Site-specific delivery of polymeric encapsulated microorganisms: a patent evaluation of US20170165201A1

Expert Opin Ther Pat. 2018 Sep;28(9):703-708. doi: 10.1080/13543776.2018.1516752. Epub 2018 Sep 6.

Abstract

Probiotics inculde live microorganisms therapeutically effective in the treatment of wide range of diseases. Probiotics possibly stimulates the growth of preferred microorganisms, crowds out potentially harmful microorganisms, and reinforces the body's natural defense mechanisms. Microencapsulation of probiotic microorganisms protects them from the destructive environment and prolongs their survival. Use of mucoadhesive and pH responsive polymers could impart extended retention, pH sensitive release and mucoadhesive properties to the system. The probiotic formulations could be used for therapeutic, diagnostic, and prophylactic purposes. Areas covered: Layer-by-layer techology was developed for encapsulating Bacillus coagulans employing chitosan and alginate as mucoadhesive polymers (for attachment to the gastrointestinal mucosa) and Eudragit EPO and Eudragit L100 as pH responsive polymers (for site-specific delivery). The formulation was evaluated for layer stability, mucoadhesion capability, protection of microorganisms from biological insults, pH responsive layer removal, in vitro evaluation in three-dimensional intestinal tissue model, probiotic bacterial delivery. Expert opinion: In this patent, a unique layer-by-layer assembly of two differently charged polymers (mucoadhesive and pH repsonsive) was achieved for encapsulating the probiotic microorganism. For assessing the clinical applicability of the invention, further studies may be needed since the conclusions are drawn solely based on in vitro data.

Keywords: Probiotics; layer-by-layer; microrganisms; mucoadhesive polymer; pH responsive polymer.

MeSH terms

  • Adhesiveness
  • Alginates / chemistry
  • Animals
  • Chitosan / chemistry
  • Drug Delivery Systems*
  • Gastrointestinal Tract / metabolism
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Humans
  • Hydrogen-Ion Concentration
  • Patents as Topic
  • Polymers / chemistry*
  • Polymethacrylic Acids / chemistry
  • Probiotics / administration & dosage*

Substances

  • Alginates
  • Hexuronic Acids
  • Polymers
  • Polymethacrylic Acids
  • methylmethacrylate-methacrylic acid copolymer
  • Glucuronic Acid
  • Chitosan
  • Eudragit E PO