Nano therapy Spotlight: Arestin™ Minocycline Microspheres

Abstract

Within the last ten years, recent advancements in nanotechnology and repurposed pharmaceutical development has led several successful therapeutics through clinical trials and subsequently onto the market. On the nanotechnology side, size, shape, charge, and formulation are all considered in improving the overall efficacy or delivery of the therapeutic. Nanoparticle therapies hit the market in the late 90’s when the FDA approved CosmoFer®, an iron sugar colloid that also saw use in the European market. While these early nano pharmaceuticals were primitive compared to today’s standards, these medications proved that a nanoparticulate therapeutic can and would be accepted by the FDA, albeit under much scrutiny. On the pharmaceutical side, older legend drugs that have been proved efficacious for many years are beginning to be repurposed for other uses. For example, Pfizer’s 2015 approval of Rapamune® (Rapamycin) is indicated for the treatment of Lymphangioleiomyomatosis (LAM) a rare lung disease infecting mostly women in early adulthood. The drug, however, was first approved in 1999 and was used in the prophylaxis of organ rejection as an immunosuppressant. Another indication for Rapamycin is in age related diseases; a 2006 paper published by Dr. Blagosklonny at the Roswell Park Comprehensive Cancer center showed that Rapamycin could inhibit certain pathways that are related to aging. Many other medications on the market such as monoclonal antibody therapies have also seen a rise in new implication discovery and there is much evidence to suggest other drugs will be researched in the future for other alternative treatments. Because of such developments, pharmaceutical companies have tapped into the nanoparticle development world to find novel therapies for diseases we once thought were unavoidable. This is shown by the sheer expected market growth of about two billion dollars from 2021-2026, and the fifteen different nanoparticle-based therapeutics that have already been FDA approved since in just the last three years. Although the nanoparticle technology scope may seem to hover over novel cancer therapies, autoimmune disorders, blood borne diseases and neurological disorders, many therapies have come about in some interesting fields of study. One such therapeutic is called Arestin®, a new dentistry medication for the treatment of severe periodontitis, better known as gum disease. Gum disease is caused by poor oral hygiene and is attributed to various bacterial infections within the gum-line and if left untreated it can cause soft tissue damage or jawbone degradation. Typically, an antibiotic mouthwash or ultrasonic dental cleaner can be used to treat minor periodontitis but, in severe cases where there is significant gum-line recession, a more direct therapeutic is needed to treat the infection directly at the source. Arestin® is a nanoparticle formulation containing minocycline HCl impregnated within a bio-reabsorable polymer that is delivered directly into the gum-line via a blunt tip syringe. Minocycline is a tried-and-true antibiotic with a rich history of over thirty years on the market as a second-generation tetracycline derivative. It is both a gram positive and gram negative [broad spectrum] antibiotic and is very well tolerated in patients making it an excellent candidate in late-stage gum disease intervention. Here, this review, discuss Arestin® and subsequently Minocycline Hydrochloride’s: history, mechanism of action, formulation/production, side effects and the future of reformulated nano pharmaceuticals that are continuing to move the market share up.