Vasoactive Intestinal Peptide for the treatment of Female Sexual Arousal Disorder

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DESCRIPTION (provided by applicant): Female sexual arousal disorder (FSAD), one of the conditions commonly described as Female sexual dysfunction (FSD) is common among older women and can be a significant reason for decreased quality of life in the aging population. FSAD is defined as the persistent or recurring inability to attain or maintain sufficient sexual excitement, causing personal distress. Disorders of arousal often include insufficient vaginal lubrication, decreased clitoral and labial sensation, decreased clitoral and labial engorgement and/or lack of vaginal smooth muscle relaxation. Often, physiological causes like previous pelvic trauma, pelvic surgery, decreased vaginal or clitoral blood flow (e.g. due to cardiovascular problems) or the side effects of certain medications, for example selective serotonin reuptake inhibitors, play an important role in the etiology of the condition. Vasoactive intestinal peptide s an important neurotransmitter in the female genitalia with smooth muscle relaxant and other pleiotropic functions. It has been shown that it can increase blood flow in female genitalia and also induce vaginal lubrication. These features make it a possible treatment for FSAD. However, given systemically it can lead to a dangerous drop in arterial blood pressure. Theses safety concerns and the pharmacokinetics profile of the free peptide require it being formulated in a way to overcome these problems before it can be used as human therapeutic. PharmaIN Corp. has succeeded in preliminary experiments with the development of an injectable, polymer-based VIP formulation called PGC-VIP. This formulation has been shown to be safe and biologically active in a model of an inflammatory disease. Additionally, it exhibits a massive increase in in-vivo half-life. This application proposes to test a topical PGC-VIP formulation for efficacy in a rat model of FSAD and to test shelf-stability of this formulation. During the Phase I of the project sufficient material to conduct the efficacy experiment as described in aim 2 of the proposal will be synthesized in aim 1. Before the start of aim 2, this material will be submitted t QC to ensure that it is of identical composition and properties as the PGC-VIP formulation used in the preliminary experiments. Aim 2 will test the efficacy of the formulation in a rat model of FSAD and in aim 3 we will conduct a stability study.