Controlled delivery system for norethindrone based on biodegradable poly-alpha,beta-(hydroxyalkyl)-DL-aspartamide

Area of Science:

• Polymer Chemistry
• Biomaterials Science
• Drug Delivery Systems

Background:

• Development of novel polymeric drug carriers is crucial for improving therapeutic efficacy and patient compliance.
• Poly-(hydroxyalkyl)-DL-aspartamide (PHAA) presents a potential candidate due to its biocompatibility and hydrophilic nature.

Purpose of the Study:

• To synthesize and characterize PHAA and its drug conjugates.
• To evaluate the biocompatibility and drug release kinetics of PHAA as a drug carrier.
• To investigate the in vivo performance of PHAA-drug conjugates.

Main Methods:

• Polymer synthesis via ring-opening polymerization.
• Characterization using FTIR, DSC, X-ray diffraction, 13C NMR, and SEM.
• In vitro drug release studies in buffer solution (pH 7.4, 37°C).
• In vivo drug release studies in rabbits over 120 days.

Main Results:

• PHAA was successfully synthesized and characterized, confirming its structure.
• PHAA demonstrated excellent biocompatibility: hydrophilic, non-toxic in vivo, and non-antigenic.
• Drug release kinetics were influenced by side chain length, drug loading, and particle size.
• In vivo studies showed sustained norethindrone (NET) release, achieving 1-2 μg/mL serum concentration after 1 month with 10% NET released.

Conclusions:

• PHAA is a promising biocompatible material for sustained drug delivery applications.
• The developed PHAA-NET conjugates exhibit controlled drug release profiles.
• Further research into PHAA-based drug delivery systems is warranted.