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Ammonolysis-based microencapsulation technique using isopropyl formate as dispersed solvent.

Hye-Yeum Im¹, Hongkee Sah

¹College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-gu, Seoul 120-750, South Korea.

International Journal of Pharmaceutics

|September 1, 2009

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This study introduces a novel ammonolysis-based microencapsulation technique using isopropyl formate for poly-D,L-lactide-co-glycolide microspheres. The method offers high encapsulation efficiency and significantly reduced solvent residues, presenting a promising alternative for drug delivery systems.

Area of Science:

Materials Science
Chemical Engineering
Pharmaceutical Technology

Background:

Traditional microencapsulation methods often involve solvent evaporation or extraction, which can lead to residual solvents in the final product.
Developing alternative techniques with improved safety profiles and efficiency is crucial for pharmaceutical applications.

Purpose of the Study:

To develop and assess a novel ammonolysis-based microencapsulation technique.
To utilize isopropyl formate, a food-grade flavoring agent, for creating poly-D,L-lactide-co-glycolide (PLGA) microspheres.
To evaluate the encapsulation efficiency, drug-polymer interactions, and residual solvent levels of the developed microspheres.

Main Methods:

An ammonolysis reaction was employed for rapid solvent removal from emulsion droplets at ambient conditions.

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Progesterone was used as a model drug for microencapsulation within PLGA microspheres.

Techniques including FTIR, DSC, XRD, and gas chromatography were used for analysis.

Main Results:

High encapsulation efficiencies were achieved, ranging from 88.0±3.6% to 97.0±3.6%.
FTIR analysis indicated no significant chemical interactions between the model drug and the polymer.
DSC and XRD data showed that drug loading influenced the physical state of progesterone within the microspheres.
Residual isopropyl formate levels were remarkably low, not exceeding 0.34±0.07%.

Conclusions:

The ammonolysis-based microencapsulation technique using isopropyl formate is feasible for preparing PLGA microspheres.
This method offers high encapsulation efficiency and significantly reduced residual solvent content.
The technique presents a potential alternative for developing safer and more efficient drug delivery systems.