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Related Concept Videos

Drugs for Peptic Ulcer Disease: Prostaglandin Analogs as Mucosal Protective Agents01:20

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The gastric mucosa produces prostaglandins E2 (PGE2) and prostacyclin (PGI2), crucial in maintaining gastric health. They exert cytoprotective effects, including increasing bicarbonate secretion, releasing protective mucin, reducing gastric acid output, and preventing harmful vasoconstriction. These effects are mediated through various receptors, such as EP1, EP2, EP3, and EP4.
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Medical treatment strategies for peptic ulcers encompass various methods. The primary goal of treatment is to diminish gastric acidity and strengthen mucosal defense mechanisms.
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Pharmacological management
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Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
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Evaluation of the In vivo Antitumor Activity of Polyanhydride IL-1α Nanoparticles
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Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in

Salma E El-Habashy1, Ahmed N Allam1, Amal H El-Kamel1

  • 1Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.

International Journal of Nanomedicine
|June 17, 2016
PubMed
Summary

Ethyl cellulose nanoparticles (EC-NPs) effectively reduced the gastric irritation of piroxicam (PX). This drug delivery system offers a promising approach to mitigate side effects associated with PX oral administration.

Keywords:
NSAIDsgastric irritationpharmacokineticspoloxamerpolymeric nanoparticles

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Drug Delivery

Background:

  • Nanoparticles (NPs) are utilized in drug formulations to enhance bioavailability, prolong drug release, and reduce toxicity.
  • Ethyl cellulose-based nanoparticles (EC-NPs) offer potential for improved drug delivery systems.
  • Piroxicam (PX) is an acidic drug known for its gastrointestinal side effects.

Purpose of the Study:

  • To evaluate ethyl cellulose-based nanoparticles (EC-NPs) for modulating piroxicam (PX) release.
  • To assess the potential of EC-NPs to reduce the ulcerogenicity of piroxicam after oral administration.

Main Methods:

  • PX-loaded EC-NPs were prepared using the solvent evaporation technique with various stabilizers.
  • The optimum formulation (poloxamer-stabilized EC-NPs, P188/0.2) was characterized for particle size, polydispersity index, and entrapment efficiency.
  • In vivo studies included pharmacokinetic analysis and evaluation of gastric irritation in rats.

Main Results:

  • The optimum formulation exhibited a particle size of 240.26±29.24 nm and 85.29%±1.57% entrapment efficiency.
  • Poloxamer-stabilized EC-NPs showed modulated PX release (88% at 12 hours) and significantly increased time to maximum plasma concentration (t max) compared to commercial capsules.
  • Encapsulation of PX in EC-NPs significantly suppressed gastric ulceration by 66% in rats.

Conclusions:

  • Poloxamer-stabilized EC-NPs (P188/0.2) demonstrate significant potential for improving piroxicam oral delivery.
  • This formulation effectively modulates drug release and substantially reduces the gastric side effects of piroxicam.
  • EC-NPs represent a viable strategy to mitigate the deleterious effects of acidic drugs like piroxicam.