A nasal spray formulation delivers testosterone or its derivatives quickly into the bloodstream via the nasal route, using water, medium-chain triglycerides, and a PEGylated surfactant. This method efficiently treats hypogonadism, low libido, and anxiety disorders .
Testosterone is a crucial hormone in the human body, playing a significant role in various physiological processes, including the development of male reproductive tissues, muscle and bone mass maintenance, and the regulation of mood and libido. Despite its importance, testosterone administration poses challenges due to the hormone's poor oral bioavailability. Traditional delivery methods, such as intravenous, intramuscular, or transdermal routes, often lead to patient discomfort, risk of cross-contamination, and inconsistent hormone levels. These issues highlight the need for more effective and patient-friendly testosterone delivery systems, particularly for treating conditions like hypogonadism, decreased libido, and anxiety-related disorders.
Current testosterone delivery methods come with significant limitations. Intravenous and intramuscular injections can be painful and inconvenient, requiring frequent administration and medical supervision. Transdermal applications, such as gels or patches, provide a slower release of testosterone, often taking days to reach optimal levels, which can be inefficient for patients needing rapid symptom relief. Additionally, these methods carry the risk of secondary exposure to others through skin contact.
Nasal formulations have been explored as an alternative, offering rapid absorption and higher brain testosterone levels. However, existing nasal formulations often use castor oil, which can cause irritation and non-selective uptake through mucosal membranes. Aqueous formulations, while less irritating, typically result in lower testosterone concentrations, limiting their therapeutic efficacy. These challenges underscore the need for innovative approaches to testosterone delivery that combine rapid absorption with minimal side effects.
This technology involves a pharmaceutical composition for delivering testosterone or its derivatives via an aqueous nasal route. The formulation includes testosterone or a derivative, water, a lipid composition, and a nonionic surfactant. The lipid composition comprises triglycerides with medium-chain fatty acids, and the surfactant is a PEGylated triglyceride, often derived from castor oil. This composition enhances the solubility and absorption of testosterone, allowing it to quickly enter the bloodstream and reach the brain.
This rapid delivery is beneficial for treating conditions like hypogonadism, decreased libido, and anxiety-related disorders. Nasal administration achieves a peak testosterone concentration within about 30 minutes, followed by a decrease, minimizing side effects associated with prolonged high testosterone levels. The composition can be administered using a nasal inhaler, providing a non-invasive alternative to traditional testosterone delivery methods.
This technology is differentiated by its unique delivery method and formulation. Unlike traditional testosterone administration methods, such as intravenous, intramuscular, or transdermal, which can have drawbacks like repeated syringe use, cross-contamination, or inefficient absorption, this nasal route offers a rapid and efficient alternative. The aqueous formulation prevents cross-contamination and irritation often associated with castor oil-based formulations.
Additionally, the rapid peak and subsequent decline in testosterone levels reduce the risk of side effects linked to sustained high levels, offering a safer and more effective treatment option. The use of a PEGylated triglyceride surfactant enhances the solubility and bioavailability of testosterone, ensuring a quick and targeted delivery to the brain, which is crucial for addressing anxiety and fear-related disorders. This innovative approach provides an improved therapeutic option for patients with testosterone deficiencies or related conditions.
https://patents.google.com/patent/US20220387447A1/en?oq=+US-2022-0387447-A1+