Simvastatin In-Situ Gel

Thermoresponsive nanoscale intranasal delivery system for enhancing direct nose-to-brain drug delivery

This technology is an intranasal gel spray that uses nanoscale simvastatin particles and mucoadhesive, thermoresponsive gel to improve brain drug delivery, increase nasal retention, and bypass first-pass metabolism for better treatment of neurological disorders.

Background

Central nervous system (CNS) disorders present significant treatment challenges, requiring targeted therapeutic interventions. Certain pharmaceutical agents, like simvastatin, possess potent neuroprotective and anticonvulsant properties that make them highly desirable for treating neurological conditions. To effectively utilize these therapeutics, there is a critical need for noninvasive delivery methods capable of transporting drugs directly to the brain. Intranasal administration has emerged as a promising route to achieve this goal. By offering a direct nose-to-brain conduit, this pathway successfully bypasses the restrictive blood-brain barrier, presenting a vital opportunity to enhance the efficacy of neurological treatments.

Despite this potential, current delivery approaches face severe limitations that hinder clinical success. A primary obstacle is the poor water solubility of these drugs, coupled with extensive first-pass metabolism that severely restricts their bioavailability. Furthermore, when administered via conventional nasal suspensions, these therapeutics suffer from inadequate uniformity and poor mucosal interaction. The most critical barrier is the natural mucociliary clearance mechanism within the nasal cavity. This physiological process rapidly sweeps away standard liquid formulations before adequate absorption occurs, drastically reducing the drug's residence time. Consequently, traditional formulations fail to maintain the localized concentration required for optimal CNS targeting.

Technology Description

This advanced intranasal delivery system administers central nervous system therapeutics, specifically simvastatin, directly to the brain. The platform integrates a nanoscale drug dispersion mechanism that significantly enhances medication solubility and uniformity. A core feature is its in-situ gelling, thermoresponsive matrix. At room temperature, the formulation remains a sprayable liquid, but upon reaching the nasal cavity's temperature of 34°C, it rapidly transitions into a gel within 60 seconds. Additionally, the system incorporates mucoadhesive properties to counteract natural mucociliary clearance. It is engineered to produce a specific spray plume geometry targeting the upper turbinate region, facilitating optimal nose-to-brain transport.

This technology is highly differentiated by its ability to overcome traditional barriers of neurological drug delivery, specifically poor water solubility and extensive first-pass metabolism. By bypassing the blood-brain barrier, it provides a highly efficient, noninvasive route for neuroprotective treatments. Unlike conventional liquid suspensions that are quickly washed away, this platform’s mucoadhesive gel ensures prolonged mucosal interaction and sustained release. Furthermore, the nanoscale dispersion achieves superior deposition and uniformity compared to standard formulations, maximizing overall bioavailability. This rationally engineered approach makes it a distinct, highly effective solution for treating complex neurological disorders.

Benefits

  • Enables direct, noninvasive nose-to-brain drug delivery, effectively bypassing the blood-brain barrier and first-pass metabolism to improve bioavailability.
  • Enhances the solubility and uniformity of poorly water-soluble drugs (like simvastatin) through advanced nanoscale dispersion.
  • Prolongs drug residence time and counteracts rapid mucociliary clearance using specialized mucoadhesive properties.
  • Improves ease of administration and retention with a thermoresponsive matrix that sprays easily as a liquid at room temperature and rapidly gels at body temperature.
  • Maximizes central nervous system (CNS) delivery efficiency by utilizing a specific spray plume geometry that precisely targets the upper turbinate region of the nasal cavity.
  • Facilitates sustained drug release and superior interaction with the nasal mucosa, offering a highly effective platform for treating neurological disorders.

Commercial Applications

  • Nose-to-brain drug delivery
  • Neurological disorder treatment
  • Poorly soluble drug administration
  • Noninvasive anticonvulsant therapy delivery
  • Neuroprotective medication delivery

Opportunity

This patent is available for exclusive licensing.

This intranasal platform employs a nanoscale simvastatin dispersion within a thermoresponsive, mucoadhesive matrix. It transitions from liquid to gel at 34°C within 60 seconds, enhancing residence time against mucociliary clearance. The system's specific spray geometry targets the upper turbinate, facilitating direct nose-to-brain delivery. By bypassing first-pass metabolism and improving drug solubility, this technology optimizes the delivery of neuroprotective agents to the central nervous system.

Provisional patent 64/030,796 filed 04/06/26

 

Patent Information: