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Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

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Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
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Drug delivery methods like oral inhalation, nasal sprays, transdermal patches, eye drops, intravitreal injection,  and rectal administration provide localized effects with reduced toxicity.
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The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
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Design, Development, and Evaluation of Treprostinil Embedded Adhesive Transdermal Patch.

Ibrahim Alissa1, Anroop B Nair1, Bandar Aldhubiab1

  • 1Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.

Pharmaceutics
|April 28, 2023
PubMed
Summary

This study developed a treprostinil transdermal patch to improve pulmonary arterial hypertension treatment. The optimized patch demonstrated effective skin delivery and enhanced bioavailability compared to oral treprostinil.

Keywords:
optimizationpatchpharmacokineticspulmonary arterial hypertensiontransdermaltreprostinil

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Pharmacology

Background:

  • Pulmonary arterial hypertension (PAH) treatment with treprostinil is limited by frequent dosing and adverse effects.
  • Transdermal drug delivery offers a potential alternative for sustained treprostinil administration.

Purpose of the Study:

  • To formulate and evaluate an adhesive-type transdermal patch of treprostinil for PAH.
  • To optimize the patch formulation using a 3^2-factorial design and assess its in vitro and in vivo performance.

Main Methods:

  • A 3^2-factorial design was employed to optimize drug amount and enhancer concentration for drug release and transdermal flux.
  • The optimized patch underwent evaluation for pharmaceutical properties, skin irritation, and pharmacokinetics in rats.
  • In vitro release studies, FTIR, DSC, and pharmacokinetic analysis were performed.

Main Results:

  • Drug amount significantly influenced drug release and transdermal flux (p < 0.0001).
  • The optimized patch exhibited high drug content (>95%), suitable morphology, drug-excipient compatibility, and amorphous drug state.
  • The patch demonstrated adequate adhesion, painless removal, safety (no skin irritation), steady Fickian diffusion release, and high transdermal delivery (~23.26 µg/cm²/h).
  • Transdermal treprostinil showed significantly higher absorption (p < 0.0001) and 237% relative bioavailability compared to oral administration.

Conclusions:

  • The developed adhesive transdermal patch effectively delivers treprostinil through the skin.
  • This transdermal patch represents a promising alternative treatment for pulmonary arterial hypertension, potentially improving patient compliance and reducing adverse effects.