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Updated: Mar 9, 2026
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Preparation and evaluation of posaconazole-loaded enteric microparticles in rats
Min Yang1, Zhonghua Dong1, Yongchun Zhang1
1a School of Pharmaceutical Sciences , Shandong University , Jinan , Shandong , PR China.
Objectives:
Posaconazole (POS) is an antifungal compound which has a low oral bioavailability. The aim of this study was to prepare POS enteric microparticles to enhance its oral bioavailability.
Methods:
POS enteric microparticles were prepared with hypromellose acetate succinate (HPMCAS) via the spray drying method. The solvent mixtures of acetone and ethanol used in the preparation of the microparticles were optimized to produce the ideal POS enteric microparticles. Multivariate data analysis using a principal component analysis (PCA) was used to find the relationship among the HPMCAS molecular characteristics, particle properties and drug release kinetics from the spray dried microparticles.
Key Findings:
The optimal spray solvent mixtures were critical to produce the POS microparticles with the defined polymer entanglement index, drug surface enrichment, particle size and drug loading. The HPMCAS molecular characteristics affected the microscopic connectivity and diffusivity of polymer matrix and eventually influenced the drug release behavior, and enhanced the bioavailability of POS.
Conclusions:
These studies suggested that the selection of suitable solvent mixtures of acetone and ethanol used in the spray drying of the microparticles was quite important to produce the entangled polymer structures with preferred polymer molecular properties of polymer coiling, overlap concentration and entanglement index. Additional studies on particle size and surface drug enrichment eventually produced HPMCAS-based enteric microparticles to enhance the oral bioavailability of POS.
Insights
Developing enteric microparticles with hypromellose acetate succinate (HPMCAS) via spray drying significantly enhanced the oral bioavailability of posaconazole (POS). Optimizing solvent mixtures was key to achieving desired particle properties and drug release.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Posaconazole (POS) exhibits low oral bioavailability, limiting its therapeutic efficacy.
- Developing advanced drug delivery systems is crucial for improving POS oral absorption.
Purpose of the Study:
- To prepare enteric microparticles of posaconazole (POS) using hypromellose acetate succinate (HPMCAS).
- To enhance the oral bioavailability of POS through optimized microparticle formulation.
Main Methods:
- POS enteric microparticles were fabricated using HPMCAS via spray drying.
- Acetone and ethanol solvent mixtures were optimized for microparticle preparation.
- Multivariate data analysis, including principal component analysis (PCA), was employed to correlate HPMCAS molecular characteristics, particle properties, and drug release kinetics.
Main Results:
- Optimal spray solvent mixtures were critical for achieving desired POS microparticle properties, including polymer entanglement index, drug surface enrichment, particle size, and drug loading.
- HPMCAS molecular characteristics influenced the polymer matrix's microscopic connectivity and diffusivity, impacting drug release behavior.
- The developed microparticles demonstrated enhanced bioavailability of POS.
Conclusions:
- The selection of appropriate acetone and ethanol solvent mixtures for spray drying is vital for creating entangled polymer structures with specific molecular properties.
- Fine-tuning particle size and surface drug enrichment resulted in HPMCAS-based enteric microparticles that effectively enhance POS oral bioavailability.
