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A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles

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PVP/aprepitant microcapsules produced by supercritical antisolvent process.

Zhuo Zhang¹, Guizhou Hao², Xuemei Sun¹

¹College of Mechanical and Vehicle Engineering, Linyi University, Linyi, 276000, China.

Scientific Reports

|May 9, 2024

Summary

This summary is machine-generated.

The supercritical antisolvent (SAS) process offers a green method for creating drug microcapsules, improving drug dissolution. This study demonstrates the SAS process

Keywords:

Aprepitant Coaxial annular nozzle Industrialization Microcapsules Supercritical antisolvent process

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Published on: January 7, 2019

Area of Science:

Pharmaceutical Technology
Green Chemistry
Materials Science

Background:

Insoluble drugs often exhibit poor bioavailability, limiting their therapeutic efficacy.
The supercritical antisolvent (SAS) process presents a sustainable approach to enhance drug solubility and delivery.
Scaling up SAS processes for industrial pharmaceutical production remains a challenge due to capacity limitations.

Purpose of the Study:

To develop microcapsules of aprepitant (APR) using the SAS process with polyvinylpyrrolidone (PVP).
To investigate the impact of process parameters on microcapsule characteristics.
To evaluate the industrial scalability of the SAS process for pharmaceutical manufacturing.

Main Methods:

A coaxial annular nozzle was employed for microencapsulation of aprepitant (APR) and polyvinylpyrrolidone (PVP) via SAS using N, N-Dimethylformamide (DMF).
Systematic analysis of polymer/drug ratio, operating pressure, temperature, and concentration effects on particle morphology, size, and distribution.
Characterization of microcapsules including morphology, particle size, thermal behavior, crystallinity, drug content, dissolution, and residual solvent.

Main Results:

Successfully produced microcapsules with mean diameters between 2.04 μm and 9.84 μm.
Optimized SAS process parameters led to improved particle characteristics and morphology.
Enhanced dissolution rates were observed for APR microcapsules compared to unprocessed APR.
Kilogram-level production capacity was demonstrated, confirming industrial feasibility.

Conclusions:

The SAS process, utilizing a coaxial annular nozzle, is effective for producing aprepitant microcapsules with enhanced dissolution.
Process parameter optimization is crucial for controlling microcapsule properties.
The study validates the industrial scalability of the SAS process for pharmaceutical production, addressing previous capacity limitations.