Production of monodisperse epigallocatechin gallate (EGCG) microparticles by spray drying for high antioxidant activity retention

Int J Pharm. 2011 Jul 15;413(1-2):155-66. doi: 10.1016/j.ijpharm.2011.04.056. Epub 2011 Apr 28.

Abstract

Epigallocatechin gallate (EGCG) originated from green tea is well-known for its pharmaceutical potential and antiproliferating effect on carcinoma cells. For drug delivery, EGCG in a micro-/nanoparticle form is desirable for their optimized chemopreventive effect. In this study, first time reports that EGCG microparticles produced by low temperature spray drying can maintain high antioxidant activity. A monodisperse droplet generation system was used to realize the production of EGCG microparticles. EGCG microparticles were obtained with narrow size distribution and diameter of 30.24 ± 1.88 μM and 43.39 ± 0.69 μM for pure EGCG and lactose-added EGCG, respectively. The EC50 value (the amount of EGCG necessary to scavenge 50% of free radical in the medium) of spray dried pure EGCG particles obtained from different temperature is in the range of 3.029-3.075 μM compared to untreated EGCG with EC50 value of 3.028 μM. Varying the drying temperatures from 70°C and 130°C showed little detrimental effect on EGCG antioxidant activity. NMR spectrum demonstrated the EGCG did not undergo chemical structural change after spray drying. The major protective mechanism was considered to be: (1) the use of low temperature and (2) the heat loss from water evaporation that kept the particle temperature at low level. With further drier optimization, this monodisperse spray drying technique can be used as an efficient and economic approach to produce EGCG micro-/nanoparticles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anticarcinogenic Agents / chemistry*
  • Anticarcinogenic Agents / metabolism
  • Anticarcinogenic Agents / pharmacology
  • Antioxidants / chemistry*
  • Antioxidants / metabolism
  • Antioxidants / pharmacology
  • Catechin / analogs & derivatives*
  • Catechin / chemistry
  • Catechin / metabolism
  • Catechin / pharmacology
  • Desiccation
  • Drug Compounding / methods*
  • Drug Delivery Systems*
  • Excipients / chemistry
  • Fluoresceins / metabolism
  • Free Radical Scavengers / metabolism
  • Hot Temperature
  • Hypromellose Derivatives
  • Lactose / chemistry
  • Methylcellulose / analogs & derivatives
  • Nanoparticles / chemistry
  • Particle Size
  • Pharmaceutical Solutions
  • Powders

Substances

  • Anticarcinogenic Agents
  • Antioxidants
  • Excipients
  • Fluoresceins
  • Free Radical Scavengers
  • Pharmaceutical Solutions
  • Powders
  • diacetyldichlorofluorescein
  • Hypromellose Derivatives
  • Catechin
  • Methylcellulose
  • epigallocatechin gallate
  • Lactose