PT-141 Peptide Nasal Spray
Share
PT-141, also known as Bremelanotide, is a synthetic peptide used primarily for the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women. It functions as a melanocortin receptor agonist, specifically targeting the MC4 receptor, which is implicated in sexual arousal pathways.
Intranasal delivery of peptides, including PT-141, offers several advantages over other routes of administration. The nasal route bypasses the gastrointestinal tract and first-pass metabolism, leading to improved bioavailability and rapid onset of action. This is particularly beneficial for peptides, which often suffer from poor oral bioavailability and degradation in the digestive system.[1]
The development of PT-141 nasal spray involves several key considerations. The peptide's molecular weight, solubility, and stability are critical factors influencing its formulation. PT-141 has a molecular weight of approximately 1025 Da, which is within the range suitable for nasal delivery.[1] The formulation must ensure adequate solubility to deliver therapeutic doses in the limited volume available for nasal sprays. Additionally, permeation enhancers and mucoadhesives can be incorporated to improve the bioavailability of PT-141 by enhancing its absorption through the nasal mucosa.[1]
Clinical studies have demonstrated the efficacy of PT-141 in treating HSDD. In a randomized, double-blind, placebo-controlled trial, PT-141 significantly improved sexual desire and reduced distress associated with low sexual desire in premenopausal women.[2] The onset of action is typically within 30 minutes to 2 hours, making it a convenient option for patients seeking rapid relief from symptoms.
The safety profile of PT-141 is generally favorable, with the most common adverse effects being transient nausea, flushing, and headache. These side effects are typically mild and resolve without intervention. The intranasal route minimizes systemic exposure, reducing the risk of systemic side effects.[2]
In summary, PT-141 peptide nasal spray represents a promising therapeutic option for HSDD, leveraging the advantages of intranasal delivery to enhance bioavailability and provide rapid onset of action. The formulation considerations, including molecular weight, solubility, and the use of permeation enhancers, are critical to its success. Clinical trials have confirmed its efficacy and safety, making it a valuable addition to the treatment landscape for sexual dysfunction.
1. Overview of Intranasally Delivered Peptides: Key Considerations for Pharmaceutical Development. Al Bakri W, Donovan MD, Cueto M, et al. Expert Opinion on Drug Delivery. 2018;15(10):991-1005. doi:10.1080/17425247.2018.1517742.
2.Intranasal Peptide Therapeutics: A Promising Avenue for Overcoming the Challenges of Traditional CNS Drug Development. Bose M, Farias Quipildor G, Ehrlich ME, Salton SR. Cells. 2022;11(22):3629. doi:10.3390/cells11223629.