Double emulsion microencapsulation of proteins as model antigens using polylactide polymers

Effect of emulsifier on the microsphere characteristics and release kinetics

B. R. Conway, H. Oya Alpar

Research output: Contribution to journalArticle

38 Citations (Scopus)

Abstract

Polylactide and polylactide-co-glycolide microspheres containing a model protein, bovine serum albumin, were prepared by a double-emulsion, solvent evaporation process. Using scanning electron microscopy, the surface characteristics of the particles were examined together with the particle size distribution. Particles were approximately 1 μm in diameter with a narrow size range. The zeta potential and hydrophobicity of the surfaces were also investigated as was the crystallinity of the polymer and the microspheres, using differential scanning calorimetry. Drug encapsulation efficiency was highest (>90%) at theoretical loadings of 10% w/w. The surfactants used during preparation of the microspheres influenced the surface properties and loading of the particles as well as the release behaviour of the protein. Keeping all other variables constant, particles were manufactured using polyvinyl alcohol or polyvinylpyrrolidone during formation of the primary emulsion phase. Those formulated with polyvinylpyrrolidone resulted in significantly higher loadings (15.2% w/w vs. 11.3% w/w at 25% w/w theoretical loading) and also exhibited a marked reduction in the 'burst' release of protein (12% vs. 35%), thereby significantly extending the protein release period with 30% released in one week.

Original languageEnglish
Pages (from-to)42-48
Number of pages7
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume42
Issue number1
Publication statusPublished - 1 Jan 1996
Externally publishedYes

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Drug Compounding
Emulsions
Microspheres
Povidone
Polymers
Antigens
Period Circadian Proteins
Polyvinyl Alcohol
Proteins
Surface Properties
Differential Scanning Calorimetry
Bovine Serum Albumin
Hydrophobic and Hydrophilic Interactions
Particle Size
Surface-Active Agents
Electron Scanning Microscopy
Pharmaceutical Preparations
poly(lactide)

Cite this

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title = "Double emulsion microencapsulation of proteins as model antigens using polylactide polymers: Effect of emulsifier on the microsphere characteristics and release kinetics",
abstract = "Polylactide and polylactide-co-glycolide microspheres containing a model protein, bovine serum albumin, were prepared by a double-emulsion, solvent evaporation process. Using scanning electron microscopy, the surface characteristics of the particles were examined together with the particle size distribution. Particles were approximately 1 μm in diameter with a narrow size range. The zeta potential and hydrophobicity of the surfaces were also investigated as was the crystallinity of the polymer and the microspheres, using differential scanning calorimetry. Drug encapsulation efficiency was highest (>90{\%}) at theoretical loadings of 10{\%} w/w. The surfactants used during preparation of the microspheres influenced the surface properties and loading of the particles as well as the release behaviour of the protein. Keeping all other variables constant, particles were manufactured using polyvinyl alcohol or polyvinylpyrrolidone during formation of the primary emulsion phase. Those formulated with polyvinylpyrrolidone resulted in significantly higher loadings (15.2{\%} w/w vs. 11.3{\%} w/w at 25{\%} w/w theoretical loading) and also exhibited a marked reduction in the 'burst' release of protein (12{\%} vs. 35{\%}), thereby significantly extending the protein release period with 30{\%} released in one week.",
keywords = "Differential scanning calorimetry, Hydrophobicity, Oral vaccines, Polylactide microspheres, Polyvinyl alcohol, Polyvinylpyrrolidone, Protein antigens, Zeta potential",
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AB - Polylactide and polylactide-co-glycolide microspheres containing a model protein, bovine serum albumin, were prepared by a double-emulsion, solvent evaporation process. Using scanning electron microscopy, the surface characteristics of the particles were examined together with the particle size distribution. Particles were approximately 1 μm in diameter with a narrow size range. The zeta potential and hydrophobicity of the surfaces were also investigated as was the crystallinity of the polymer and the microspheres, using differential scanning calorimetry. Drug encapsulation efficiency was highest (>90%) at theoretical loadings of 10% w/w. The surfactants used during preparation of the microspheres influenced the surface properties and loading of the particles as well as the release behaviour of the protein. Keeping all other variables constant, particles were manufactured using polyvinyl alcohol or polyvinylpyrrolidone during formation of the primary emulsion phase. Those formulated with polyvinylpyrrolidone resulted in significantly higher loadings (15.2% w/w vs. 11.3% w/w at 25% w/w theoretical loading) and also exhibited a marked reduction in the 'burst' release of protein (12% vs. 35%), thereby significantly extending the protein release period with 30% released in one week.

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KW - Zeta potential

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