Polymer-Lipid Microparticles for Pulmonary Delivery

Langmuir. 2018 Mar 20;34(11):3438-3448. doi: 10.1021/acs.langmuir.7b03645. Epub 2018 Mar 9.

Abstract

Toward engineering approaches that are designed to optimize the particle size, morphology, and mucoadhesion behavior of the particulate component of inhaler formulations, this paper presents the preparation, physicochemical characterization, and preliminary in vitro evaluation of multicomponent polymer-lipid systems that are based on "spray-drying engineered" α-lactose monohydrate microparticles. The formulations combine an active (budesonide) with a lung surfactant (dipalmitoylphosphatidylcholine) and with materials that are known for their desirable effects on morphology (polyvinyl alcohol), aerosolization (l-leucine), and mucoadhesion (chitosan). The effect of the composition of formulations on the morphology, distribution, and in vitro mucoadhesion profiles is presented along with "Calu-3 cell monolayers" data that indicate good cytocompatibility and also with simulated-lung-fluid data that are consistent with the therapeutically useful release of budesonide.

MeSH terms

  • 1,2-Dipalmitoylphosphatidylcholine / chemistry
  • 1,2-Dipalmitoylphosphatidylcholine / toxicity
  • Administration, Inhalation
  • Budesonide / chemistry*
  • Cell Line, Tumor
  • Chitosan / chemistry
  • Chitosan / toxicity
  • Drug Carriers / chemistry*
  • Drug Carriers / toxicity
  • Drug Compounding
  • Drug Liberation
  • Excipients / chemistry*
  • Excipients / toxicity
  • Female
  • Humans
  • Lactose / chemistry*
  • Lactose / toxicity
  • Leucine / chemistry
  • Leucine / toxicity
  • Male
  • Mucus / chemistry
  • Particle Size
  • Polyvinyl Alcohol / chemistry*
  • Polyvinyl Alcohol / toxicity
  • Pulmonary Surfactants / chemistry
  • Pulmonary Surfactants / toxicity

Substances

  • Drug Carriers
  • Excipients
  • Pulmonary Surfactants
  • 1,2-Dipalmitoylphosphatidylcholine
  • Budesonide
  • Polyvinyl Alcohol
  • Chitosan
  • Leucine
  • Lactose