Identification of penetration enhancers for testosterone transdermal delivery from spray formulations

Leichtnam, Marie-Laure; Rolland, Hervé; Wüthrich, Patrick; Guy, Richard H.

doi:10.1016/j.jconrel.2006.03.008

Cited by 30 publications

(19 citation statements)

References 17 publications

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“…The excess deposited drug on the surface of skin is hypothesized to maintain drug saturation levels in the SC [5,26,27,32]. A recent study focused on the development of a testosterone TSS, showed that plasma testosterone concentrations increased promptly after TSS application and peaked within the first 2 h followed by a gradual decrease [5]. In a similar study where fentanyl was deposited on skin from a volatile solvent, the amount of drug in skin and that remaining on skin surface were quantified.…”

Section: Drug Depot In Skinmentioning

confidence: 99%

“…While there are numerous conditions effectively treated with transdermal products, including angina, hypertension, smoking cessation, motion sickness and hormone deficiency, the number of drugs incorporated in transdermals are limited. In the past three decades, numerous approaches have emerged to enhance transdermal drug delivery (TDD) [3,[5][6][7][8][9][10][11][12][13][14]. Despite the scientific dedication to expand the portfolio of transdermally delivered drugs [8,9,15,16], the number of commercially available transdermal products is limited [3,17,18].…”

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confidence: 99%

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Spray-on transdermal drug delivery systems

Ibrahim

2014

Expert Opinion on Drug Delivery

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TSS is easily applied, delivering flexible drug dosage and associated with lower incidence of skin irritation. TSS provides a fast-drying product where the volatile solvent enables uniform drug distribution with minimal vehicle deposition on skin. TSS ensures precise dose administration that is aesthetically appealing and eliminates concerns of residual drug associated with transdermal patches. Furthermore, it provides a better alternative to traditional transdermal products due to ease of product development and manufacturing.

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Section: Drug Depot In Skinmentioning

confidence: 99%

mentioning

confidence: 99%

Spray-on transdermal drug delivery systems

Ibrahim

2014

Expert Opinion on Drug Delivery

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“…Comparing the pharmacokinetics of this spray (T 50 mg per dose) with those of T gel 50 mg, the serum T concentrations in the first 12 h following administration were found to be bioequivalent to the T gel. Another group is also working on the development of T transdermal sprays [147,148].…”

Section: Other Novel Approaches For Transdermal Testosterone Deliverymentioning

confidence: 99%

Therapeutic Potential of Testosterone Gels

Lunenfeld

Oettel

2009

Aging Health

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Aging Health (2009) 5(2), 227-245 of male primary hypogonadism is due to testicular failure, with Klinefelter's syndrome accounting for the majority of cases. Abnormalities at the testicular level result in hypergonadotropic hypogonadism (primary hypogonadism) and at the hypothalamic-pituitary level result in hypogonadotropic hypogonadism (secondary h ypogonadism) (Figure 1).In addition, it has been clearly demonstrated that aging is associated with a decline in both total T and free T levels, with a 20 and 35% incidence of hypogonadism in men aged 60 years and in those over 80 years of age, respectively [2,9]. This decline in T is the result of a combination of a primary steroidogenic defect in the aging Leydig cells [10], decreased pituitary secretory capacity and responsiveness to gonadotropin-releasing hormone [11]. This type of testicular deficiency has been termed late-onset hypogonadism (LOH). Aging is also asso ciated with an increase in sex hormone-binding globulin levels and, consequently, with a slower decline in total T than in free T [12]. The normal diurnal rhythm of T secretion observed in young men is partially lost with aging [13]. Aging is also associated with a decrease in lean body mass, muscle mass and strength, diminished libido, erectile function, decreased bone mass, increased fracture risk and diminished sleep quality -symptoms similar to those observed in hypogonadism, which may need treatment with T. Per definition, male hypogonadism is a clinical syndrome characterized by a reduction in circulating androgens and the presence of signs and symptoms of androgen deficiency. The existence of clinical symptoms is In demographic terms, the global population is estimated to grow from the current 6.5 billion to approximately 9 billion by the year 2050. However, owing to the worldwide prolongation of the mean life expectancy and the drastic reduction of fertility rate, it is projected that the elderly (>60 years) will double during the same period from 688-1964 million [1].Approximately 30% of men aged 60-70 years and 70% of men aged 70-80 years have low bioavailable or free testosterone (T) levels [2]. Symptoms and findings of T deficiency are more or less similar to those associated with aging. They include loss of energy, depressed mood, decreased libido, erectile dysfunction, decreased muscle mass and strength, increased fat mass, frailty, osteopenia and osteoporosis [3]. Clinical trials indicate that T therapy can improve many of these findings [4][5][6][7][8].Testosterone is the principal androgen in men, as well as the prohormone for the biosynthesis of two other sexual steroids: 5α-dihydrotestosterone (DHT) and 17β-estradiol. In human males, T 6-7 mg is secreted by the testes in a circadian rhythm with a nocturnal rise in T followed by a decline during the day. T is necessary for spermatogenesis, penile function, to induce and maintain secondary sexual characteristics, lean muscle mass, bone density and for normal sexual behavior and cognitive function.The administration of T is appropri...

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“…4 Furthermore, their physicochemical properties make them exceptional candidates in the therapeutic field as they can easily diffuse through the human skin, notably because of their low molecular weight and adequate lipophilicity.…”

Section: Introductionmentioning

confidence: 99%

“…However, emulsions have attracted increasing attention over the recent years as they not only mimic clinical performance of a patch but also lower the incidence of skin irritation, thus enhancing the patients' compliance. 4 As their application assumes the physiological hormonal environment, emulsions are able to exploit this advantage and reduce the side effects and risks associated with hormone therapy. 5 Despite the numerous advances, transdermal semisolid pharmaceuticals pose a few specific challenges, e.g., to reach systemic circulation in sufficient quantity to exert their biological activities, the pharmaceuticals have to applied over a large surface area.…”

Section: Introductionmentioning

confidence: 99%

TRANSDERMAL FORMULATIONS CONTAINING HUMAN SEXUAL STEROIDS: DEVELOPMENT AND VALIDATION OF METHODS ANDIN VITRODRUG RELEASE

et al. 2014

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In vitro release of bioidentical hormones in four different liposomal transdermal emulsions (containing testosterone, progesterone, estradiol, or estradiol and estriol) was assessed. For this purpose, novel high-performance liquid chromatography methods were developed and validated in an eco-friendly manner and used to determine the in vitro release of such products. The methods were suitable for our intended goal, and the emulsions employed were found to be effective as transporting candidates for the efficient release of hormones in the transdermal delivery of human sexual steroids.

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Identification of penetration enhancers for testosterone transdermal delivery from spray formulations

Cited by 30 publications

References 17 publications

Spray-on transdermal drug delivery systems

Spray-on transdermal drug delivery systems

Therapeutic Potential of Testosterone Gels

TRANSDERMAL FORMULATIONS CONTAINING HUMAN SEXUAL STEROIDS: DEVELOPMENT AND VALIDATION OF METHODS ANDIN VITRODRUG RELEASE

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