Development of metformin hydrochloride loaded dissolving tablets with novel carboxymethylcellulose/poly-l-lysine/TPP complex

Int J Biol Macromol. 2020 Jul 15:155:411-420. doi: 10.1016/j.ijbiomac.2020.03.191. Epub 2020 Mar 26.

Abstract

Natural polymers like polysaccharides, polypeptides and their derivatives are broadly applied in drug delivery due to excellent biocompatibility and biodegradability. In this study, the dissolving tablets, formed with carboxymethylcellulose/poly-l-lysine/tripolyphosphate (CMC/PLL/TPP) complex, were prepared using metformin hydrochloride (MetHCl) as model drug. Confocal laser scanning microscopy observation manifested that FITC-labeled PLL interacted with CMC and formed a uniform interior microstructure. Scanning electron microscope images showed the drug-loaded tablets had well-formed shapes with smooth surfaces. MetHCl embedded interior the microstructures of the tablets and represented in a crystal form. Thermo-gravimetric analysis and differential scanning calorimetry indicated that the drug-loaded tablets had stable thermal properties with less moisture content (3.52%). Fourier transform infrared spectrometer confirmed that the CMC/PLL/TPP complex was fabricated via the electrostatic interactions between -NH3+, -COO- and -[P2O54-]- groups. The drug-loaded tablets had a high drug loading efficiency of 85.76% and drug encapsulation efficiency of 81.47%, and a shorter wetting time of 2.16 min in SSF (pH 6.8) and lower swelling ratio of 233.34%. The drug loaded in the samples could be released completely within 10 min in simulated saliva fluid (SSF pH 6.8), indicating a rapid drug release and dissolving profile in the environment, which could be developed for dissolving tablets.

Keywords: Dissolving tablets; Sodium carboxymethylcellulose; ε-Poly-l-lysine.

MeSH terms

  • Carboxymethylcellulose Sodium / chemistry*
  • Delayed-Action Preparations
  • Drug Liberation
  • Humans
  • Hypoglycemic Agents / chemistry*
  • Hypoglycemic Agents / metabolism
  • Metformin / chemistry*
  • Metformin / metabolism
  • Polylysine / chemistry*
  • Polymers / chemistry*
  • Polyphosphates / chemistry*
  • Solubility
  • Tablets / chemistry

Substances

  • Delayed-Action Preparations
  • Hypoglycemic Agents
  • Polymers
  • Polyphosphates
  • Tablets
  • Polylysine
  • Metformin
  • Carboxymethylcellulose Sodium
  • triphosphoric acid