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Approaches for Gastro-Retentive Drug Delivery Systems (GRDDS)

  • Gastro-Retentive Drug Delivery Systems (GRDDS) aim to prolong and control drug release in the stomach, improving therapeutic efficacy and bioavailability for drugs with a narrow absorption window in the upper gastrointestinal (GI) tract.

Approaches for Gastro-Retentive Drug Delivery Systems (GRDDS)

Floating Systems

Mechanism:

  • Dosage forms with lower density than gastric fluids float on the stomach contents, remaining buoyant until the drug is released.

Key Components:

  • Polymers: Hydroxypropyl methylcellulose (HPMC), ethylcellulose.

  • Gas-Generating Agents: Sodium bicarbonate, citric acid (produce CO₂ for buoyancy).

Types:

  • Effervescent Systems: Generate CO₂ to float (e.g., tablets with bicarbonate and acid).

  • Non-Effervescent Systems: Rely on polymer swelling for buoyancy.

Applications:

  • Drugs acting in the stomach (e.g., antacids).

  • Drugs absorbed from the stomach (e.g., levodopa).

  • Drugs with narrow absorption windows in the upper intestine (e.g., furosemide).

High-Density Systems

Mechanism:

  • Dosage forms sink to the bottom of the stomach due to higher density (>1.5 g/cm³) and remain there.

Key Components:

  • High-density materials like barium sulfate, zinc oxide.

Applications:

  • Drugs causing gastric irritation (keep away from sensitive areas).

  • Drugs acting locally in the stomach.

  • Drugs absorbed in the upper intestine.

Inflatable Systems

Mechanism:

  • Expand in the stomach to prevent passing through the pyloric sphincter, ensuring prolonged retention.

Key Components:

  • Drug core with an inflatable shell containing gas-generating agents (e.g., sodium bicarbonate).

Types:

  • Balloon Systems: Inflate in the stomach for buoyancy.

  • Collapsible Capsules: Inflated chamber seals the drug reservoir.

Applications:

  • Drugs absorbed in the stomach or upper intestine.

  • Controlled drug release with extended therapeutic effects.

Gastroadhesive (Bioadhesive) Systems

Mechanism:

  • Adhere to the gastric mucosa using bioadhesive polymers, prolonging gastric residence time.

Key Components:

  • Bioadhesive polymers: HPMC, chitosan, poly(acrylic acid), carbopol.

Types:

  • Bioadhesive Tablets: Traditional tablets with adhesive properties.

  • Films or Patches: Thin adhesive layers applied to the gastric mucosa.

  • Micro/Nanoparticles: Small particles with bioadhesive capabilities.

Applications:

  • Localized action (e.g., for ulcers).

  • Drugs with narrow absorption.


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