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pH-triggered release of macromolecules from spray-dried polymethacrylate microparticles
Daniel S Kohane1, Daniel G Anderson, Christine Yu
1Massachusetts General Hospital and Harvard Medical School, Boston, Massachusetts, USA.
Pharmaceutical Research
|November 19, 2003
Summary
New pH-triggered microparticles, incorporating Eudragit E100 (E100), show efficient intracellular drug delivery. These safe, inhalable particles release therapeutics at acidic pH, demonstrating potential for enhanced drug targeting.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Nanotechnology
Background:
- pH-triggered microparticles enhance intracellular drug delivery by releasing payloads at acidic pH.
- Lipid-based microparticles are known for safety and efficacy in neural applications and potential inhalability.
Purpose of the Study:
- To modify existing lipid-based microparticles for pH-triggerable drug release.
- To incorporate Eudragit E100 (E100), an acid-soluble polymethacrylate, into microparticles.
- To assess the potential for inhalable, pH-triggered intracellular drug delivery.
Main Methods:
- Microparticles were fabricated using spray-drying.
- Characterization included electron microscopy, Coulter counting, density measurements, and protein release kinetics.
- Biocompatibility and cellular uptake were evaluated in vivo in rats.
Main Results:
- Spray-dried microparticles were 3-5 microm in diameter with densities of 0.12-0.25 g/L.
- Microparticles with ≥20% E100 exhibited rapid protein release at pH 5 and slow release at pH 7.4.
- pH-triggerability persisted for over 2 weeks; particles were biocompatible in rat tissue, with macrophage uptake observed.
Conclusions:
- Microparticles containing Eudragit E100 (E100) demonstrated sustained pH-triggerable release.
- Macrophage uptake suggests utility for intracellular drug delivery.
- These modified microparticles show promise for efficient and targeted therapeutic applications.