Preparation of targeted isoniazid microspheres

Area of Science:

• Pharmaceutical Sciences
• Biomaterials Engineering
• Drug Delivery Systems

Background:

• Albumin microspheres offer a promising platform for drug delivery.
• Controlling microsphere stability is crucial for predictable drug release kinetics.
• Targeted delivery to specific organs, like the lungs, can enhance therapeutic efficacy.

Purpose of the Study:

• To prepare and characterize isoniazid-loaded albumin microspheres using different stabilization methods.
• To investigate the impact of albumin denaturation on microsphere stability and drug release.
• To evaluate the potential of these microspheres for passive lung targeting.

Main Methods:

• Microsphere preparation via chemical (glutaraldehyde) and heat denaturation of albumin.
• Characterization of microsphere stability through solubility measurements.
• In vitro assessment of drug release profiles.
• Factorial design approach to optimize microsphere properties (size, payload, release) by varying protein concentration, temperature, time, and aqueous volume.
• In vivo tracking of microspheres in experimental animals for lung targeting validation.

Main Results:

• Heat-denatured albumin microspheres exhibited slower drug release rates, correlating with increased denaturation.
• Increased severity of denaturation conditions led to decreased drug payload and slower drug release.
• Microsphere size, payload, and release profile were significantly influenced by factorial design parameters.
• In vivo studies provided validation for the passive lung targeting capability of the prepared microspheres.

Conclusions:

• Albumin denaturation is a key factor in modulating isoniazid release from microspheres.
• Optimized albumin microspheres demonstrate potential for passive lung targeting.
• The developed microspheres offer a viable approach for controlled delivery of isoniazid to the lungs.