Impact of Antinucleants on Transdermal Delivery ofTestosterone from a Spray

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

doi:10.1002/jps.20670

Cited by 20 publications

(16 citation statements)

References 22 publications

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“…New diffusion medium is added at the same time, replacing aliquots that are taken to maintain sink conditions. 31,32,34,41,68,81,115 This compartment system can be seen in Figure 5. In addition to the methods previously mentioned, the fluorescence method is also useful in observing the extent to which the drug penetrates the skin layer.…”

Section: In Vitro Drug Penetration/release Studymentioning

confidence: 98%

“…88 However, after being measured, the level of methylphenidate penetration was greater with the Eudragit RS film compared to Eudragit E. 80 In addition, films with Eudragit L100 have been reported to be unable to prevent the crystallisation of testosterone. 68 Eudragit RS 100 has been reported to have good sprayability, adhesiveness, and flexibility. However, use above a concentration of 15% can reduce the ability to wash with water, whereas Eudragit RLPO produces better films at a level of 10.05% in a mixture with ethyl cellulose 5.02 %.…”

Section: Eudragitmentioning

confidence: 99%

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<p>Film-Forming Sprays for Topical Drug Delivery</p>

Umar¹,

Butarbutar²,

Sriwidodo³

et al. 2020

DDDT

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Film-forming sprays offer many advantages compared to conventional topical preparations because they can provide uniform drug distribution and dose, increased bioavailability, lower incidence of irritation, continuous drug release, and accelerated wound healing through moisture control. Film-forming sprays consist of polymers and excipients that improve the characteristics of preparations and enhance the stability of active substances. Each type of polymer and excipient will produce films with different features. Therefore, the various types of polymers and excipients and their evaluation standards need to be examined for the development of a more optimal form of film-forming spray. The selected literature included research on polymers as film-forming matrices and the application of these sprays for medical purposes or for potential medical use. This article discusses the types and concentrations of polymers and excipients, sprayer types, evaluations, and critical parameters in determining the sprayability and film characteristics. The review concludes that both natural and synthetic polymers that have in situ film or viscoelastic properties can be used to optimise topical drug delivery.

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Section: In Vitro Drug Penetration/release Studymentioning

confidence: 98%

Section: Eudragitmentioning

confidence: 99%

<p>Film-Forming Sprays for Topical Drug Delivery</p>

Umar¹,

Butarbutar²,

Sriwidodo³

et al. 2020

DDDT

View full text Add to dashboard Cite

show abstract

“…This application protocol may not be easy for fluid systems in clinical practice. Alternatively, fluid systems are better employed by an open application protocol through the formulation of spray [12]. The open application is always associated with evaporation of the volatile components of the microemulsion, resulting in phase transition, which may create systems with varying thermodynamic activity and may lead to supersaturation, an effect which requires investigation.…”

Section: Introductionmentioning

confidence: 99%

Occlusive and Non-Occlusive Application of Microemulsion for Transdermal Delivery of Progesterone: Mechanistic Studies

Maghraby

2012

Sci. Pharm.

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This work evaluated the occlusive versus non-occlusive application of microemulsion (ME) for the transdermal delivery of progesterone. The mechanisms of enhanced skin penetration were investigated. ME comprised of oleic acid, Tween 80, propylene glycol, and water, was used neat or with ethanol as a volatile cosurfactant. The ME formulations enhanced progesterone transdermal flux compared to the saturated drug solution in 14% aqueous propylene glycol (control). Ethanol-containing ME (EME) was better than the ethanol-free system (EFME). Open application of EFME produced a marginal reduction in flux compared to occlusive application. For EME, open application reduced the flux by 26–28% with the flux remaining significantly higher than that obtained with EFME. The mechanistic studies revealed synergism between ethanol and EFME with EME, producing greater flux than the sum of fluxes obtained from 40% ethanol in water and EFME. Penetration enhancement and supersaturation played a role in enhanced transdermal delivery, but other mechanisms were also possible. This study thus introduced EME as a transdermal delivery system for progesterone with good potential for open application as a spray.

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“…Polymer microparticles or fused crystalline T implants are being developed [149,150]. The goal was to explore whether the incorporation of antinucleant polymers into a T spray formulation could stabilize a putative supersaturated state and improve the delivery of the drug across the skin.…”

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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Impact of Antinucleants on Transdermal Delivery ofTestosterone from a Spray

Cited by 20 publications

References 22 publications

<p>Film-Forming Sprays for Topical Drug Delivery</p>

<p>Film-Forming Sprays for Topical Drug Delivery</p>

Occlusive and Non-Occlusive Application of Microemulsion for Transdermal Delivery of Progesterone: Mechanistic Studies

Therapeutic Potential of Testosterone Gels

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