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Pectin microparticles for peptide delivery: Optimization of spray drying processing.

Tingting Li¹, Bo Wan¹, Rajan Jog¹

¹Department of Pharmaceutical Sciences, University of Connecticut, Storrs, CT 06269, United States.

International Journal of Pharmaceutics

|December 17, 2021

Summary

Spray-dried pectin microparticles show promise for peptide oral delivery. Optimizing spray drying parameters using design of experiments (DoE) significantly improved microparticle yield, crucial for effective peptide formulations.

Keywords:

Design of experiments Octreotide acetate Pectin microparticles Spray drying

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Area of Science:

Pharmaceutical Technology
Materials Science
Biotechnology

Background:

Pectin microparticles offer mucoadhesion for enhanced peptide oral bioavailability.
Spray drying process parameters critically affect microparticle quality attributes, posing formulation challenges.

Purpose of the Study:

To investigate the impact of spray drying parameters on pectin microparticle yield and particle size.
To develop a predictive model for optimizing pectin microparticle production for peptide delivery.

Main Methods:

Utilized a central composite design (DoE) to study input temperature, aspirator rate, feed flow rate, and polymer concentration.
Spray drying was employed to prepare pectin microparticles, with yield and particle size as key metrics.
Validated the yield prediction model using octreotide acetate-loaded microparticles.

Main Results:

A statistically significant mathematical model predicted microparticle yield with good accuracy, achieving a maximum yield of 72.2%.
Particle size (D50, 2.16-3.67 μm) was largely independent of the spray drying parameters investigated.
Octreotide acetate incorporation increased surface roughness and decreased melting enthalpy; high esterification pectin enhanced drug release.

Conclusions:

Design of Experiments (DoE) is vital for optimizing spray drying of pectin-based peptide microparticles.
The developed yield prediction model can aid in formulating similar peptide-loaded microparticle drug products.
This study presents the first use of spray-dried pectin microparticles for octreotide delivery.