Featured Research

from universities, journals, and other organizations

Molecular container gives drug dropouts a second chance

Date:
May 8, 2012
Source:
University of Maryland
Summary:
Chemists have designed a molecular container that can hold drug molecules and increase their solubility, in one case up to nearly 3,000 times.

Researchers created their "new class of general-purpose solubilizing agents" based on a type of compound called cucurbit[n]urils - or CB[n]. These are 'macrocyclic' molecules made up of units of bicyclic glycoluril C4H4N4O2 monomers. The n in CB[n] refers to the number of repeat units in the macrocycle. This is cucurbit[n]urils - or CB[n] n=5,6,7,8,10.
Credit: Image courtesy of University of Maryland

A cross-disciplinary team of researchers at the University of Maryland has designed a molecular container that can hold drug molecules and increase their solubility, in one case up to nearly 3000 times. Their discovery opens the possibility of rehabilitating drug candidates that were insufficiently soluble. It also offers an opportunity to improve successful drugs that could be made even better with better solubility.

The team's innovative findings were recently published in a study in Nature Chemistry, in which the authors note that "the solubility characteristics of 40-70 percent of new drug candidates are so poor that they cannot be formulated on their own, so new methods for increasing drug solubility are highly prized."

The Maryland scientists where able to increase the solubility of ten insoluble drugs by between 23 and 2,750 times, by forming container-drug complexes. They also show that their containers have low toxicity in human cell line and mice studies, and that the molecular containers can be built from inexpensive and readily available reagents.

"We already are working with drug companies to help them solubilize their interesting drug candidates and hope to get them interested in licensing our technology," says co-leader Volker Briken, an associate professor in the department of cell biology and molecular genetics and also a scientist in the Maryland Pathogen Research Institute.

The team, led by Briken and UMD Chemistry & Biochemistry Professor Lyle Isaacs, created their "new class of general-purpose solubilizing agents" based on a type of compound called cucurbit[n]urils -- or CB[n]. These are 'macrocyclic' molecules made up of units of bicyclic glycoluril C4H4N4O2 monomers. The n in CB[n] refers to the number of repeat units in the macrocycle.

Many previous attempts have been made to capture drug molecules within these and other synthetic cages and capsules to increase drugs' solubility, but with limited success.

Issacs and Briken say that next their team would like to increase the variety of novel acyclic CBs in order to be able to solubilize a maximal number of small chemical drug candidates, and also would like to generate CBs that can be specifically targeted -- for example to cancer cells.

Macrocycles have long been studied and used for a variety of applications such as synthetic dyes and for fabric softeners and other household products. Medical applications related to the current UMD study include cyclodextrin molecular containers currently used for the formulation of hydrophobic insoluble drugs that are on the market.

Examples of biological macrocyclic molecules are Heme, the active site in hemoglobin (the protein in blood that transports oxygen) and the chlorin ring in chlorophyll (the green photosynthetic pigment found in plants).


Story Source:

The above story is based on materials provided by University of Maryland. Note: Materials may be edited for content and length.


Journal Reference:

  1. Da Ma, Gaya Hettiarachchi, Duc Nguyen, Ben Zhang, James B. Wittenberg, Peter Y. Zavalij, Volker Briken, Lyle Isaacs. Acyclic cucurbit[n]uril molecular containers enhance the solubility and bioactivity of poorly soluble pharmaceuticals. Nature Chemistry, 2012; DOI: 10.1038/nchem.1326

Cite This Page:

University of Maryland. "Molecular container gives drug dropouts a second chance." ScienceDaily. ScienceDaily, 8 May 2012. <www.sciencedaily.com/releases/2012/05/120508152129.htm>.
University of Maryland. (2012, May 8). Molecular container gives drug dropouts a second chance. ScienceDaily. Retrieved October 22, 2014 from www.sciencedaily.com/releases/2012/05/120508152129.htm
University of Maryland. "Molecular container gives drug dropouts a second chance." ScienceDaily. www.sciencedaily.com/releases/2012/05/120508152129.htm (accessed October 22, 2014).

Share This



More Matter & Energy News

Wednesday, October 22, 2014

Featured Research

from universities, journals, and other organizations


Featured Videos

from AP, Reuters, AFP, and other news services

Chameleon Camouflage to Give Tanks Cloaking Capabilities

Chameleon Camouflage to Give Tanks Cloaking Capabilities

Reuters - Innovations Video Online (Oct. 22, 2014) — Inspired by the way a chameleon changes its colour to disguise itself; scientists in Poland want to replace traditional camouflage paint with thousands of electrochromic plates that will continuously change colour to blend with its surroundings. The first PL-01 concept tank prototype will be tested within a few years, with scientists predicting that a similar technology could even be woven into the fabric of a soldiers' clothing making them virtually invisible to the naked eye. Matthew Stock reports. Video provided by Reuters
Powered by NewsLook.com
Jet Sales Lift Boeing Profit 18 Pct.

Jet Sales Lift Boeing Profit 18 Pct.

Reuters - Business Video Online (Oct. 22, 2014) — Strong jet demand has pushed Boeing to raise its profit forecast for the third time, but analysts were disappointed by its small cash flow. Fred Katayama reports. Video provided by Reuters
Powered by NewsLook.com
Internet of Things Aims to Smarten Your Life

Internet of Things Aims to Smarten Your Life

AP (Oct. 22, 2014) — As more and more Bluetooth-enabled devices are reaching consumers, developers are busy connecting them together as part of the Internet of Things. (Oct. 22) Video provided by AP
Powered by NewsLook.com
What Is Magic Leap, And Why Is It Worth $500M?

What Is Magic Leap, And Why Is It Worth $500M?

Newsy (Oct. 22, 2014) — Magic Leap isn't publicizing much more than a description of its product, but it’s been enough for Google and others to invest more than $500M. Video provided by Newsy
Powered by NewsLook.com

Search ScienceDaily

Number of stories in archives: 140,361

Find with keyword(s):
 
Enter a keyword or phrase to search ScienceDaily for related topics and research stories.

Save/Print:
Share:  

Breaking News:

Strange & Offbeat Stories

 

Space & Time

Matter & Energy

Computers & Math

In Other News

... from NewsDaily.com

Science News

Health News

Environment News

Technology News



Save/Print:
Share:  

Free Subscriptions


Get the latest science news with ScienceDaily's free email newsletters, updated daily and weekly. Or view hourly updated newsfeeds in your RSS reader:

Get Social & Mobile


Keep up to date with the latest news from ScienceDaily via social networks and mobile apps:

Have Feedback?


Tell us what you think of ScienceDaily -- we welcome both positive and negative comments. Have any problems using the site? Questions?
Mobile iPhone Android Web
Follow Facebook Twitter Google+
Subscribe RSS Feeds Email Newsletters
Latest Headlines Health & Medicine Mind & Brain Space & Time Matter & Energy Computers & Math Plants & Animals Earth & Climate Fossils & Ruins