Spray-dried cyclophosphamide-loaded polyhydroxyalkanoate microparticles: design and characterization

Area of Science:

• Biomaterials Science
• Drug Delivery Systems
• Polymer Chemistry

Background:

• Cyclophosphamide (CP) is a vital antitumor and immunosuppressive drug.
• CP's high cytotoxicity, carcinogenicity, and teratogenicity necessitate strategies to mitigate adverse effects.
• Limited biodegradable polymers are suitable for CP encapsulation and sustained release.

Purpose of the Study:

• To develop and characterize novel cyclophosphamide-loaded poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) microparticles.
• To evaluate the potential of PHBV microparticles as a sustained-release delivery system for CP.
• To assess the impact of microencapsulation on CP's physical properties and cytotoxicity.

Main Methods:

• Spray-drying technique was employed to prepare CP-loaded PHBV microparticles.
• Characterization included particle size, polydispersity index, zeta potential, surface morphology, encapsulation efficiency, drug loading, and thermal properties.
• Cytotoxicity was evaluated against 3T3 cells, and in vitro drug release was monitored over 18 days.

Main Results:

• Spherical PHBV microparticles with uniform size (4.21±0.04 μm) and negative zeta potential (-34.2±0.2 mV) were obtained.
• Microencapsulation altered CP's thermal properties and reduced its cytotoxicity by 28% while increasing metabolic activity by 20%.
• Sustained CP release was observed for up to 18 days, confirming the potential of the formulation.

Conclusions:

• A novel and effective platform for cyclophosphamide delivery using PHBV microparticles was successfully established.
• The developed microparticles demonstrate potential for improved cancer therapy through sustained drug release and reduced toxicity.
• This research offers promising prospects for advancing chemotherapy treatments.