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Sustained release biodegradable solid lipid microparticles: Formulation, evaluation and statistical optimization by

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Solid lipid microparticles (SLMs) were developed for nebivolol delivery using carnauba wax and glyceryl monostearate. Optimized SLMs demonstrated good stability and drug release, potentially enhancing nebivolol oral bioavailability.

Keywords:
carnauba waxcentral composite designdifferential scanning calorimetrymicroencapsulationnebivololsolid lipid microparticles

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Area of Science:

  • Pharmaceutical Technology
  • Materials Science

Background:

  • Nebivolol is a beta-blocker used for hypertension.
  • Improving nebivolol's oral bioavailability is crucial for effective treatment.

Purpose of the Study:

  • To develop and optimize nebivolol-loaded solid lipid microparticles (SLMs).
  • To investigate the impact of formulation variables on SLM characteristics and drug release.

Main Methods:

  • Solvent evaporation microencapsulation using carnauba wax and glyceryl monostearate.
  • Central composite design for optimization of yield, entrapment efficiency, and drug release.
  • Characterization using FTIR, DSC, XRD, and zeta potential measurements.

Main Results:

  • Spherical SLMs (10-40 μm) with good rheology and smooth surfaces were produced.
  • Formulation components showed compatibility; zeta potential confirmed stability (-20 to -40 mV).
  • Yield (29-86%), entrapment efficiency (45-83%), and drug release (49-86%) were optimized.
  • Drug release was influenced by lipid concentration and followed Higuchi/zero-order models with diffusion/erosion mechanisms.

Conclusions:

  • Optimized SLMs offer a promising platform for nebivolol delivery.
  • The developed SLMs have the potential to enhance nebivolol oral bioavailability.