Preparation and release pattern study of long-term controlled release Blonanserin microspheres

Int J Pharm. 2024 Dec 5:666:124756. doi: 10.1016/j.ijpharm.2024.124756. Epub 2024 Sep 27.

Abstract

To prepare a PLGA microsphere loaded with the antipsychotic Blonanserin without release leg period and released in a near-zero model for long time, in this study, 15 kDa and 75 kDa PLGA were chosen to be mixed with different ratios, and Blonanserin microspheres (Bn-MS) without significant differences in the particle size, drug loading capacity, and encapsulation rate were prepared by microfluidics. The release kinetic model was fitted to the release behavior by monitoring the changes in particle size and morphology during the Bn-MS release to investigate microspheres' in vitro release pattern. The results showed that the addition of appropriate ratios of mixed molecular weights to Bn-MS could eliminate the release hysteresis period. When the ratio of 15 kDa and 75 kDa was 1:9 (F3), the Bn-MS had a low burst release rate, moderate release rate, no release hysteresis period, a long release period of up to 35 days, and a stable release pattern close to the zero level. The results of the release mechanism study indicated that the hybrid PLGA improved the release behavior of the microspheres by adjusting the dissolution degradation rate of Bn-MS, which in turn affected the release mechanism of the microspheres.

Keywords: Blonanserin; Lag time; Microfluidic technology; Microspheres; PLGA blends; Schizophrenic.

MeSH terms

  • Antipsychotic Agents / administration & dosage
  • Antipsychotic Agents / chemistry
  • Antipsychotic Agents / pharmacokinetics
  • Delayed-Action Preparations* / chemistry
  • Drug Carriers / chemistry
  • Drug Compounding / methods
  • Drug Liberation*
  • Lactic Acid* / chemistry
  • Microspheres*
  • Molecular Weight
  • Particle Size*
  • Piperazines* / administration & dosage
  • Piperazines* / chemistry
  • Piperazines* / pharmacokinetics
  • Piperidines* / administration & dosage
  • Piperidines* / chemistry
  • Polyglycolic Acid / chemistry
  • Polylactic Acid-Polyglycolic Acid Copolymer* / chemistry

Substances

  • Delayed-Action Preparations
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • blonanserin
  • Piperidines
  • Piperazines
  • Lactic Acid
  • Antipsychotic Agents
  • Polyglycolic Acid
  • Drug Carriers