Fast releasing oral electrospun PVP/CD nanofiber mats of taste-masked meloxicam

Int J Pharm. 2015 Jun 20;487(1-2):213-22. doi: 10.1016/j.ijpharm.2015.04.044. Epub 2015 Apr 18.

Abstract

Fast release and taste masking of meloxicam (MX)-loaded polyvinylpyrrolidone (PVP)/cyclodextrin (CD) nanofiber mats were developed using an electrospinning process. CDs were blended to improve the stability of the mats. The morphology and diameter of the mats were determined using scanning electron microscopy (SEM); physical and mechanical properties were also studied. The MX content, disintegration time, MX release and cytotoxicity of the mats were investigated. In vivo studies were also performed in healthy human volunteers. The results indicated that the mats were successfully prepared with fiber in the nanometer range. MX was well incorporated into the mats, with an amorphous form. The mats showed suitable tensile strength. CDs improved the physical stability by their cage-like supramolecular structure to protect from humidity and moisture, and create bead free nanofiber mats. The nanofiber mats with CDs were physically stable without any hygroscopicity and fusion. A fast disintegration and release of MX was achieved. Moreover, this mat released MX faster than the MX powder and commercial tablets. The cytotoxicity test revealed that mats were safe for a 5-min incubation. The disintegration studies indicated that in vivo disintegration agreed with the in vitro studies; the mat rapidly disintegrated in the mouth. The less bitter of MX was occurred in the mats that incorporated CD, menthol and aspartame. In addition, this mat was physical stable for 6 months. The results suggest that these mats may be a good candidate for fast dissolving drug delivery systems of bitter drugs to increase the palatability of dosage forms.

Keywords: Cyclodextrin; Electrospinning; Meloxicam; Nanofiber mats; Taste masking.

MeSH terms

  • Administration, Oral
  • Adult
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage*
  • Cell Line
  • Cell Survival / drug effects
  • Cyclodextrins / chemistry*
  • Drug Delivery Systems
  • Drug Stability
  • Female
  • Humans
  • Male
  • Meloxicam
  • Nanofibers*
  • Povidone / chemistry*
  • Solubility
  • Taste / drug effects*
  • Thiazines / administration & dosage*
  • Thiazines / toxicity
  • Thiazoles / administration & dosage*
  • Thiazoles / toxicity
  • Young Adult

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclodextrins
  • Thiazines
  • Thiazoles
  • Povidone
  • Meloxicam