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Enteric micro-particles for targeted oral drug delivery
Annalisa Dalmoro1, Gaetano Lamberti, Giuseppe Titomanlio
1Dipartimento di Ingegneria Chimica e Alimentare, Università degli Studi di Salerno, via Ponte don Melillo, 84084, Fisciano, Salerno, Italy.
AAPS Pharmscitech
|October 9, 2010
Summary
Researchers developed pH-sensitive micro-particles for oral drug delivery using a novel copolymer. Optimizing emulsion stabilizer and stirring power significantly improved encapsulation efficiency for better drug delivery.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Polymer Chemistry
Background:
- Developing effective oral drug delivery systems requires careful control over particle properties.
- pH-sensitive polymers are crucial for targeted drug release in specific gastrointestinal environments.
- Solvent evaporation techniques are widely used for micro-particle formulation.
Purpose of the Study:
- To produce enteric-coated micro-particles for oral administration using a water-in-oil-in-water solvent evaporation technique.
- To optimize the encapsulation efficiency of pH-sensitive micro-particles using a novel poly(methyl methacrylate-acrylic acid) copolymer.
- To investigate the impact of emulsion stabilizer (polyvinyl alcohol) percentage and stirring power on encapsulation efficiency.
Main Methods:
- Utilized a water-in-oil-in-water solvent evaporation technique for micro-particle production.
- Initially employed cellulose acetate phthalate (CAP) for encapsulation, then transitioned to a novel synthesized poly(methyl methacrylate-acrylic acid) (poly(MMA-AA)) copolymer.
- Investigated the effects of varying polyvinyl alcohol (PVA) concentration and stirring power on double emulsion stability and encapsulation efficiency.
Main Results:
- Theophylline encapsulation in CAP yielded desired pH-dependent release but low encapsulation efficiency.
- Using poly(MMA-AA) copolymer, encapsulation efficiency increased with higher polyvinyl alcohol (PVA) percentage.
- Increased PVA content and decreased stirring power led to a more stable double emulsion, significantly enhancing encapsulation efficiency.
Conclusions:
- The novel synthesized poly(MMA-AA) copolymer is a promising material for developing pH-sensitive enteric-coated micro-particles.
- Optimizing process parameters, specifically PVA concentration and stirring power, is critical for achieving high encapsulation efficiency in double emulsion solvent evaporation.
- The developed micro-particles demonstrate potential for controlled oral drug delivery with improved drug loading.
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