Sugar coated ceramic nanocarriers for the oral delivery of hydrophobic drugs: formulation, optimization and evaluation

Drug Dev Ind Pharm. 2012 May;38(5):577-86. doi: 10.3109/03639045.2011.617884. Epub 2011 Sep 30.

Abstract

In order to enhance the delivery of poorly-soluble drugs, we have explored aquasomes (three-layered, ceramic core based, oligosaccharide coated nanoparticles) as potential carriers for the delivery of model hydrophobic drug piroxicam (log P = 3.1). Ceramic nanoparticles were prepared using two techniques; namely, co-precipitation by refluxing and co-precipitation by sonication. Core preparation was finally done using sonication approach; based on the higher % yield (42.4 ± 0.4%) and shorter duration (1 day) compared to the reflux method (27.4 ± 2.05%, 6 days). Lactose loading onto ceramic core was achieved using adsorption. Colorimetric analysis of lactose coating was done using Anthrone method. Optimization of process variables namely, incubation time and core to coat ratio (for sugar loading) was carried out. Optimum time of incubation was 3 h and the core to coat ratio was 4:1. The drug loading was achieved by incubating the sugar loaded cores in different concentrations of piroxicam solution and it was found that 1.5% w/v piroxicam was optimal. Structural characterization using Fourier-Transform Infra Red Spectroscopy (FTIR) confirmed the presence of sugar coating onto the core. Morphological evaluation using transmission electron microscopy (TEM) revealed spherical nanoparticles (size 56.56 ± 5.93 nm for lactose coated core and 184.75 ± 13.78 nm for piroxicam loaded aquasomes) confirming the nanometric dimensions.

MeSH terms

  • Analysis of Variance
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Biocompatible Materials / chemistry
  • Biological Availability
  • Ceramics / chemistry
  • Drug Delivery Systems
  • Durapatite / chemistry*
  • Excipients / chemistry
  • Hydrophobic and Hydrophilic Interactions
  • Lactose / chemistry*
  • Nanoparticles / chemistry*
  • Particle Size
  • Piroxicam / chemistry*
  • Solubility
  • Sweetening Agents / chemistry

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Biocompatible Materials
  • Excipients
  • Sweetening Agents
  • Piroxicam
  • Durapatite
  • Lactose