive model for gene therapy because skin fibroblasts are easily obtained and propagated in culture. This study evaluated expression of the gene for human transferrin (hTf) by genetically modified fibroblasts in vitro and in vivo. NIH 3T3 fibroblasts, which form non-metastasizing tumors in athymic mice, were transduced with a retroviral vector encoding hTf. The transduced cells were cloned by limiting dilution and hTf production by the cloned cells measured. Two clones of cells producing high levels of hTf were used to seed collagen-coated nylon matrices, which were maintained in culture for up to 53 d. The rate of synthesis of hTf by the seeded matrices was constant after 22 d in vitro. Matrices seeded with cloned, transduced cells were implanted subcutaneously into seven athymic mice, and plasma levels of hTf were assessed biweekly. In all animals, the plasma level of hTf was detectable at week 6 after implantation. Levels of hTf remained elevated in the animals until the implants were removed at week 12. At week 10, the level of hTf in the plasma correlated with tumor volume in tumors less than 2000 mm3 in size. The half-life of hTf in the mice was 39.5 h. In this model, gene expression did not decline for the 12-week observation period.

3T3 Cells

Pathogenesis of psoriasis.

The information summarized in this article supports the "framework hypothesis." The details of cells of the immune system in the pathogenesis are covered elsewhere in this issue. We believe the observations reported herein allow the following conclusions. The entire epidermis of any individual with the psoriatic phenotype has the capacity to express overt clinical disease. Control of expression is linked to a complex interaction of cells of the epidermis, cells of the dermis, cells of the immune system, and possibly other noncellular humoral elements. The keratinocytes of psoriatic patients are unique in that the inherent phenotype has a capacity for hyperproliferation and altered differentiation. Proliferation and differentiation are controlled at the level of the gene. Thus, it is important to consider not only cytokines and growth factors released by the various cell types, but also the role of regulators of transcription, translation, and the modification of the cytokines and growth factors. The large number of alterations of cytokine and growth factor profiles within psoriasis cause us to postulate that the genetic aberration in psoriasis is quite basic, that is, it is proximal to the common element in the cascade of inflammatory events that lead to a lesion of psoriasis. We speculate that such a defect may be in transcription regulatory elements associated with one or more cytokines (or growth factors). This mutation could occur (1) in the regulatory element itself; (2) in the receptor, which binds both ligand and regulatory element; (3) in the ligand (cytokine or growth factor); or (4) in a gene responsible for the control of proliferation that is under the influence of the sites mentioned in 1, 2, and 3. A mutation within a key regulatory element for a gene controlling proliferation could produce the following scenario of lesional expression. Such a mutation will probably result in less affinity for a receptor/ligand complex. Because this regulatory element in interaction with the receptor/ligand complex normally suppresses gene expression of a promoter of proliferation, the result is a phenotype that tends to be more proliferative and less differentiative. Conversely, if such a mutation produced a regulatory element that has increased affinity for a promoter receptor/ligand complex, then the same phenotype can evolve. Because a wide variety of receptor/ligand complexes can modulate each regulatory element, such a genetic defect could have wide-ranging effects on phenotypic expression. Moreover, as this change in affinity for binding the receptor/ligand complexes only represents a change in sensitivity, not total unresponsiveness, one can expand on the scenario to conclude that the clinical phenotype is only expressed once the system is overwhelmed. This scenario fits the information presented. Both keratinocytes and fibroblasts from psoriatic subjects are hyperproliferative, but only under specific culture conditions. Furthermore, psoriatic keratinocytes appear to be relatively resistant to the antiproliferative and prodifferentiative effects of retinoids or the vitamin D analogues that have antipsoriatic activity. If a genetic defect decreases the affinity of a suppressive receptor/ligand complex for the regulatory element of IL-6 or TGF-alpha, for example, then these cells could be relatively resistant to homeostatic regulation by indigenous corticosteroids, vitamin D, and retinoids. This would result in a situation in which any trigger phenomenon that releases a cytokine, whose receptor/ligand complex upregulates this regulatory element, would overwhelm the defective counterregulatory signal. Subsequently, cells in the skin generate additional cytokines that invoke an inflammatory cascade that eventuates in the egress of immune cells into the skin and the evolution of a lesion of psoriasis. Similar scenarios could be derived from mutations in the other pathways described in this article.

Cytokines