title: PP072. Development of polyphenols-containing nanoparticles for the treatment of vaginal inflammation.
abstract: BACKGROUND
  Vaginal inflammation during pregnancy is linked to miscarriage, preterm labour, placental dysfunction and perinatal complications. Despite the availability of several anti-inflammatory drugs, there is no general consensus regarding safe formulation especially for use in early pregnancy. On the other hand, polyphenols especially "curcumin" from Turmeric (powdered rhizome of Curcuma longa) and "catechins" from green tea have been traditionally used and widely discussed (>16,000 citations for curcumin and >24,000 for catechin in SciFinder) as pharmacologically active anti-inflammatory components and considered as safe. However, due to their poor solubility, low bioavailability and stability, their clinical application remains to be limited.
  
  
  OBJECTIVE
  Our aim was to develop a non-teratogenic and non-toxic polyphenol-bearing nanoparticles which can be safely used in early pregnancy for the treatment of vaginal inflammation.
  
  
  METHODS
  Vesicle-based liposomal formulations for polyphenols (curcumins and catechins) were developed and standardized. Liposomal curcumins and catechins were characterized in respect to their stability, size and entrapment efficiency. Antioxidant activities were evaluated by DPPH/ABTS+/O2.- and SOD activities. Anti-inflammatory activities were evaluated by measuring LPS-induced NO and pro-inflammatory cytokines such as IL-1B and TNF-A in macrophages (J774.1) and LPG-induced cytokines IL-8 in human vaginal cells lines (End1/E6E7, Ect1/E6E7, VK2/E6E7). Antioxidant and anti-inflammatory activities of curcumin/catechin and their corresponding vesicle-based formulation were compared.
  
  
  RESULTS
  Phospholipid-based nanoparticles (approx. 200 nm) were found to be stable and incorporating high amount of curcumins or catechins. Liposomal curcumin was found to be 2- to 6-folds more potent than curcumin in inhibiting NO production and pro-inflammatory cytokines in macrophages. IL-8 was inhibited up to 67% by the liposomal curcumin in human vaginal cell lines (End1/E6E7, Ect1/E6E7, VK2/E6E7) as compared to curcumin. However, similar vesicle formulations of catechins were not significantly superior to non-vesicle formulations of catechins.
  
  
  CONCLUSIONS
  Standardized liposomal curcuminoids have potential as an effective and safe topical formulation for the treatment of vaginal inflammation in early pregnancy.
authors.forename: Purusotam
authors.initials: P
authors.lastname: Basnet
authors.forename: Natasa
authors.initials: N
authors.lastname: Skalko-Basnet
authors.forename: Martha Agnes
authors.initials: MA
authors.lastname: Hentemann
authors.forename: Ganesh
authors.initials: G
authors.lastname: Acharya