Juniper Pharmaceuticals, Inc., announced the publication of promising results from a Phase I proof-of-concept study exploring the potentials of its proprietary intravaginal ring (IVR) to deliver large molecules, including peptides and proteins, to treat diseases that afflict women.
The study, “A novel approach to administration of peptides in women: Systemic absorption of a GnRH agonist via transvaginal ring delivery system,” published in the Journal of Controlled Release, investigated the ability of IVR to deliver the nine amino acid peptide leuprolide, a gonadotropin-releasing hormone agonist (GnRHa) that is commercially available as an injection (Eligard and Lupron) for the treatment of precocious puberty, infertility, and endometriosis, among others diseases.
“Therapies based on peptides are notoriously difficult to deliver and typically cannot be taken orally,” Alexa B. Kimball, M.D., MPH, from Massachusetts General Hospital and Harvard Medical School, and the study’s principal investigator, said in a press release. “This study demonstrates the potential of a new delivery route for peptide therapeutics for women. To further explore transvaginal absorption capabilities, future studies will need to examine larger molecules and the administration of these molecules for longer periods of time and in larger numbers of women.”
This Phase I trial enrolled six healthy volunteers, who received 18 or 36 mg of leuprolide via Juniper’s ethylene vinyl acetate intravaginal ring drug delivery system. Consistent with the leuprolide’s biologic activity, serum levels increased within eight hours of insertion and were dose dependent. GnRHa biological activity was verified by secretion of gonadotropins and sex steroids. Results also showed that the vaginal pathway allows for rapid absorption of a biologically active peptide, and has the potential for a transvaginal drug delivery system to deliver not only peptides but other macromolecules, such as proteins, CRISPR therapeutics, mRNA, or monoclonal antibodies, as well.
Peptides cannot be given orally because the stomach’s activity breaks them down before they can be absorbed. The skin is a more attractive way to deliver medications, but its intrinsic barrier function often makes the route untenable, especially for larger peptides and proteins, and can affect compliance in some patients, since transdermal patches need to be switched more than once a week. The vaginal epithelium is not keratinized, which facilitates the absorption of other molecules. Juniper’s IVR technology can hold one to two orders of magnitude more drug than transdermal patches, expanding the number and types of drugs that can be delivered this way, as well as duration of use from a single dose.
“A self-administered vaginal ring provides patients with a simplified drug delivery system and should improve compliance and therefore treatment effectiveness,” said Bridget A. Martell, Juniper’s chief medical officer.
Juniper claims that its IVR, because of its unique polymer composition and segmentation capability, is the only single ring that allows for dosing of small and large molecular weights of multiple drugs at multiple release rates and dosages, including lipophilic and lipophobic molecules. This capacity opens the system to the possibility of offering other therapeutics.
The company plans to file an Investigational New Drug application for JNP-0101, its oxybutynin IVR candidate to treat overactive bladder in women, later in 2016.