Local delivery system of doxycycline hyclate based on ε-caprolactone copolymers for periodontitis treatment

Int J Pharm. 2015 Aug 1;491(1-2):335-44. doi: 10.1016/j.ijpharm.2015.06.034. Epub 2015 Jul 2.

Abstract

The aim of the study was to evaluate kinetics of doxycycline hyclate release from polymeric bioresorbable implants and to examine suitability of this system for local treatment of periodontitis. Selected trimethylene carbonate/ϵ-caprolactone (TMC/CL) and glycolide/caprolactone (GL/CL) copolymers were synthesized and used as carriers in the form of small elastic rings with 5 wt% and 10 wt% doxycycline hyclate content, or in the form of flakes obtained through electro-spinning technique. The release of the drug under in vitro conditions has been tested. The study has shown that equimolar TMC/CL copolymer loaded with 10 wt% of doxycycline hyclate appears to be the most suitable copolymer for assumed system. The drug release proceeds mainly by diffusion of medium into the polymeric matrix and then the drug is washed out. Daily validation of doxycycline doses released by the system should ensure accurate course of the therapy.

Keywords: 1,3-Trimethylene carbonate (PubChem CID: 123834); Biodegradable copolyester; Controlled drug release; Diethylzinc (PubChem CID: 11185); Doxycycline; Doxycycline hyclate (PubChem CID: 54705095); Glycolide (PubChem CID: 65432); Periodontitis treatment; Zirconium (IV) acetylacetonate (PubChem CID: 5463922); ϵ-Caprolactone (PubChem CID: 10401).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / therapeutic use*
  • Anti-Infective Agents, Local / administration & dosage*
  • Anti-Infective Agents, Local / therapeutic use*
  • Caproates
  • Delayed-Action Preparations
  • Dioxanes
  • Doxycycline / administration & dosage*
  • Doxycycline / therapeutic use*
  • Drug Carriers
  • Drug Delivery Systems
  • Drug Design
  • Drug Implants
  • Lactones
  • Molecular Weight
  • Periodontitis / drug therapy*
  • Periodontitis / microbiology
  • Water / chemistry

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents, Local
  • Caproates
  • Delayed-Action Preparations
  • Dioxanes
  • Drug Carriers
  • Drug Implants
  • Lactones
  • Water
  • trimethylene carbonate
  • caprolactone
  • Doxycycline