INVESTORS

EXECUTIVE SUMMARY

What is the idea?

A biocompatible intra-vaginal ring (IVR) composed of nanoporous elastomere hydrogel for the delivery of non-hormonal contraceptives and/or anti-HIV agents. The IVR will be an effective multipurpose prevention technology (MPT) for protection against both undesired pregnancy and sexually transmitted HIV infection.

Why this idea is an unconventional AND creative approach to contraception and HIV protection.

The novel IVR is a reliable and easy-to-use device that can prevent the harmful side effects of long-term hormonal contraceptive use. It can improve women’s lives by providing a better quality of maternal and fetal health, especially in regions where unsafe sex is the largest cause of disease in females. It is an innovative approach for family planning and protection against sexually transmitted infections that women can control themselves. The drugs and IVR are made of compounds that are already FDA approved for human use.

The scientific basis for our idea and why we expect it to succeed.

The IVR is made up of nanoporous elastomeres of hydrophilic polymeric hydrogel to provide sustained and effective delivery of drugs in the vagina over the period of a month or longer. The non-hormonal contraceptives incorporated are ferrous gluconate (loading dose: 0.8g/ring) to cause spermiostasis, ascorbic acid (loading dose: 0.7g/ring) to increase cervical mucus viscosity, and a natural buffer (loading dose: 0.5mL/ring) to stabilize the pH at 4 – 4.5 which is healthy for vaginal flora, but lethal to sperm and other microbes thereby preventing other vaginal infections, like Bacterial Vaginosis (BV). The amounts of these compounds used in the loading dose of the IVR are significantly lower than the US Pharamcopeia suggested toxic levels.

Mode of action:

Contraceptives

  1. Ferrous gluconate causes oxidative damage to the lipid bilayer of the sperm tail by promoting lipid peroxidation leading to spermiostasis. Any systemic absorption of ferrous gluconate may compensate for the loss of blood during menstruation in undernourished women;
  2. Ascorbic acid acts as a reducing agent for disulfide bonds of mucopolysaccharides of the cervical mucus resulting in conformational changes from the open cellular structure found in midcycle of the menstrual period to the closed structure resulting in viscous cervical mucus that acts as a barrier to inhibit sperm penetration;
  3. Mixture of polyamino-polycarboxylic acid (ampholines) and/or Poly L-Glutamic Acid (PLGA) sodium bicarbonate buffer sustain the vaginal pH at 4 – 4.5.

Methods and Materials:

On the basis of current data, spermiostasis, along with an increase in cervical mucus viscosity and sustained acidic pH, allows for this non-hormonal contraceptive system to be extremely likely to succeed in immobilizing sperm in less than a minute in the vaginal tract. Preliminary testing in vivo in rabbits attests to the success of inhibiting fertilization. The IVR may also be used to deliver anti-HIV microbicides, such as tenofovir (loading dose: 5mg/ring). Multiple microbicides act at different sites of the viral life cycle to be more effective at a lower dose and may minimize drug resistance. Tenofovir (PMPA) is a nucleotide analogue reverse-transcriptase inhibitor (NtRTI). Reverse transcriptase is an enzyme essential to all retroviruses for replication of its DNA in the host cell. PMPA acts as an analogue of deoxynucleotides, which is necessary for viral replication and causes premature termination of the RNA replication process.

Next steps

The next steps will include animal studies for toxicology, as well as, pharmacokinetic & pharmacodynamic studies of the non-hormonal contraceptive agents and microbicides. In addition, preparation and approval of an Investigational New Drug (IND), Investigational New Device (IDE), and Institutional Review Board (IRB) will be undertaken to initiate a Phase I clinical human trial.

Contact:

Sidney Lerner

Inventor/President

BioRings LLC

info@biorings.org