Nanoencapsulated delta-9-tetrahydrocannabinol
Inventors
Castor, Trevor Percival • Purdum, Geoffrey
Assignees
Publication Number
US-8629177-B2
Publication Date
2014-01-14
Expiration Date
2031-08-23
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Abstract
Embodiments of the present invention are directed to articles of manufacture and methods of making such articles having utility for the delivery of cannabinoids as a therapeutic. One embodiment of the present invention directed to the article of manufacture comprises a lyophilized particle or sphere having a diameter of about 100 to 500 nanometers having a shell and comprising a biodegradable polymer containing a cannabinoid. A featured cannabinoid is delta-9-tetrahydrocannabinol (delta-9-THC).
Core Innovation
The invention relates to articles of manufacture and methods for making lyophilized particles or spheres with diameters of about 100 to 500 nanometers, each with a shell comprising a biodegradable polymer and containing a cannabinoid, specifically delta-9-tetrahydrocannabinol (delta-9-THC). These nanospheres are produced using biodegradable polymers such as poly(D,L-lactide-coglycolide polymer) and polycaprolactone, with defined ratios of lactide to glycolide, and involve lyophilization following formation in a specially composed buffer.
The background of the invention highlights that cannabinoids like delta-9-THC have therapeutic potential for a range of chronic diseases but have not been effectively utilized due to challenges in stable formulation and societal or legal constraints. In particular, the instability and ready degradation of cannabinoids have severely limited viable administration routes. There exists a need for compositions and processes that protect cannabinoids, improve their stability, and deliver them effectively as therapeutics.
The solution provided by the present invention is a process and article wherein delta-9-THC is encapsulated within nanospheres of biodegradable polymer. The process employs supercritical, critical, or near-critical carbon dioxide as a solvent medium for mixing the cannabinoid with the polymer, which is then formed into spheres in a deareated, cross-linking buffer and lyophilized to stabilize the final nanospheres. The nanoparticles can be included in various dosage forms for therapeutic delivery, and buffer components such as sugars, alcohols, and polyvinyl alcohol are utilized to optimize encapsulation and stability.
Claims Coverage
There is one independent claim which defines the main inventive feature of the patent.
Method for making lyophilized nanospheres containing delta-9-tetrahydrocannabinol with biodegradable polymer shells
A method comprising: 1. Forming a mixture of poly(D,L-lactide-coglycolide polymer) or polycaprolactone containing delta-9-tetrahydrocannabinol in carbon dioxide under supercritical, critical, or near critical conditions. 2. Injecting the mixture as a stream into a deareated solution comprising a cross-linking agent in a buffer to form one or more particles or spheres with diameters of 100 to 500 nanometers. 3. Lyophilizing the resulting particles or spheres to produce a lyophilized particle or sphere with a shell comprising the biodegradable polymer containing delta-9-tetrahydrocannabinol. Notable features include the use of a supercritical, critical, or near critical fluid for encapsulation, the use of biodegradable polymers, and the defined nanoscale particle size.
The claimed inventive feature covers a specific method for creating lyophilized, nanoscale particles or spheres containing delta-9-tetrahydrocannabinol encapsulated within a biodegradable polymer using supercritical, critical, or near critical carbon dioxide, and special buffer conditions for stability.
Stated Advantages
Nanoencapsulation significantly improves the stability of delta-9-tetrahydrocannabinol, especially during storage at 4°C.
The articles of manufacture are stable and bioavailable.
The encapsulation environment limits exposure to oxygen and other reactants that degrade the cannabinoid.
Pegylation of PLGA in the polymeric system can increase biological half-life, improve stability and water solubility, and optimize immunologic characteristics.
The process produces nanoparticles that can remain stable in acidic gastric environments, allowing oral delivery.
Documented Applications
Therapeutic delivery of cannabinoids, specifically delta-9-tetrahydrocannabinol, for chronic diseases such as cancer pain, AIDS wasting, emesis, cachexia, obesity, smoking cessation, schizophrenia, multiple sclerosis, and Parkinson's disease.
Inclusion in dosage forms such as inhalers, capsules, gel caps, tablets, pills, powders, suspensions, implants, and transdermal patches.
Oral delivery via compressed tablets or suspensions in biocompatible solvents.
Encapsulation into softgel or hard capsules using liquid suspensions of the nanospheres to enhance oral bioavailability and prevent aggregation.
Interested in licensing this patent?