A growing body of evidence supports the use of medical cannabis as a substitute and adjunct to prescription opiates in the treatment of chronic pain. Learn how cannabis can be effective treatment to pain.Read More
We are pleased to announce that we have signed a Letter of Intent dated December 22, 2016, with Corazon Gold Corp. (TSX VENTURE: CGW) for 100% acquisition of NanoSphere’s issued and outstanding shares.
The LOI contemplates a three-way amalgamation, pursuant to which NanoSphere will become a wholly-owned subsidiary of Corazon, in which Corazon will change its name to NanoSphere Health Sciences, Inc. Upon completion of the transaction, Corazon will also complete a financing of up to C$9,000,000 and NanoSphere will receive 56% ownership.
“This compelling transaction will delivery significant and immediate value to our company and will provide new opportunities for NanoSphere as part of a larger, more diversified company,” said David Sutton, President and Chief Operating Officer of NanoSphere Health Sciences. "This will bring NanoSphere and Corazon’s strengths together to accelerate innovation in this space. We look forward to working together to bring our patent-pending NanoSphere Delivery System™ to consumers worldwide."
The timing of the announcement also coincides with the launch of NanoSphere’s new cannabis-based line of products called Evolve. Evolve’s cannabinoid products are uniquely designed to be administered intra-orally, intra-nasally and transdermally in precision, dose-metered dispensers. The convenient-to-use liquid NanoGels bypass the GI tract and avoid 1st pass liver metabolism. NanoSphere’s dynamic membrane structure efficiently transports cannabinoids into the circulatory system and across the cell membranes to bind endocannabinoid and synergistic receptors.
NanoSphere Health Sciences plans on launching its patent-pending products this spring in Colorado for the recreational and medical cannabis markets with advanced intra-oral and transdermal formulas.
Cannabinoids are NOT User Friendly
Within the cannabis plant there are at least 480 distinct compounds. Among those at least 111 have been identified as phytocannabinoids and another 111 have been identified as terpenes. The principal cannabinoids appear to be delta-9-tetrahydrocannabinol (Δ9-THC) cannabinol (CBN), and cannabidiol (CBD). Working together they produce “Entourage Effects.” Their relative concentrations depends on a number of factors such as the cannabis strain plant genetics, the soil climate conditions, the cultivation techniques and most important the extraction technology for producing cannabis extracts.
Cannabinoids are nearly insoluble in water. Their poor solubility and low dissolution rate in the aqueous gastrointestinal fluids and significant first-pass liver metabolism result in low and unpredictable oral cannabinoid bioavailability Consequentially, cannabinoids require high doses to reach therapeutic plasma concentrations, especially when ingested.
Owing to their lipophilicity, cannabinoids accumulate in the lipid part of cell membranes and occupy binding sites localized on hydrophobic portions of integral membrane proteins. It is thought that various adverse effects associated with chronic use of cannabis, including increased tolerance over time, result from the interaction of cannabinoids with cell membranes. Furthermore, cannabinoids exhibit a slow clearance from the body.
Limitations of Current Methods of Use
The current methods of taking cannabis and cannabinoid products include:
- Inhalation delivery methods of smoking, vaporization and aerosols.
- Oral ingestion methods into the GI tract of infused products, edibles, extract oils, tinctures, soft gel caps, drinks, tablets, lozenges and gum.
- Intra-oral delivery methods via sprays tinctures, extracts, and emulsion compositions, and cannabis-containing chewing gums.
Each of these delivery methods has numerous problems and limitations.
Inhalation Delivery Methods of smoking and vaporization have no reliable dosage as medicine. Bioavailability following the smoking route was reported as 2−56%, due in part to intra- and inter-subject variability in smoking dynamics, which contributes to uncertainty in dose delivery. Bioavailability varies according to depth of inhalation, duration and breathhold. About 30% of the Δ9-THC present in a cigarette is destroyed by pyrolysis. Additional, THC is lost in the cigarette buttside-stream smoke, and incomplete lung absorption in the lungs. Inhaling the smoke of burning cannabis can irritate the lungs.
Oral Delivery Methods of ingesting extracts, infusions, edibles cannabinoid capsules have a delay in the onset of their actions making it extremely difficult to ingest the correct dosage of cannabinoids. Oral absorption of Δ9-THC is slow and unpredictable, with peak blood concentrations occurring 1–5 hours post dose. Psychotropic effects after oral use have been shown to set in after 30–90 minutes, peak between 2 to 4 hours, and decline to low levels after 6 hours.
Initial degradation of Δ9-THC is caused by digestive acids in the stomach and intestine. Extensive first-pass liver metabolism further reduces oral bioavailability of THC before it reaches the sites of action. The oral absorption of THC and CBD are typically reported as 6% bioavailability (4-12%) to the systemic circulation.
The hydroxylation of ingested Δ9-THC in the liver to 11-hydroxy-THC creates significantly higher levels of this metabolite compared with inhalation that produces stronger psychotropic effects and greater tendency for adverse effects without warning.
Intra-oral delivery methods of cannabinoids to the sublingual or buccal oral mucosa delivery in the forms of oral mucosal sprays (like Sativex), tinctures, aerosols, drops, lollipops and chewable are an ineffective delivery system for transporting cannabinoids through the oral mucosa. The physiology of epithelium lining and oral mucosa poses a formidable barrier that prevents cannabinoids from penetrating the mucosa and entering systemic circulation to produce any noticeable effects.
These products fail at intra-oral delivery for a number of reasons:
- The native cannabinoid molecular structure has poor permeability across the oral mucosa
- Their cannabinoid molecules are too large in size and weight to pass through mucosal layers into the systemic circulation.
- They deliver too high a fluid volume to diffuse across the approximately 100cm2 of surface area of oral mucosa into the systemic circulation. Effective dosages are measured in microliters not millimeters.
- They have unfavorable oil-to-water partition coefficients and lipophilcity (fat-solubility) of uniozable compounds for sublingual absorption.
- Salivary washout causes the cannabis to be swallowed.
A continual flow of saliva causes premature swallowing of the cannabinoids to pass from the mouth down your throat and are metabolized the same as ingesting an edible. They do not produce significant pharmacokinetic differences from orally ingested cannabis products.
Proof of this is found in the product monograph of the oral mucosal spray cannabis product Sativex by GW Pharma. Maximum plasma concentrations of both CBD and THC are quoted as typically occurring within 2 to 4 hours, like eating edibles. Sativex’s Δ9-THC forms the same blood profile of 11-hydroxy-THC from first pass liver metabolism as expected from being swallowed.
Viscoelastic NanoGels …The Delivery Solution
NanoSphere encapsulated cannabinoids are manufactured as stable viscoelastic nanoparticle gels that we refer as NanoGels. Patent-pending NanoGel Cannabinoids are a major advancement in delivery technology.
- NanoGel Cannabinoids, are proven effective as carriers for sublingual, buccal, intranasal, oral and transdermal delivery. Their fluidity, adhesive and viscoelastic properties effectively transport cannabinoids across cell mucosal membranes into the blood stream, past the blood brain barrier, binding to receptors and signal transduction.
- As a delivery platform, NanoGel Cannabinoids effective cannabinoid loading and allows administering NanoCanoids™ in precision-metered dosages through intra-nasal, intra-oral, perusal and transdermal routes of administration.
- NanoGel Cannabinoids can enter the bloodstream within 15 minutes and achieve peak blood concentrations within 60 minutes.
- NanoGel Cannabinoids can increase the bioavailability bioactivity of cannabinoids 2-fold to 8-fold compared to bioavailability without NanoSphere encapsulation.
- NanoGel Cannabinoids can decrease the dose of cannabinoids 2-fold to 8-fold less than an amount of cannabinoids needed to produce the same effect compared to non-encapsulated cannabinoids.
- Lipid based NanoGel Cannabinoids are highly-stable, biocompatible, biodegradable and easily produced by versatile and scalable and replicable patent-pending unified sequential assembly process.
DENVER – May 26, 2016 – NanoSphere Health Sciences, LLC, innovative developers of the industry-first, patent-pending NanoSphere Delivery System™, announced today positive pharmacokinetics (PK) and pharmacodynamics (PD) results for its nano-encapsulated THC intra-oral formula.
NanoSphere Health Sciences is the world’s first and only patent-pending nanoparticle delivery system for medical and recreational cannabis. Concentrated “NanoSpheres” deliver standardized profiles of whole plant cannabis extracts, purified cannabinoids and terpenes in convenient, microliter dosages with increased bioavailability, bioactivity and therapeutic potential. At the same time, the natural phospholipid spheres of nanoparticles decrease the adverse effects of cannabis. This is a major advancement in cannabis delivery technology.
“The PK data confirmed that our NanoSphere Delivery System has significant advantages over edibles and smoking in general. The nano-encapsulated THC is rapidly delivered into circulation in less than 10 minutes after administration,” said David Sutton, Chief Operating Officer of NanoSphere Health Sciences. "The data also supports our expectations that our product is rapidly absorbed through buccal and sublingual mucosa by intra-oral administration. We look forward to continuing our research and evaluations of our nano-encapsulated THC products in the months to come."
Highlights from the study:
- Measurable THC blood concentrations within 10 minutes.
- Peak THC blood levels that were 141%, 130%, 289% greater than 5mg oral, 5.4 mg Sativex® Spray and 5mg Namisol ® sublingual THC.
- Peak THC blood levels in 60 minutes, occurring 3.5x faster than oral ingested THC and Sativex® Spray .
- Significantly longer THC circulating half-life.
- High Peak THC levels and Low 11-OH-THC formation demonstrated NanoGel THC is absorbed into the blood stream sub-mucosally.
- Onset of pharmacodynamic effects under 10 minutes.
- Rapid cannabinoid distribution to the brain, peripheral tissues and receptors.
“Intra-oral delivered nanoparticle encapsulation of THC (NanoGel THC) demonstrated advantageous pharmacokinetic and pharmacodynamic characteristics that were significantly different from inhaling and ingesting cannabis and cannabinoid extracts. This represents a new delivery dose form of cannabis-based medicines that show advantages that signify therapeutic importance. Our NanoGel cannabinoids are the next generation and future of cannabis products,” said Dr. Richard Clark Kaufman, Chief Science Officer of NanoSphere Health Sciences.
“Among the main disadvantages of currently available THC methods of use are dosing difﬁculties due to unpredictable absorption and poor pharmacokinetic characteristics. NanoGel THC is a novel viscoelastic gel nanoparticle encapsulation of THC formulated for intraoral delivery, which improves THC absorption, distribution bioavailability and bioactivity. NanoGel THC establishes a high concentration gradient across the oral mucosa by intracellular and intercellular routes, favoring THC diffusion into the underlying tissue and absorption into the bloodstream,” said Dr. Kaufman.
NanoSphere’s cannabinoid products are uniquely designed to be administered intra-orally, intra-nasally and transdermally in precision dose-metered dispensers. The convenient-to-use liquid NanoGels bypass the GI tract and avoid 1st pass liver metabolism. The NanoSphere’s dynamic membrane structure efficiently transports cannabinoids into the circulatory system and across the cell membranes to bind endocannabinoid and synergistic receptors.
NanoSphere Health Sciences plans on launching its patent-pending products this summer in the U.S. and Canada for the recreational and medical cannabis markets with advanced, intra-oral and intra-nasal and transdermal formulas.
Typical oral mucosal sprays, tinctures, aerosols and drops lack an effective delivery system for transporting cannabinoids through the oral mucosa. Learn how they could be more readily-absorbed with our NanoSphere Delivery System.Read More
We are announcing that today the U.S. Patent and Trademark office issued “Patent Pending” status for our new cannabis NanoSphere technology platform.
We are the first and only patent-pending nanoparticle delivery system for medical and recreational cannabis. Concentrated “NanoSpheres” deliver plant extracts of cannabis and purified cannabinoids in convenient, standardized dosages to increase bioavailability, bioactivity and therapeutic potential. At the same time, the natural phospholipid particles decrease the adverse effects of cannabis.
While significant advancements and investments have been made in the medical cannabis industry, we are the first to apply nanotechnology to improve the bioavailability and efficacy of cannabis extracts and standardized dosages. This disruptive technology introduces a significant advancement in the medical and recreational cannabis markets, and meets the regulatory demands for product purity, uniformity and the reporting of active cannabinoid levels.
The NanoSphere Delivery System revolutionizes how cannabis delivers its benefits. Liquid NanoSpheres nanosize, encapsulate and rapidly deliver concentrated plant extracts and cannabis, purified cannabinoids, with increased bioavailability, bioactivity and therapeutic potential in standardized dosages printed on the product labels. At the same time, the biocompatible, phospholipid nanoparticles spheres (less than 70 nm in diameter) help decrease the adverse effects of cannabinoids.
NanoSphere’s cannabinoid products are uniquely designed to be administered intra-orally, intra-nasally and transdermally in precision dose-metered dispensers. The convenient-to-use liquid NanoGels bypass the GI tract and avoid 1st pass liver metabolism. The NanoSphere’s dynamic membrane structure of purified essential phospholipids efficiently transports cannabinoids into the circulatory system and across the cell membranes to bind endocannabinoid and synergistic receptors.
Our patent-pending NanoSphere phospholipid nanoparticle encapsulation of cannabinoids provides practical solutions for cannabinoid therapy with benefits of:
Standardized Dose-Metered Dosages
Higher Concentration of Bioactive Cannabinoids
Increased Bioavailability of Cannabinoids (2-fold to 8-fold)
Decreased Dosages (2-fold to 8-fold)
Decreased Adverse Effects
Decreased Tolerance to Cannabis from Prolonged Use
More Efficacious Cannabinoid Therapy and Medical Cannabis Treatments
Improved Cannabinoid-to-Receptor Binding and Signal Transduction
Enhanced Therapeutic Value
Ideal for Long-Term and Daily Use
Our business model integrates into the regulatory and product manufacturing chain-of-possession. NanoSphere is partnering with cannabis growers, extractors, product manufacturers and dispensaries in providing this revolutionary product. The NanoSphere Delivery System satisfies the regulatory requirements for quality control, standardized cannabis dosages, full disclosure labeling and complete transparency.
There is a new tech wave. And it's small. Real small. About a billionth of a meter small.
Nanotechnology is firmly positioning itself as the next tech revolution. Microscopic computer chips, operating in flexible units, are being developed to complement existing infrastructure, be it digital, physical, or biological. That's right — microscopic particles, working together in complex networks, could help heal, or even augment, the human body. They could allow nerves to bypass spinal injuries, heal damaged tissue at the microscopic level, override detrimental brain signals and dramatically increase bioavailability and bioactivity.
Nanotechnology offers the ability to truly change the human condition. By augmenting and changing existing systems and infrastructure nanoparticles will be able to target the bloodstream and cells.
How do we do this at NanoSphere Health?
Over the last decade, the researchers at NanoSphere Health Sciences have developed a patent-pending “NanoSphere Delivery System” that can produce desirable exposure of nutraceuticals and medications for optimal effects. The NanoSphere Delivery System can overcome many of the absorption problems of traditional pills and capsules.
Our NanoSphere Gel encapsulates ingredients in an all natural nano-sized protective membrane carrier. Made from the same phospholipids that form the membranes around the cells in the human body, NanoSpheres help shield ingredients from dilution and degradation. They are more efficiently transported into the circulatory system and target cells. These carriers help prevent early destruction and elimination of ingredients in the gut, by the liver, and immune system to increase bioavailability and extend their circulation time.
By using Nanotechnology, NanoSphere Health offers the ability to achieve better health rapidly and more effectively.
We are proud to announce that the U.S. Patent and Trademark office issued “Patent Pending” status for its new NSAID NanoSphere technology platform.
We are the first to encapsulate prescription and over-the-counter (OTC) NSAIDs (non-steroidal anti-inflammatory drugs such as (Ibuprofen, Aspirin, Naproxen, etc.) as a method to treat and prevent inflammatory disorders and global inflammation and pain. The use of the NanoSphere delivery technology eliminates and alleviates many of the severe side effects NSAIDs can have, such as stomach irritation, stomach bleeding and GI bleeding, among others. At the same time, it increases the therapeutic activity of NSAIDs for safe, long-term and more effective therapy.
NanoSphere NSAIDs are uniquely designed to be administered intraorally, intranasally and transdermally. The convenient liquid nanogels bypass the GI tract avoiding gastrointestinal irritation. When taken perorally, NanoSphere NSAIDs’ structure of purified essential phospholipids maintains the protective GI tract mucosa barrier from damage by NSAIDs. The NanoSphere NSAIDs are then efficiently transported into the circulatory system for greater therapeutic activity in safely treating inflammatory conditions and relieving pain.
“We are excited to announce that NanoSphere’s NSAID technology platform has achieved a ‘Patent Pending’ status, protecting the intellectual property of our NanoSphere delivery system within NSAIDs,” said Dr. Richard Kaufman, Chief Science Officer at NanoSphere Health Sciences. “Our disruptive NanoSphere delivery biotechnology introduces a significant advancement in the therapeutic potential and safety of OTC and prescription NSAIDs along with a tremendous growth potential.”
NSAIDs cause a range of gastrointestinal problems from mild upset stomach to serious conditions such as stomach bleeding, ulcers and kidney damage, factors which often limit their use. Among patients using NSAIDs, 30-40% have some degree of GI intolerance. NSAIDs physically damage the protective GI mucosa surface and promote bleeding. Furthermore, NSAIDs are fat-soluble drugs with low solubility and dissolution in water. This makes OTC and prescription NSAID pills hard to absorb and contributes to their causing GI problems.
“The problems with current NSAID therapy is glaringly apparent,” says Terry Grossman M.D., Medical Director at NanoSphere Health Sciences. “NSAIDs have low bioavailability and limited delivery into inflamed areas. They produce adverse effects, compounded with the fact that nearly half the population has difficulties swallowing currently sold NSAID pills and capsules.”
Our patent-pending phospholipid nanoparticle encapsulation of NSAIDs technology provides the following potential benefits:
- Higher Concentration of NSAIDs
- Increased Bioavailability of NSAIDs (2-fold to 10-fold)
- Decreased Dosage of NSAIDS (2-fold to 10-fold)
- Enables Safe, Long-Term Use and More Efficacious NSAID Therapy and Treatment
- Reduced Risk of Gastrointestinal Problems
- Transport into and Targeting of Specific Body Sites
- Delivery into the Central Nervous System
- Enhanced Therapeutic Value
- Ideal for Long-Term and Daily Use
NanoSphere Health expects availability of commercial licensing by the second quarter of 2015, after clinical trials have been completed.