Screening of drug-sericin solid dispersions for improved solubility and dissolution

Int J Biol Macromol. 2018 Feb;107(Pt B):1683-1691. doi: 10.1016/j.ijbiomac.2017.10.035. Epub 2017 Oct 10.

Abstract

The aim of present attempt deals with preparation of binary dispersion of sericin, waste of sericulture industry in order to enhance solubility and dissolution of poorly soluble drugs. Solid dispersions (SDs) of BCS-II drugs were prepared by spray drying, solvent evaporation, ball milling and physical mixing in ratio of drug:sericin (1:0.5, 1:1, 1:1.5, 1:2, 1:2.5 and 1:3). Further, SDs were investigated by solubility, ATR-FTIR, XRD, DSC, micromeritics and tablettability, surface morphology and in-vitro dissolution. Results demonstrated that, sericin improves solubility of drugs by 8-10 fold. The ATR-FTIR showed the slight shifting/broadening of principle peaks corresponding to NH and OH. Spray dried (1:2w/w) SDs showed maximum reduction in crystallinity of drugs indicating drug was molecularly distributed and was in amorphous state. Spray dried SDs of meloxicam showed better compressibility and compactibility. The microphotograph of spray dried SDs of lornoxicam and meloxicam showed bowl shaped and blend of bowl and spherical particles respectively, while spray dried SDs of felodepine showed spherical shape. The spray dried SDs (1:2w/w) displayed better dissolution performance than other methods Conclusively, sericin offers a hydrophilic matrix to deliver poor water soluble drugs and its aerodynamic shape may show a great potential for various drug deliveries.

Keywords: Binary dispersion; Dissolution enhancement; Poorly soluble drugs; Silk sericin; Solubility improvement.

MeSH terms

  • Calorimetry, Differential Scanning
  • Pharmaceutical Preparations / chemistry*
  • Sericins / chemistry*
  • Solubility
  • Solutions
  • Spectroscopy, Fourier Transform Infrared
  • Tablets
  • Thermodynamics
  • Water / chemistry
  • X-Ray Diffraction

Substances

  • Pharmaceutical Preparations
  • Sericins
  • Solutions
  • Tablets
  • Water