Anionic Methacrylate Copolymer Microparticles for the Delivery of Myo-Inositol Produced by Spray-Drying: In Vitro and...

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Reproductive Medicine

Background:

• Myo-inositol (MI) is crucial for ovarian function and insulin sensitivity, often used in polycystic ovary syndrome (PCOS) management.
• Traditional MI formulations may have suboptimal oral absorption and therapeutic efficacy.
• Developing advanced drug delivery systems can improve MI's biological response and patient compliance.

Purpose of the Study:

• To develop and characterize a novel micro delivery system for myo-inositol using spray-drying technology.
• To evaluate the release profile, ex vivo intestinal permeation, and in vivo bioavailability of the myo-inositol microparticles.
• To assess the efficacy of the micro delivery system in increasing myo-inositol concentration at the ovarian site.

Main Methods:

• Anionic methacrylate copolymer microparticles loaded with myo-inositol were produced via spray-drying.
• Drug loading, particle size, release profiles, and ex vivo intestinal permeation were analyzed.
• In vivo studies in a rat model assessed pharmacokinetic parameters (AUC, Cmax) and ovarian follicle myo-inositol levels after single and repeated administration.

Main Results:

• The spray-dried microparticles achieved 14% drug loading and particle size <15 µm, suitable for oral administration.
• Batch n. 3 (Eudragit/MI ratio = 6) exhibited optimal modified release and minimal myo-inositol loss in acidic conditions.
• In vivo studies demonstrated a 1.5-fold increase in AUC and Cmax, and enhanced ovarian follicle myo-inositol levels (1.25-fold single, 1.66-fold repeated dose) compared to pure myo-inositol.

Conclusions:

• The developed micro delivery system significantly improves myo-inositol oral bioavailability and delivery to ovarian follicles.
• This advanced formulation offers a promising therapeutic strategy for PCOS by enhancing myo-inositol's biological effects.
• Spray-drying is an effective method for creating microparticles with improved pharmacokinetic profiles for myo-inositol.