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PubMed2006

Effect of DC/mDC iontophoresis and terpenes on transdermal permeation of methotrexate: in vitro study.

The systemic toxicity caused by methotrexate limits its use and transdermal delivery would be a possible alternative. Transdermal permeation of methotrexate loaded into polyacrylamide-based hydrogel patch, across mice skin was studied in vitro after pretreatment with terpenes and ethanol, alone or in combination with iontophoresis (DC/mDC). Polyacrylamide patches gave the maximum flux as compared to the copolymers of acrylamide and acrylic acid. Of the terpenes used, pure menthol showed maximum enhancement (38%), whereas pure limonene elicited a minimum of 9.9% enhancement. Binary combination of menthol and ethanol increased the permeation to 54.9%, which was further enhanced to 93.69% and 117% when used in combination with DC and square wave (mDC) iontophoresis, respectively. ATR-FTIR of the stratum corneum treated with terpenes showed a split in the asymmetric C-H stretching vibrations along with decrease in peak heights and areas of asymmetric, symmetric C-H stretching, C=O stretching and amide bands. A split in amide II band was observed with iontophoresis. ATR-FTIR studies suggest conformational changes in the lipid-protein domains thereby increasing permeation. Histopathological studies on treated skin samples, gave an insight about the anatomical changes brought by the application of various enhancers. Binary mixture of menthol and ethanol in combination with square wave gave best results.

Acrylic Resins↗
PubMed1997

Efficacy and tolerability of Estraderm MX, a new estradiol matrix patch.

OBJECTIVES: To assess the efficacy and tolerability of a new matrix patch delivering 0.05 mg estradiol per day (Estraderm MX 50) in postmenopausal women with moderate to severe postmenopausal symptoms. METHODS: A multicenter, double-blind, randomized, between-patient, placebo controlled trial in 109 postmenopausal women was carried out. Patches were applied twice weekly for 12 weeks. Patients were assessed at 4, 8 and 12 weeks of treatment. The primary efficacy variable was change from baseline in mean number of moderate to severe hot flushes (including night sweats) per 24 h during the last 2 weeks of treatment. Other variables included Kupperman Index, local and systemic tolerability. Plasma concentrations of estradiol (E2), estrone (E1) and estrone sulfate (E1S) were determined before and after treatment. RESULTS: Estraderm MX was significantly superior to placebo (P < 0.001) in reducing mean number of moderate to severe hot flushes (including night sweats) per 24 h after 4, 8 and 12 weeks of treatment. The estimate of treatment group differences after 12 weeks was 4.2 hot flushes (95% confidence interval: 2.6-5.8). Estraderm MX also significantly reduced Kupperman Index at all time points compared to placebo (P < 0.001). Estraderm MX induced increases in mean E2, E1 and E1S plasma levels as expected (E2: baseline 2.7 pg/ml, 12 weeks 38.9 pg/ml; E1: baseline 18.8 pg/ml, 12 weeks 41.6 pg/ml; E1S: baseline 235.6 pg/ml, 12 weeks 765.1 pg/ml). Overall rates of adverse experiences were similar for Estraderm MX and placebo. The number of patients reporting skin irritation was low and similar in both groups. CONCLUSIONS: Estraderm MX 50, a new matrix patch, offers an effective and well tolerated dosage form for transdermal delivery of 0.05 mg E2 per day.

Administration, Cutaneous↗
PubMed2003

Physicochemical characterization and percutaneous delivery of 2,3,5,6-tetramethylpyrazine.

The objective of this work is to investigate the percutaneous permeability of 2,3,5,6-tetramethylpyrazine (TMP), an active ingredient originally isolated from Ligusticum wallichii Franch. Certain physicochemical properties of TMP, including its partition coefficient and pH-solubility profile, were studied. The influence of pH on the percutaneous permeation of TMP was studied in vitro using hairless mouse skin. Comparative in vitro permeability of TMP through hairless mouse, rat, rabbit, and human cadaver skin was also investigated. The results indicate that hairless mouse skin and rat skin were about three to four times more permeable to TMP than human cadaver skin. The permeability of TMP through rabbit skin was not significantly different from that of human cadaver skin. The observed lag times for all skin membranes were about 1-2h. Although pharmacokinetic data are not currently available to permit precise calculation of a clinically effective patch size, the data from this study indicate that the transdermal delivery of TMP should nevertheless be possible.

Administration, Cutaneous↗
PubMed2001

Effects of adhesives and permeation enhancers on the skin permeation of captopril.

To formulate a transdermal drug delivery system of captopril, monolithic adhesive matrix type patches containing 20% captopril, different pressure-sensitive adhesives, and various permeation enhancers were prepared using a labcoater. The effects of the adhesives and permeation enhancers on skin permeation of captopril from the prepared patches were evaluated using Franz diffusion cells fitted with excised rat skins. The permeation rate of the drug through the excised skin was dependent on the type of polyacrylate copolymers studied. Fatty alcohols resulted in a pronounced enhancing effect on the skin permeation of captopril, while dimethyl sulfoxide, N-methyl-2-pyrrolidone, oleic acid, Transcutol, and polysorbate 20 showed no significant enhancing effect. The permeation-enhancing effect of the fatty alcohols reached the maximum at the level of 100%. Based on these results, a captopril patch may be developed with further optimization.

Acrylates↗
PubMed2005

Male hypogonadism : an update on diagnosis and treatment.

Male hypogonadism is one of the most common endocrinologic syndromes. The diagnosis is based on clinical signs and symptoms plus laboratory confirmation via the measurement of low morning testosterone levels on two different occasions. Serum luteinizing hormone and follicle-stimulating hormone levels distinguish between primary (hypergonadotropic) and secondary (hypogonadotropic) hypogonadism. Hypogonadism associated with aging (andropause) may present a mixed picture, with low testosterone levels and low to low-normal gonadotropin levels. Androgen replacement therapy in hypogonadal men has many potential benefits: improved sexual function, an enhanced sense of well-being, increased lean body mass, decreased body fat, and increased bone density. However, it also carries potential risks, including the possibility of stimulating the growth of an occult prostate cancer. The benefits of androgen therapy outweigh the risks in men with classic hypogonadism. However, for men with mild hypogonadism or andropause, the balance between benefits and risks is not always clear. Unfortunately, studies to date have included too small a number of patients and have been too short in duration to provide meaningful data on the long-term risks versus the benefits of androgen replacement therapy in these populations. Several products are currently marketed for the treatment of male hypogonadism. Weekly-to-biweekly injections of testosterone cypionate (cipionate) or testosterone enanthate (enantate) are widely used, as they are economical and generally well tolerated. However, once-daily transdermal therapies have become increasingly popular and now include both patch and gel systems. Intramuscular injection of testosterone undecanoate is an attractive new therapy that can be administered quarterly. To confirm an adequate replacement dosage, assessment of clinical responses and measurement of serum testosterone levels generally suffice. For selected men, serial measurement of bone mineral density during androgen therapy might be helpful to confirm end-organ effects. For men aged >50 years, we advocate measurement of hematocrit for detection of polycythemia and a digital rectal examination with a serum prostate-specific antigen level measurement for prostate cancer screening during the first few months of androgen therapy. Subsequently, a hematocrit should be obtained yearly or after changes in therapy, and annual prostate cancer screening can be offered to the patient after a discussion of its risks and benefits.

Hormone Replacement Therapy↗
PubMed2001

[Pharmacotherapy for neuropathic pain caused by injury to the afferent nerve fibers].

Phantom pain, a form of neuropathic pain, is caused by damage to somatosensible afferent nerve fibres in the peripheral or central nervous system. Often, the pain cannot be satisfactorily treated with nonsteroidal anti-inflammatory drugs. Dependent on the underlying mechanism the pain is treated with either antidepressants (for more or less continuous pain) or anti-epileptics (for paroxysmal pain). Of the antidepressants, the tricyclic antidepressants are the best studied and most prescribed. The activity of new drugs, such as the selective serotonin reuptake inhibitor paroxetine as well as venlafaxine, has yet to be clearly shown. Of the anti-epileptics, carbamazepine and phenytoin are the most prescribed. New drugs which provide greater pain relief than the placebo are oxcarbazepine, gabapentine and lamotrigine. Other effective drugs for phantom pain are: gamma-butyric acid agonists (baclofen), opiates (morphine preparations with a regulated release; phentanyl patch), the N-methyl-D-aspartate receptor antagonist amantadine, transdermally administered clonidine and locally applied lidocaine.

Amantadine↗
PubMed1997

Subgroups of smokers with different success rates after use of transdermal nicotine.

To identify subgroups of smokers with different success rates, we applied "tree-structured survival analysis" (TSSA) to data from a previously published trial of transdermal nicotine. The subjects who received active treatment (14 mg patch, n = 275, or the 21 mg patch, n = 262) constituted the sample for this analysis. Using age, gender, the Fagerstrom Tolerance Questionnaire (FTQ), motivation to quit, number of cigarettes smoked at baseline, and body mass index (BMI) as classification variables, TSSA identified two subgroups within the 14 mg patch group and four subgroups of smokers within the 21 mg patch group. Among those receiving the 14 mg patch, individuals with a BMI greater than 26.4 kg/m2 relapsed sooner than did those with a BMI less than or equal to this value. Within the 21 mg patch group, the survival curve for males was significantly different from that observed in females, with males experiencing a longer time to relapse after treatment than did females. Among females, those with a higher motivation to quit relapsed more slowly than did those women with less motivation to quit. This information may be helpful to clinicians seeking to match specific patients to specific treatments with traditional nicotine in order to maximize treatment outcomes.

Administration, Cutaneous↗
PubMedDate not supplied

Initial evaluation of transdermal timolol: serum concentrations and beta-blockade.

The serum concentrations and beta-blockade after dermal application of timolol ointment were evaluated in six healthy men (21-31 years old; 74-82 kg). Two patches (25 cm2) containing placebo and either 30 (n = 2) or 60 mg (n = 4) timolol base were randomly applied to the chest for 30 h. Serial serum concentrations of timolol were measured by a radioligand receptor assay. Bicycle ergometry, at a predetermined workload, was performed before and at 3, 8, 24, and 48 h after patch application; mean +/- SD heart rates (beats/min) at these times were 167 +/- 2, 158 +/- 7, 125 +/- 7, 120 +/- 5, and 150 +/- 5 (last 3 values: p less than 0.05 from pretreatment), and beta-blockade was evident in all subjects. Measurable serum concentrations in the therapeutic range were achieved in all subjects. The change in exercise-induced heart rate (y) was closely related to log timolol serum concentration (x) (y = -36 X - 5.3; r = -0.92; p less than 0.001). Based on the amount of timolol in the residual ointment, 50-60% of the original timolol dosage was delivered from the patch. Skin irritation under the patch compared with placebo was minimal. Further studies are warranted to assess the potential clinical utility of transdermal timolol.

Adult↗
PubMed2001

Treatment options for a patient experiencing pruritic rash associated with transdermal testosterone: a review of the literature.

A 22-year-old man with hypogonadotropic hypogonadism was receiving monthly intramuscular injections of testosterone replacement therapy. The patient refused to self-administer the injections because of discomfort, so the therapy was switched to testosterone patches. He experienced a pruritic, macular, erythematous rash underneath the reservoir area of two different transdermal formulations, which did not improve after pretreatment with topical corticosteroids. Eventually, he tolerated application of a testosterone gel and his serum testosterone levels returned to normal after 1 month of therapy. Commercially available and investigational testosterone products and therapeutic monitoring guidelines for androgen replacement are reviewed.

Administration, Cutaneous↗
PubMed2005

Feasibility of transdermal delivery of fluoxetine.

Feasibility of developing a transdermal drug delivery of fluoxetine has been investigated. Permeation studies of fluoxetine across human cadaver skin were carried out using Franz diffusion cells. The receptor phase consisted of pH 7.4 phosphate buffer maintained at 37 degrees C. Permeation enhancement of fluoxetine, either in the salt or base form, was achieved using various enhancers like azone, SR-38, and ethanol. Various O/W microemulsion systems of fluoxetine were developed to study their effect on the skin permeation of fluoxetine. The results indicated that ethanol at 65% vol/vol was able to increase the permeation of fluoxetine the most, while microemulsion systems showed decrease in the permeation of fluoxetine. The permeation of fluoxetine obtained using a 65% vol/vol ethanolic solution was found to be sufficient to deliver the required dose (20-80 mg) from a patch of feasible size. The results seem promising for developing a transdermal drug delivery system of fluoxetine.

Administration, Cutaneous↗
PubMed1990

Transdermal scopolamine reduces nausea and vomiting after outpatient laparoscopy.

The authors evaluated the effect of transdermal scopolamine on the incidence of postoperative nausea, retching, and vomiting after outpatient laparoscopy in a double-blind, placebo-controlled study. A Band-Aid-like patch containing either scopolamine or placebo was placed behind the ear the night before surgery. Anesthesia was induced with fentanyl (0.5-2 micrograms/kg iv), thiopental (3-5 mg/kg iv), and succinylcholine (1-1.5 mg/kg iv) and maintained with isoflurane (0.2-2%) and nitrous oxide (60%) in oxygen. Scopolamine-treated patients had less nausea, retching, and vomiting compared with placebo-treated patients (P = 0.0029). Severe nausea and/or vomiting was present in 62% of the placebo group but only 37% of those getting the scopolamine patch. Repeated episodes of retching and vomiting were also less frequent in the scopolamine group compared with the placebo group (23% vs. 41%; P = 0.0213) as was the need for additional antiemetic therapy (13% vs. 32%; P = 0.0013). Patients in the scopolamine group were also discharged from the hospital sooner (4 +/- 1.3 vs. 4.5 +/- 1.5 h; P = 0.0487). Side effects were more frequent among those patients treated with the scopolamine patch (91% vs. 45%; P less than 0.05) but were not troublesome. The authors conclude that transdermal scopolamine is a safe and effective antiemetic for outpatients undergoing laparoscopy.

Administration, Cutaneous↗
PubMed1991

Effects of vehicle supplementation on total estradiol absorption from a transdermal estradiol delivery system.

OBJECTIVE: To evaluate the effects of vehicle supplementation on serum estradiol (E2) delivery pharmacokinetics from the Ciba-Geigy (Summit, NJ) 0.1-mg Estraderm Patch. DESIGN: Postmenopausal women were randomized to a 28-day crossover treatment protocol separated by a 14-day wash out period. SETTING: Normal human volunteers were studied in an academic research environment. PATIENTS, PARTICIPANTS: The subject pool included eight healthy postmenopausal women between 32 and 60 years of age. INTERVENTIONS: In treatment A, a 0.1-mg Estraderm Patch was worn for 7 days; in treatment B, and identical patch was worn into which 0.6 mL of ethanol was injected on day 3 of use. MAIN OUTCOME MEASURES: Serum E2 levels were measured in both groups. RESULTS: Although E2 absorption showed characteristic interpatient variability, addition of ethanol significantly extended the mean time for serum E2 levels to return to baseline, without increasing peak absorption. The mean extension was 50 hours. CONCLUSION: The addition of ethanol to the Estraderm Patch increased the duration of elevated serum E2 levels measured in menopausal women, thus potentially increasing the effective life span of the transdermal therapeutic system.

Absorption↗
PubMed1984

Transdermal administration of clonidine for treatment of high BP.

The effectiveness of transdermally administered clonidine hydrochloride was evaluated in a multicenter study in 85 patients with mild essential hypertension. The drug was incorporated into small self-adhesive delivery systems (pliable skin patches, 3.5-sq-cm area) designed to continuously deliver 0.1 mg of clonidine hydrochloride per day. These devices were changed by the patients themselves at weekly intervals. Diastolic BP fell by at least 10% in 37 patients and was normalized (less than 90 mm Hg) in 54 patients (64%); 17 of these responding patients required only one skin patch, 27 required two, and the other ten responders required three. The antihypertensive action of the transdermal clonidine was sustained for the full three months of study. Side effects were similar to those during conventional oral treatment, but appeared to be milder.

Age Factors↗
PubMed1984

Post-marketing surveillance of the Transiderm-Nitro patch in general practice.

Post-Marketing Surveillance (PMS) of Transiderm-Nitro, a new transdermal form of nitroglycerin, was undertaken during the 6 months following its introduction to general practitioners in the United Kingdom. Two thousand four hundred and seventy-five record forms were received. Excluding the fourteen patients who died during the surveillance, treatment in the remaining 2461 was judged as effective in 80.6% of patients and was well tolerated, with 70.5% having no unwanted effects. The incidences of withdrawal from Transiderm-Nitro in all patients analyzed were 5.7% due to headaches, 3.6% due to other unwanted effects and only 3.1% due to the treatment being judged as ineffective. This PMS confirms that Transiderm-Nitro is an effective, well tolerated addition to the therapy of angina pectoris.

Adult↗
PubMed1998

Importance of chronopharmacokinetics in design and evaluation of transdermal drug delivery systems.

Circadian and meal effects on nicotine kinetics determine in part blood nicotine concentrations and in doing so may influence cigarette smoking behavior throughout the day. We have shown previously that nicotine clearance varies by approximately 17% (from peak to through) due to diurnal factors throughout the day and that meals increase nicotine clearance by about 42%. Until now pharmacokinetic analyses of nicotine absorption from patches have assumed a constant clearance of nicotine over 24 hr. Using 11 individual kinetic estimates from a previous study, we analyzed plasma nicotine concentrations vs. time data of two nicotine patch studies, and conducted a set of simulations to determine the extent to which time-varying kinetics would influence the design of transdermal drug delivery systems, intented to maintain a constant plasma nicotine concentration over 24 hr. Not incorporating time-varying kinetics leads to biased estimates of the delivery rate of the nicotine patches, and increases the variability in the delivery rates estimates. The hypothetical transdermal drug delivery systems designed assuming constant nicotine clearance results in a systematical underdosing during the first 12 hr after beginning therapy. The transdermal drug delivery systems obtained assuming the correct time-varying clearance shows three components: 1) an early high delivery rate, followed by 2) a rather constant, but slightly decreasing at night, release rate and 3) transient increases in delivery rate for 2 hr after each meal. The effect of circadian variations in clearance could be compensated for in patch design by decreasing the delivery rate during the night. Transient variations in clearance due to meals would require the corresponding use of rapid drug delivery dosage forms. The methods we devise to predict optimal dosing regimens in presence of chronopharmacokinetics might be useful for other medications in which blood levels need to be precisely controlled.

Administration, Cutaneous↗
PubMed2002

A pilot controlled trial of transdermal nicotine in the treatment of attention deficit hyperactivity disorder.

OBJECTIVE: To test the hypothesis that transdermal nicotine would be efficacious for the treatment of children and adolescents with attention deficit hyperactivity disorder (ADHD). METHOD: This was a double-blind, placebo-controlled, randomized, pilot trial that compared the effects of daily transdermal nicotine (5 mg/16 hrs) to placebo in children and adolescents with ADHD. There was a three-day washout period of all psychotropic medication followed by a one-week treatment period. RESULTS: All 10 subjects enrolled (six males, four females; mean age = 10 years, SEM = 0.8) completed the study. As assessed by the 48-item Conners Parent Rating Scale at endpoint and during the trial, there was a significantly greater reduction in ADHD symptoms on "Learning Problems" and "Hyperactivity" subfactors. Nausea, stomach ache, itching under patch and dizziness were the most frequently reported adverse effects associated with transdermal nicotine. CONCLUSIONS: While the results of this study support previous research indicating that nicotinic receptor modulation may be a potentially useful strategy for the treatment of ADHD, therapeutic uses of nicotine are limited due to side effects. Thus, future research should investigate ways of improving the therapeutic index of nicotinic ligands in the treatment of ADHD, such as testing selective nicotinic antagonists alone or in combination with cholinergic agonists.

Administration, Cutaneous↗
PubMed2003

Dermal penetration of fentanyl: inter- and intraindividual variations.

Fentanyl is a potent synthetic opioid that is increasingly being used in transdermal drug delivery systems. The target organ concentration of a drug administered dermally will depend on the rate of dermal absorption and the systemic elimination. We have studied the intra- and interindividual variation in dermal penetration of fentanyl in an in vitro model (static diffusion cells) with human skin, and compared the absorption of fentanyl from an aqueous solution with absorption from a commercial patch. The intraindividual variation in dermal penetration of fentanyl in aqueous solution was limited (18%) and no differences in penetration characteristics were observed between breast and abdominal skin. The interindividual variation in dermal penetration of fentanyl was extensive, with maximal fluxes ranging from 21-105 ng/cm2/hr following application of an infinite dose of fentanyl to the donor chamber. Use of transdermal drug delivery systems (patches) reduced the inter-individual variation. The permeability coefficients after application of fentanyl in aqueous solution and through patches were identical (0.0011 cm/hr). One person had a higher than average penetration rate following patch application, which may indicate that the human skin and not the patch barrier was the rate-determining factor for the other individuals included in this study.

Administration, Cutaneous↗
PubMed1999

Double-blind, randomized, placebo-controlled clinical trial on the efficacy and tolerability of a physostigmine patch in patients with senile dementia of the Alzheimer type.

Owing to the pharmacokinetic properties of physostigmine when administered by conventional routes, long-term cholinergic treatment of Alzheimer's disease is difficult to manage. In order to overcome the problems associated with the oral and intravenous application of physostigmine, and to improve patients' compliance, a transdermal therapeutic system was developed. The efficacy and tolerability of this system were evaluated in a double-blind, randomized, multicenter study comparing patches containing 30 mg and 60 mg physostigmine with a placebo patch. The clinical trial followed the basic principles of the various guidelines on the evaluation of anti-dementia drugs, and included patients with mild to moderate probable Alzheimer's disease. A total of 204 patients with probable Alzheimer's disease were included in the study. Of these, 136 patients were eligible for the according-to-protocol analysis of efficacy, 167 subjects for the intention-to-treat analysis of efficacy, and 181 patients were included in the safety analysis. In contrast to the hypothesis to be tested, the efficacy of physostigmine was not superior to that of placebo after a treatment period of 24 weeks. On the contrary, there was even a slight, but not statistically significant, trend toward a better outcome in the placebo group. Median physostigmine plasma concentrations of approximately 100 pg/ml were measured, showing a high degree of interindividual variability and no linear dose relationship between the 30 mg and 60 mg dosages. Plasma cholinesterase activity was not significantly affected by physostigmine. The physostigmine patch application in doses of 30 mg and 60 mg apparently did not lead to physostigmine plasma concentrations that were sufficient to compensate for cholinergic deficiencies in affected brain areas and produce clinical benefits. Both the drug and the transdermal system were generally well tolerated under the study conditions. Modifications of the patch system may perhaps make it possible to achieve higher physostigmine plasma concentrations, which seem to be required to induce the expected beneficial effects during long-term treatment of Alzheimer's disease.

Administration, Cutaneous↗