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Related Concept Videos

Modified-Release Drug Delivery Systems: Rate-Programmed I01:22

Modified-Release Drug Delivery Systems: Rate-Programmed I

Rate-programmed drug delivery systems (DDS) are designed to release drugs at specific, controlled rates to maintain consistent therapeutic levels. These systems are categorized based on their release mechanisms, including dissolution-controlled DDS, diffusion-controlled DDS, and combined dissolution-diffusion-controlled DDS.In dissolution-controlled DDS, the release rate depends on the slow dissolution of the drug itself or the surrounding matrix. Drugs with inherently slow dissolution rates,...
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors01:20

Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors

Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Site-Targeted Drug Delivery Systems: Polymeric Carriers01:24

Site-Targeted Drug Delivery Systems: Polymeric Carriers

Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
Modified-Release Drug Delivery Systems: Overview01:19

Modified-Release Drug Delivery Systems: Overview

Modified-release dosage forms are designed to address the limitations of drugs with short biological half-lives. These forms maintain stable therapeutic drug concentrations over extended periods, reducing the need for frequent dosing. A consistent drug level helps minimize peak-trough fluctuations, which can reduce adverse effects, lower the risk of drug resistance, and improve overall treatment effectiveness.One common type of modified-release form is the extended-release (ER) formulation. ER...
Modified-Release Drug Delivery Systems: Rate-Programmed II01:19

Modified-Release Drug Delivery Systems: Rate-Programmed II

Rate-programmed drug delivery systems release drugs in a controlled manner to maintain therapeutic levels. Three main designs include reservoir, matrix, and hybrid systems.Reservoir systems consist of a drug core enclosed within a membrane that controls drug release. In non-swelling reservoir systems, polymers like ethyl cellulose or polymethacrylates are used. These do not hydrate in aqueous media and control release through membrane thickness, porosity, or insolubility. This type includes...
Oral Drug Delivery Systems: Delayed-Release Systems01:11

Oral Drug Delivery Systems: Delayed-Release Systems

Delayed-release drug delivery systems are specialized pharmaceutical formulations designed to postpone the release of active compounds until the drug reaches a specific region of the gastrointestinal (GI) tract, typically the intestine. These systems are essential for drugs that may cause gastric irritation, are unstable in acidic environments, or need to exert therapeutic effects locally in the intestinal or colonic regions.The core feature of delayed-release systems is the use of enteric...

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Updated: Jun 17, 2026

Encapsulation of Cancer Therapeutic Agent Dacarbazine Using Nanostructured Lipid Carrier
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Published on: April 26, 2016

Darapladib.

Quang T Bui1, Robert L Wilensky

  • 1University of Pennsylvania, Hospital of the University of Pennsylvania, Cardiovascular Institute, Cardiovascular Division, Philadelphia, PA 19104, USA.

Expert Opinion on Investigational Drugs
|December 17, 2009
PubMed
Summary
This summary is machine-generated.

Darapladib, a selective inhibitor of lipoprotein-associated phospholipase A(2) (Lp-PLA(2)), targets inflammation in atherosclerosis. This new therapeutic agent shows promise for treating high-risk atherosclerosis by inhibiting Lp-PLA(2) activity.

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Antibiotic Dereplication Using the Antibiotic Resistance Platform
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Area of Science:

  • Cardiovascular Medicine
  • Inflammation Research
  • Pharmacology

Background:

  • Atherosclerosis is an inflammatory disease where plaque rupture causes major cardiovascular events.
  • Lipoprotein-associated phospholipase A(2) (Lp-PLA(2)) plays a key role in developing high-risk atherosclerotic lesions.
  • Darapladib is a selective Lp-PLA(2) inhibitor developed to target this process.

Purpose of the Study:

  • To review studies supporting darapladib's development (1990-2009).
  • To discuss darapladib's potential as a therapeutic agent for high-risk atherosclerosis.
  • To elucidate the role of Lp-PLA(2) in atherogenesis.

Main Methods:

  • Literature review of studies on darapladib and Lp-PLA(2) from 1990-2009.
  • Analysis of the biological role of Lp-PLA(2) in atherosclerosis.
  • Discussion of the therapeutic potential of selective Lp-PLA(2) inhibitors.

Main Results:

  • Understanding the inflammatory basis of atherogenesis.
  • Insight into the pro-atherogenic role of Lp-PLA(2).
  • Recognition of selective Lp-PLA(2) inhibitors as potential therapeutic agents.

Conclusions:

  • Darapladib selectively inhibits Lp-PLA(2).
  • Darapladib represents a novel therapeutic class targeting inflammation in atherosclerosis.
  • This approach aims to treat high-risk atherosclerosis effectively.