Lexaria Files New Patent Application for Enhancement of Delivery of Lipophilic Agents Across the Blood-Brain Barrier and Methods for Treating Central Nervous System Disorders Kelowna, British Columbia

Lexaria Files New Patent Application for Enhancement of

Delivery of Lipophilic Agents

Across the Blood-Brain Barrier and

Methods for Treating Central Nervous System Disorders

Kelowna, British Columbia June 29, 2018 Lexaria Bioscience

Corp. (OTCQX: LXRP) (CSE: LXX) (the Company or Lexaria ) a drug delivery

platform innovator, announces it has filed an important new patent application

with the United States Patent and Trademark Office ( USPTO ) for innovation in

treatment options related to central nervous system disease or disorders

including viral infection, cancer, neurodegenerative disorders, ADHD, anxiety,

depression, OCD, schizophrenia, Alzheimer s, Huntington s, Parkinson s,

neuropathic pain and more.

In recent laboratory testing, Lexaria s breakthrough discovery

evidenced greatly enhanced drug delivery to brain tissue. Nicotine

in-vivo (animal) studies showed that up to 560% more nicotine was

delivered to brain tissue utilizing DehydraTECHTM than

concentration-matched controls lacking DehydraTECHTM enhancements.

The study provided evidence of surprising effectiveness in crossing the

blood-brain barrier ( BBB ) which the Company is investigating more extensively,

leading to Lexaria s patent application titled: Enhancement of Delivery of

Lipophilic Active Agents Across the Blood-Brain Barrier and Methods for Treating

Central Nervous System Disorders.

It is well documented that nicotine while addictive does

not cause cancer. It is the tar and other chemicals formed when cigarettes are

combusted that cause cancer. Thus, an efficient delivery mechanism of minute

quantities of nicotine that does not require combustion could lead to greatly

reduced death and disease through the avoidance of smoking, while also

potentially aiding reduced chemical dependence on nicotine until such time as

addictive-avoidance behaviours can be empowered.

Lexaria s surprising discovery of the DehydraTECHTM

apparent effectiveness in crossing the BBB also opens the door to possibilities

of delivering other therapeutic drugs in the treatment of intractable diseases.

The BBB, while providing effective protection to the brain

against circulating toxins, also creates major difficulties in the

pharmacological treatment of brain diseases. Most charged molecules, and most

molecules over 700 Daltons in size, are unable to pass through the barrier, and

smaller molecules may be conjugated in the liver. These factors create major

difficulties in the pharmacological treatment of diseases of the brain and

central nervous system ( CNS ), such as Alzheimer's disease, Parkinson's

disease, bacterial and viral infections and cancer.

Many therapeutic agents for the treatment of diseases and

disorders of the brain and CNS are sufficiently hydrophilic to preclude direct

transport across the BBB. Furthermore, these drugs and agents are susceptible to

degradation in the blood and peripheral tissues that increase the dose necessary

to achieve a therapeutically effective serum concentration. However, as

described above, although lipophilicity is generally associated with molecules

that are easily able to cross the blood-brain barrier, lipophilicity is not the leading characteristic

for molecules that transverse the blood-brain barrier. Seelig and colleagues

studied the association of different factors with the ability of molecules to

diffuse across the blood-brain barrier, including lipophilicity, Gibbs

Adsorption Isotherm, a Co CMC Plot, and the surface area of the drug to water

and air (Seelig et al. (1994) Proc. Nat. Acad. Sci. (USA) 91:68-72).

Their results showed that barrier permittivity is based on a complex interaction

between relative size and the surface activity of the molecule, in which the

surface activity includes the molecular properties of both hydrophobic and

charged residues (Seelig et al. (1994) Proc. Nat. Acad. Sci. (USA) 91:68-72).

Prior methods for delivering drugs across the BBB involve three

general categories: (1) liposome-based methods, where the therapeutic agent is

encapsulated within the carrier; (2) synthetic polymer-based methods, where

particles are created using synthetic polymers to achieve precisely-defined size

characteristics; and (3) direct conjugation of a carrier to a drug, where the

therapeutic agent is covalently bound to a carrier such as insulin. Liposomes

are attractive for transporting drugs across the BBB because of their large

carrying capacity. However, liposomes are generally too large to effectively

cross the BBB, are inherently unstable, and their constituent lipids are

gradually lost by absorption by lipid-binding proteins in the plasma. Synthetic

polymers have run into difficulties having the drug carried across the cell only

to be trapped in an endothelial cell or a lysosome, instead of the desired

result of being ejected into the brain parenchyma.

Direct conjugation of pharmacological agents with the

substances that can be transported across the BBB, such as insulin, has also

been attempted. Insulin and insulin-like growth factors are known to cross the

blood brain barrier by specialized facilitated diffusion systems. (Reinhardt et

al. (1994) Endocrinology 135(5): 1753-1761). Specific transporters also exist

for glucose and for large amino acids such as tryptophan. However, the

specificity of the insulin transporter has proved to be too high to allow

pharmacological agents covalently linked to insulin to cross into the brain.

Similar results have been obtained with glucose and amino acid conjugates, whose

uptake has been observed to obey the same general principles as other

low-molecular weight substances, with only uncharged molecules below 700 Da

achieving significant access to the brain.

Lexaria s application requests patent protection for the

delivery of cannabinoids, terpenes and terpenoids, non-steroidal

anti-inflammatory drugs (i.e., NSAIDs), vitamins, nicotine, phosphodiesterase

type 5 (PDE5) inhibitors, estrogen, progestin, testosterone, scopolamine and

more, utilizing Lexaria s already-patented DehydraTECHTM methodology

combined with any of a wide variety of emulsifiers, starches, oils, flavorings

With approximately 50 patents now granted or pending worldwide,

the Company s policy has evolved to continue to issue news releases on material

patent filings and issuances, but not on every patent-related development.

Lexaria Bioscience Corp. has developed

and out-licenses its disruptive delivery technology that promotes healthier

ingestion methods, lower overall dosing and higher effectiveness of lipophilic

active molecules. Lexaria has multiple patents pending in over 40 countries

around the world and has patents granted in the USA and in Australia for utilization

of its DehydraTECHTM delivery technology. Lexaria s technology

provides increases in intestinal absorption rates; more rapid delivery to the

bloodstream; and important taste-masking benefits, for orally administered

bioactive molecules including cannabinoids, vitamins, non-steroidal

anti-inflammatory drugs (NSAIDs), nicotine and other molecules.