Connect with us

Heartland

Analog Derivatization of Cannabidiol for Improved Ocular Permeation

Purpose: Cannabidiol (CBD), active component of plant Cannabis sativa, has anti-inflammatory properties that could potentially help treat diabetic retinopathy-induced pain and inflammation. However, CBD is a lipophilic molecule making its topical delivery to back of the eye challenging. This study aims at improving ocular penetration of CBD by means of analog derivatization. Methods: Analogs were designed using various ligands, such as amino acids (AAs) and dicarboxylic acids (DCAs) and their…

Republished by Plato

Published

on

Purpose: Cannabidiol (CBD), active component of plant Cannabis sativa, has anti-inflammatory properties that could potentially help treat diabetic retinopathy-induced pain and inflammation. However, CBD is a lipophilic molecule making its topical delivery to back of the eye challenging. This study aims at improving ocular penetration of CBD by means of analog derivatization. Methods: Analogs were designed using various ligands, such as amino acids (AAs) and dicarboxylic acids (DCAs) and their combinations. Select analogs were screened in vitro with respect to their stability in ocular tissue homogenates. Based on in vitro stability, analogs were selected for in rabbits testing. Formulations containing these compounds were tested in rabbits to determine ocular tissue disposition of CBD and the analogs after topical application. The rabbits were sacrificed 90 min post-topical application and the aqueous humor, vitreous humor (VH), iris-ciliary bodies (IC), and retina-choroid (RC) were analyzed for CBD and analog content. Results: CBD-divalinate-dihemisuccinate (CBD-Di-VHS) and CBD-divalinate (CBD-Di-Val) were stable in the ocular tissue homogenates. Post-topical application, CBD and CBD-Di-Val analog levels were detected only in RC. Dosing of CBD-Di-VHS nanoemulsion generated analog levels both in the VH and in the RC, respectively. In contrast, post dosing of CBD-monovalinate-monohemisuccinate (CBD-Mono-VHS), both the analog and CBD were detected in the IC and RC. Conclusion: The analogs demonstrated superior penetration into ocular tissues in comparison with CBD. CBD-Di-VHS and CBD-Mono-VHS exhibited better permeation properties, possibly due to improved stability and physicochemical characteristics imparted by AA and DCA combination derivatives.

Keywords: analogs; anti-inflammatory; cannabidiol; ocular bioavailability.

Source: https://pubmed.ncbi.nlm.nih.gov/30998110/?utm_source=no_user_agent&utm_medium=rss&utm_campaign=pubmed-2&utm_content=1TQbL92JdzYTve0m3OsSoggMby2JyZDVBLRHiDMYZkT1hs6YNQ&fc=20200804223051&ff=20200816030733&v=2.11.5

Heartland

Republished by Plato

Published

on

Checkout PrimeXBT
Trade with the Official CFD Partners of AC Milan
Source:

Continue Reading

Heartland

Republished by Plato

Published

on

Checkout PrimeXBT
Trade with the Official CFD Partners of AC Milan
Source:

Continue Reading

Heartland

Republished by Plato

Published

on

Checkout PrimeXBT
Trade with the Official CFD Partners of AC Milan
Source:

Continue Reading
Heartland4 days ago

CBD Vape Oil Market 2021: Global Trends, Business Overview, Challenges, Opportunities …

Heartland5 days ago

Industrial Hemp in Automotive Market Estimated Forecast Analysis 2021-2030

Material4 days ago

Microstructure, characterization of interfacial phases and mechanical properties of high Nb–TiAl/Al2O3 joints brazed by novel Nb particle-reinforced Ag–Cu filler alloy

Heartland4 days ago

Drew Carey CBD – How Does It Work For Body Pain

Heartland5 days ago

Heartland5 days ago

Heartland5 days ago

Natures Method CBD Gummies : How To Order & Basic Price Detail?

Material5 days ago

Experimental study on evolution of oxidation behavior on high-temperature continuous casting slab surface

Heartland4 days ago

Hemp a budding industry in New Mexico

Heartland5 days ago

Cannabis and the Autistic Spectrum

Material4 days ago

Corrosion resistance and electrical contact resistance of a thin permanganate conversion coating on dual-phase LZ91 Mg–Li alloy

Heartland5 days ago

Heartland4 days ago

The CBD Skincare Line Nicole Kidman Swears By

Heartland4 days ago

Heartland3 days ago

Hello, im new to CBD and I just got this e-liquid and a pen. I looked up the vape juice after, and it doesn’t seem to exist.. Has anyone else used this brand?

Material5 days ago

The effect of flux chemistry on element transfer in Submerged Arc Welding: application of thermochemical modelling

Metal4 days ago

ExOne names distributor in South Korea

Heartland4 days ago

House passes $1.9 trillion COVID relief plan

Heartland4 days ago

Metal2 days ago

ArcelorMittal raises CRC and HDG prices in Europe

Heartland4 days ago

Hemp a budding industry in New Mexico

Heartland3 days ago

Top 5 reasons people use CBD tinctures

News2 days ago

Automated processing of aerospace scrap for precious elements

Heartland1 day ago

CBD and Menopause

Heartland5 days ago

Global CBD Hemp Oil Market 2021 Analysis Trend, Applications, Industry Chain Structure, Growth …

Heartland4 days ago

https://gayle-king-cbdoil-review.medium.com/gayle-king-cbdoil-real-reviews-and

Heartland3 days ago

Metal2 days ago

US manufacturing PMI rises to 60.8 percent in February

Heartland2 days ago

Best CBD store in Europe?

Heartland5 days ago

Can I Use My MMJ Card in States Where It’s Not Legal?

Trending

A Cloud Nine Capital Entity Copyright © 2020 – All Rights Reserved Proudly Made in America