By Nanomerics
Drug Delivery · Ocular & CNS Biocompatible polymer nanoparticles that package hydrophobic drugs and deliver them across epithelial barriers — to the front and back of the eye, and to the CNS via the oral or nasal route. Non-irritant, aqueous, and engineered for patient compliance. - 5–10× enhanced ocular penetration - Phase I complete — primary endpoints met - Compatible with small molecules & peptides An award-winning Active Excipient platform that engineers biocompatible polymer nanoparticles to dramatically increase the amount of drug available at the disease site. Phase I ✓ Primary Endpoints Met — SUNLIGHT Trial · OC134 · March 2025 5–10× Enhanced Ocular Penetration vs Conventional Eye Drops Non-irritant — Pain-free Aqueous Formulation — No Burning or Stinging Not Your Usual Nanoparticle: A polymer matrix — not a micelle with a hydrophobic core. MET is a synthetically controlled polymer that self-assembles into sub‑100 nm nanoparticles. Unlike conventional micelles — which form a core‑shell structure with a hydrophobic interior — MET creates a matrix architecture through non‑covalent cross‑linking of multiple amphiphilic groups on a single polymer chain. This matters because in a micelle the hydrophobic core is an ideal environment for the drug — there is no thermodynamic incentive for the API to leave. The result: poor release and limited tissue penetration. In the MET matrix, drugs sit in dynamic binding pockets — a ‘Goldilocks’ environment that accommodates hydrophobic compounds readily, but only while the pockets exist. When the positively charged particle binds to a negatively charged cell surface, electrostatic forces exceed the forces maintaining the binding pockets. The pockets collapse, and the drug is released at high local concentration directly at the cell membrane — driving tissue penetration rather than trapping the API indefinitely. MET Matrix: Dynamic binding pockets. Drug released on cell contact. Conventional Micelle: Hydrophobic core sequesters drug. No release trigger. Stability Means Safety: Multiple amphiphilic groups in one molecule create extremely stable self‑assemblies with ultra‑low CMC — orders of magnitude more stable and safer than other self‑assembling systems. 10 GCPQ chains forming an intertwined matrix · 200 ns MD Why ‘Molecular Envelope’: Polymer chains change conformation to maximise drug binding — enveloping individual API molecules throughout the matrix. Unlike surface adsorption or passive entrapment, MET polymers actively adapt their conformation around each drug molecule. Intra‑ and inter‑polymer binding pockets form dynamically, accommodating hydrophobic compounds through induced‑fit interactions — enabling up to 50% drug loading compared to 1–10% with conventional technologies. All-Atom Molecular Dynamics — Drug Enveloped by Polymer Matrix: Curcumin (orange) progressively enveloped by GCPQ polymer chains (translucent surface). Multiple chains contribute to the dynamic binding pocket. Initial contact 110 ns: 65% Surface buried, 90 Contacts, 6 Chains involved. Multi-chain wrapping 121 ns: 77% Surface buried, 123 Contacts, 5 Chains involved. Pocket forming 137 ns: 81% Surface buried, 117 Contacts, 6 Chains involved. Envelope closing 171 ns: 85% Surface buried, 117 Contacts, 6 Chains involved. Fully enveloped 192 ns: 86% Surface buried, 121 Contacts, 6 Chains involved. System 10× GCPQ + 11 curcumin. Simulation 200 ns · OPLS_2005. Atoms 311,960. Contact cutoff 0.6 nm (heavy atoms). Mechanism of Action: MET nanoparticles envelope drug molecules and release them at the cell surface via charge-triggered conformational change. 01 Self-Assembly: Individual MET polymer chains spontaneously self-assemble into stable matrix nanoparticles at ultra-low critical micellar concentration (CMC~20 μM) — orders of magnitude more stable than conventional self-assembling systems. CMC 20 μM (~0.2–0.4 mg/mL). Size 100–500 nm (drug-loaded). 02 Drug Loading: Polymer chains change conformation to form dynamic binding pockets that envelope individual drug molecules throughout the matrix — enabling up to 50% drug loading vs 1–10% with conventional technologies. Loading Up to 50% w/w. Mechanism Induced binding pockets. 03 Aqueous Transport: Cationic nanoparticles carry a high drug payload in a water-like aqueous formulation. Low dynamic viscosity (<5 mPa·s) preserves visual acuity with no burning or stinging. Charge Permanent cationic (+). Viscosity <5 mPa·s (water-like). 04 Cell Binding & Conformational Change: Electrostatic forces at the cell surface exceed the dynamic pocket-forming forces. Polymer chains flatten against the membrane, losing the ability to envelope drug molecules. Trigger Electrostatic (+/−) binding. Effect Pocket collapse & drug release. 05 Drug Release & Tissue Penetration: Released drug creates a high local concentration at the cell membrane, facilitating partitioning into cells and sustained tissue retention without systemic exposure. Enhancement 5–18× ocular delivery. Systemic No detectable exposure. Comparative Efficiency: Head‑to‑head comparison of ocular delivery technologies using published CsA data. The rabbit eye is the recognised preclinical model for human ocular pharmacokinetics — drug concentrations in the rabbit are predictive of human eye concentrations, allowing direct comparison of eye drop technologies. Using cyclosporine A (CsA) — the drug for which comparable published data exist across all major platforms — MET penetration enhancement dramatically outperforms competing technologies. ▶ 2–3× more drug to cornea than Santen’s cationic emulsion ▶ 4–10× more drug to cornea than Restasis (Allergan) ▶ 7–11× more drug to conjunctiva than NOVA22007 or Restasis C max (ng/g per μg dosed) · Rabbit model · Published data Engineered Supramolecular Self-assembly: Biocompatible polymers are tailored to form nano-scaled containers that package hydrophobic drugs in aqueous media. The highly dynamic encapsulation allows efficient drug loading and rapid release at the target barrier. Ocular & CNS Delivery: MET delivers drugs to the front and back of the eye via non-irritant aqueous eye drops, and to the brain via the nose-to-brain route — bypassing barriers that defeat conventional formulations. Broad Platform Applicability: Compatible with low molecular weight hydrophobic drugs and peptides across ophthalmic, nose-to-brain CNS, oral, and subcutaneous routes.
