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Optimization of a nanoparticle-based topical PDE5i formulation for treatment of erectile dysfunction

Award Information
Agency: Department of Health and Human Services
Branch: National Institutes of Health
Contract: 1R41DK129147-01A1
Agency Tracking Number: R41DK129147
Amount: $263,446.00
Phase: Phase I
Program: STTR
Solicitation Topic Code: 400
Solicitation Number: PA21-262
Timeline
Solicitation Year: 2021
Award Year: 2022
Award Start Date (Proposal Award Date): 2022-09-15
Award End Date (Contract End Date): 2023-08-31
Small Business Information
111 E MCBEE AVE
Greenville, SC 29601-4824
United States
DUNS: 080999429
HUBZone Owned: No
Woman Owned: No
Socially and Economically Disadvantaged: No
Principal Investigator
 ANDREW DRAGANSKI
 (908) 420-4814
 adraganski@zylotherapeutics.com
Business Contact
 SCOTT PANCOAST
Phone: (908) 420-4814
Email: spancoast@zylotherapeutics.com
Research Institution
 ALBERT EINSTEIN COLLEGE OF MEDICINE, INC
 
1300 MORRIS PARK AVE
BRONX, NY 10461-1975
United States

 Domestic Nonprofit Research Organization
Abstract

Abstract
It is increasingly recognized that erectile dysfunction (ED) not only affects a man’s sex life but also impacts his
relationships and overall psychological well-being. An indication of the importance of erectile function to men is
that, in the first 6 years after FDA approval of Viagra® (sildenafil, an oral treatment for ED), 23 million men
worldwide filled Viagra® prescriptions, with average annual sales of about $1.7 billion, making it one of the more
commercially successful drugs of all time. Sildenafil is a member of the phosphodiesterase-type-5 inhibitors
(PDE5i) drug class, which is by far the most commonly prescribed treatment for ED. However, because of side
effects, use restrictions (dietary, contraindications), and long time-to-response, a significant percentage of men
with ED either discontinue use of PDE5i within the first year or never begin treatment in the first place.
Several of the drawbacks associated with an oral/systemic route of administration could potentially be overcome
by a local, topical delivery vehicle. However, an aqueous sildenafil citrate solution has not been shown to
transdermally penetrate with any significance, as the physicochemical characteristics of these amphoteric drugs
make formulation and permeation challenging. With this in mind, our group initiated studies to determine if a
proprietary silica particle delivery system developed at Albert Einstein College of Medicine and licensed to Zylö
Therapeutics Inc. could act as an effective topical delivery system for PDE5i. Initial studies utilizing first-
generation technology demonstrated the feasibility of this approach using nano-sized particles in treating ED in
animal models of aging. Since then, a second-generation delivery system has been developed by Zylö for topical
delivery of other payloads such as lidocaine and cannabidiol (CBD). The goal of this proposal is to adapt this
second-generation technology to sildenafil and optimize it for clinical and commercial translation with the overall
hypothesis that topical delivery of sildenafil through the use of a nanoparticle delivery system (sildenafil-NP) can
improve erectile function.
The proposal will be conducted over the course of one year and will incorporate two specific aims. In Specific
Aim 1, Zylö will generate an optimized prototype formulation of sildenafil-NP. This will include modulations to the
chemical formulation of the nanoparticles such that a significant increase in the carrying capacity for PDE5i will
be realized. In Specific Aim 2, proof-of-principle experiments will be conducted to assess the efficacy of topical
application of these second-generation sildenafil-NP in eliciting an erectile response in an animal model of ED
resulting from aging.
At the conclusion of these proposed Phase I studies, we will have identified a lead sildenafil-NP formulation that
is optimized for clinical translation as a topical treatment of ED.Narrative
Sildenafil is a member of the phosphodiesterase-type-5 inhibitors (PDE5i) drug class, which is by far the most
commonly prescribed treatment for erectile dysfunction (ED). However, because of side effects, use restrictions
(dietary, contraindications), and long time-to-response, a significant percentage of men with ED either
discontinue use of PDE5i within the first year or never begin treatment in the first place. In these proposed Phase
I studies, Zylö Therapeutics will optimize for clinical translation a nanoparticle delivery system that would facilitate
local topical application of the leading PDE5i (sildenafil), which has the potential to overcome several of the
drawbacks associated with an oral/systemic route of PDE5i administration.

* Information listed above is at the time of submission. *

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