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Minocycline Hydrochloride Controlled-release Microsphere Preparation Process Optimization Based on the Robust Design

Mohammad Karim Haidar1, Fumiyoshi Yamashita2, Mitsuru Hashida2

  • 1Erzincan Binali Yıldırım University Faculty of Pharmacy, Department of Pharmaceutical Technology, Erzincan, Turkey.

Turkish Journal of Pharmaceutical Sciences
|January 4, 2022
PubMed
Summary
This summary is machine-generated.

This study optimized minocycline hydrochloride (MCH) microsphere preparation using Taguchi

Keywords:
Design of experimentPLGA microspheresminocycline hydrochloride

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Microsphere drug delivery systems offer controlled release.
  • Minocycline hydrochloride (MCH) is an antibiotic with potential for microsphere formulations.
  • Developing a robust MCH microsphere preparation method is crucial for consistent drug delivery.

Purpose of the Study:

  • To establish a robust preparation method for minocycline hydrochloride (MCH) microspheres.
  • To ensure consistent MCH microsphere production irrespective of the poly(D,L-lactide-co-glycolide) (PLGA) polymer type used.

Main Methods:

  • Taguchi's Robust Experimental Design methodology was utilized.
  • Seven controllable factors were optimized for MCH-loaded PLGA microspheres.
  • The solid-in-oil-in-water (S/O/W) method was compared against the co-solvent method.

Main Results:

  • The S/O/W method yielded significantly higher encapsulation efficiency (EE) and faster drug release compared to the co-solvent method.
  • Preparation method, aqueous phase pH, and volume were key factors influencing EE.
  • Confirmation experiments showed a 5.76 dB increase in signal-to-noise ratio, indicating successful optimization.

Conclusions:

  • Taguchi's method effectively optimized PLGA microsphere preparation for MCH.
  • The S/O/W method is superior for achieving high EE and rapid drug release.
  • Aqueous phase pH and volume are critical parameters for enhancing EE in MCH microspheres.