Method for Enhancing Passenger Molecule Loading

a passenger molecule and loading technology, applied in the field of surfactants, can solve the problems of only stable aqueous-diluted nano-lipid formulations, reduced overall stability and usability of preparations, logistical difficulties in the preparation and use of uniform materials for study or administration, etc., to achieve enhanced loading of passenger molecules, reduce precipitation of passenger molecules, and increase the encapsulation concentration of passenger molecules

Pending Publication Date: 2020-06-18
NUVESSL INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent text describes a method to encapsulate cannabinoid compounds in phospholipid structures using surfactants, which allows for a higher concentration of cannabinoids to be encapsulated. The encapsulates can be used for oral, transmucosal, or transdermal administration and can be diluted without the cannabinoid precipitating from the preparation. The technical effect of this method is the ability to stably encapsulate cannabinoid compounds in phospholipid structures, resulting in improved absorption and reduced separation of the cannabinoid from the preparation.

Problems solved by technology

Active components have been sequestered in phospholipid particles using prior art methods and compositions, but these known prior art methods and compositions fail to retain all types of active components, especially at higher concentrations, in a solubilized state for extended periods of time, which decreases the overall stability and usability of the preparations.
Moreover, these Fountain prior art references rely on aqueous-diluted formulations using an aqueous phase to close the particles with the passenger molecules encapsulated within the particles, which is believed to contribute to the precipitation problem for certain lipophilic passengers.
So, it has been found that for certain lipophilic passenger molecules, such aqueous-diluted nano-lipid formulations are only stable for up to three days using the prior art methods and compositions.
This precipitation necessitates preparation of materials at the point of use and in small batch quantities over the course of multiple days, presenting logistical difficulties in the preparation and use of uniform materials for study or administration.
And, formulations prepared at point of use are totally inadequate for large-scale use, which prevents a wider use of these lipophilic passengers in lipid particles.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

ive Solubilized CBD in the Cannabinoid Encapsulate

[0072]

Product Name: 100 mg / g CBD ConcentrateBatch Size 150.00Phase / DZ #IngredientINCI Name%Wt.A DZ 4130Phospholipid StockAlcohol, Lecithin, Water14.0021.00A DZ 2330EthanolAlcohol56.0084.00A DZ 4730CannabidiolCannabidiol10.0015.00A DZ 4800PEG-40 HydrogenatedPEG-40 Hydrogenated20.0030.00Castor OilCastor Oil100.00150.00StepsProcedure:1In a suitable vessel, add the phospholipid stock and ethanol. Mix together for 5-10mins.2Add CBD to mixing solution. Allow to mix for 15-20 mins or until all CBD hasfully dissolved.3Once solution is homogenous. Add PEG-40 Hydrogenated Castor Oil. Allow tomix for 15-20 minutes or until homogenous.4Dilute an aliquot of final product 1:1000 and test for PSA.

[0073]The table below is an illustrative example of component concentration shown in descending order for a sample of passenger encapsulate prepared according to the present invention. The top section of the chart shows the solvent broken down by the perce...

example 2

ive Product Composition in the Cannabinoid Encapsulate

[0074]

ComponentINCI Name% in Product% BreakdownSolvent (diluent)Alcohol56.0056.00SurfactantPEG-4020.0020.00HydrogenatedCastor OilSolvent (stock)Alcohol14.0011.26PassengerCannabidiol10.0010.00Phospholipid (stock)Lecithin2.42Water (stock)Water0.32Final BreakdownFinal % BreakdownAlcohol67.26PEG-40 Hydrogenated Castor Oil20.00Cannabidiol10.00Lecithin2.42Water0.32100.00

[0075]The chart below illustrates several possible examples of oral preparations that may be prepared using a passenger encapsulate prepared according to the present invention. The passenger encapsulate used in these examples is a THC encapsulate having about 5% THC that is diluted to around 0.5% prior to use in the final preparation.

example 3

ive Oral Preparations Using the Cannabinoid Encapsulate

[0076]

Batch 3CompositionBatch 1Batch 2Chill #2Energy #2Water98.16296.8170.00QSSugar7.007.00Stevia Extract0.25Yerba Mate0.55Green Coffee Bean0.085Monk Fruit Extract 50%0.010.01Citric Acid0.670.670.450.18Potassium Sorbate0.100.100.100.10Black pepper Extract0.02Lemon Extract0.10Ginger0.070.07Tulsi Distillate0.10Turmeric Powder0.25Theanine0.10Water2.50EtOH0.35740.02EtOH Stock0.260.10Xanthan Gum0.050.150.200.10Glycerin0.501.501.501.50THC Encapsulate (adjusted0.51790.5160.4420.442for potency of THC)THC EncapsulateTHC5.005.005.005.00EtOH69.0069.6069.6069.60EtOH Stock25.5024.0024.0024.00PEG-40 Hydrogenated0.501.001.001.00Castor OilPolysorbate 200.400.400.40QS Water

[0077]The illustrative oral preparations in Example 3 are examples where the composition of Surfactant-Enhanced Phospholipid Vesicles with a THC passenger incorporated within the vesicles is combined with additional ingredients suitable for oral delivery of the passenger subst...

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Abstract

A composition comprising surfactant-enhanced phospholipid vesicles with one or more cannabinoid substance encapsulated therein is disclosed, wherein one or more surfactant is utilized for enhancing loading and increasing encapsulation efficiency of cannabinoid passenger molecules within phospholipid structures. A method is disclosed for making a surfactant-enhanced phospholipid vesicles with one or more cannabinoid substance encapsulated therein, wherein one or more surfactant is used for enhancing loading and increasing encapsulation efficiency of passenger molecules in phospholipid structures. A method of using surfactant-enhanced phospholipid vesicles with one or more cannabinoid substance encapsulated therein is disclosed wherein one or more surfactant enhances loading and increases encapsulation efficiency of cannabinoid substances in phospholipid structures. A composition and method of making surfactant-enhanced phospholipid vesicles with one or more lipophilic passenger substance encapsulated therein is disclosed wherein one or more surfactant is utilized for enhancing loading and increasing encapsulation efficiency of passenger molecules within phospholipid structures.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit of U.S. Provisional Application Nos. 62 / 779,797 filed Dec. 14, 2018, and 62 / 890,940, filed Aug. 23, 2019, which are incorporated by reference into this utility patent application.STATEMENT REGARDING FEDERALLY SPONSORED RESEARCH OR DEVELOPMENT[0002]Not applicable.TECHNICAL FIELD OF INVENTION[0003]This invention relates to the field of using surfactants to enhance encapsulation of lipophilic passenger molecules in nano-sized phospholipid structures.BACKGROUND OF THE INVENTION[0004]Active components have been sequestered in phospholipid particles using prior art methods and compositions, but these known prior art methods and compositions fail to retain all types of active components, especially at higher concentrations, in a solubilized state for extended periods of time, which decreases the overall stability and usability of the preparations.[0005]For instance, known nanolipid particle prior art, U.S. Pat...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): A61K9/127A61K31/05A61K47/26A61K47/44
CPCA61K47/44A61K31/05A61K36/185A61K31/352A61K47/26A61K9/1277A23P10/35A23L2/52A23L2/60A23L2/56A61K9/127A61K9/0095A61K9/0014A61K9/0053A61K47/24A23V2002/00A61K9/006A23L33/105A61K9/7023
InventorREYNOLDS, JEFFREY S.
OwnerNUVESSL INC