Surface-Eroding Poly(ortho ester amides) for Highly Efficient Oral Chemotherapy.

Area of Science:

• Polymer Chemistry
• Biomaterials Science
• Drug Delivery Systems

Background:

• Poly(ortho ester amide) (POEA) copolymers are being explored for biomedical applications.
• Developing effective oral drug delivery systems for chemotherapy remains a significant challenge.

Purpose of the Study:

• To synthesize and characterize novel POEA copolymers (POEA-4 and POEA-5).
• To evaluate the drug release kinetics, biocompatibility, and in vivo efficacy of 5-fluorouracil (5-FU)-loaded POEA materials for oral chemotherapy.

Main Methods:

• Polycondensation of a novel ortho ester diamine monomer with aliphatic diacids to form POEA copolymers.
• In vitro studies to assess POEA mass loss and 5-FU release kinetics.
• In vitro cytotoxicity and in vivo acute toxicity tests in mice.
• In vivo antitumor efficacy evaluation of 5-FU-loaded POEA tablets against H22 transplanted tumors.

Main Results:

• POEA-4 and POEA-5 were successfully synthesized.
• Nearly zero-order kinetics were observed for both POEA mass loss and 5-FU release, indicating surface-restricted erosion and drug release.
• Excellent biocompatibility was confirmed through in vitro cytotoxicity tests.
• No adverse effects were observed in mice orally administered high doses of POEA-4 and POEA-5.
• 5-FU-loaded POEA tablets demonstrated in vivo antitumor efficacy against H22 transplanted tumors.

Conclusions:

• POEA-4 and POEA-5 exhibit controlled drug release properties and excellent biocompatibility.
• These POEA copolymers show significant potential as carriers for oral chemotherapy drug delivery.
• Further optimization of POEA-based materials could lead to advanced oral chemotherapy treatments.