Increased stability and controlled release of anticonvulsant drugs

Anticonvulsant drugs, such as Gabapentin and Pregabalin, are known to decompose rapidly in aqueous solution, precluding the delivery of these therapeutic agents as liquid doses. Researchers at the University of Oxford have developed a method to intercalate the drug molecules within a layered double hydroxide (LDH). The LDH-drug nanohybrids have been shown to possess increased stability and offer a more controlled release of the bioactive payload. This development will allow more facile administration of Gabapentin and Pregabalin to paediatric patients, and those who have difficulty swallowing tablets, such as geriatrics or individuals with limited muscle control.

Drug instability

Gabapentin and pregabalin are anticonvulsant drugs, which are widely used in the treatment of epilepsy and neuropathic pain. They have also found off-label uses in the prevention of migraines and treatment of social anxiety disorder. However, the poor stability of gabapentin and pregabalin in aqueous solution prevents administration of the drugs in a liquid form. As such, patients who require a liquid dose, including children, geriatrics and individuals with reduced muscle control, cannot be treated with these drugs.

Layered double hydroxides (LDHs) and drug delivery

Layered double hydroxides (LDHs) are ionic solids which comprise layers of hydroxide anions and metal cations with other small molecules, such as water, intercalated within this matrix. Their facile, inexpensive synthesis and biocompatibility, have led to LDHs being extensively studied for use in drug delivery and controlled release systems.

Drugs become 15x more stable

Oxford researchers have developed a methodology for the intercalation of gabapentin and pregabalin into a biocompatible LDH matrix. The process proves to be highly adaptable and can be altered to vary the drug loading. Tests have shown that the synthesis of these LDH-drug nanohybrids decreased the rate of decomposition of gabapentin under aqueous conditions by a factor of 15.

The main benefits of this approach include:

  • Inexpensive LDH synthesis
  • Controlled release of the bioactive payload
  • Facile variation of the drug loading
  • Order of magnitude increase in drug stability
  • Applications in pharmaceutical suspensions and wet formulation

Patent protection

Oxford University Innovation has filed a patent (WO2017/089804) covering this process and is interested in talking to prospective partners with the aim of commercialising the technology.

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