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Improving topical non-melanoma skin cancer treatment: In vitro efficacy of a novel guanosine-analog phosphonate.

Abstract
Actinic keratosis, a frequent carcinoma in situ of non-melanoma skin cancer (NMSC), can transform into life-threatening cutaneous squamous cell carcinoma. Current treatment is limited due to low complete clearance rates and asks for novel therapeutic concepts; the novel purine nucleotide analogue OxBu may be an option. In order to enhance skin penetration, solid lipid nanoparticles (SLN, 136-156 nm) were produced with an OxBu entrapment efficiency of 96.5 ± 0.1%. For improved preclinical evaluation, we combined tissue engineering with clinically used keratin-18 quantification. Three doses of 10(-3) mol/l OxBu, dissolved in phosphate-buffered saline as well as loaded to SLN, were effective on reconstructed NMSC. Tumour response and apoptosis induction were evaluated by an increase in caspase-cleaved fragment of keratin-18, caspase-7 activation as well as by reduced expression of matrix metallopeptidase-2 and Ki-67. OxBu efficacy was superior to equimolar 5-fluorouracil solution, and thus the drug should be subjected to the next step in preclinical evaluation.
AuthorsC Ali-von Laue, C Zoschke, N Do, D Lehnen, S Küchler, W Mehnert, T Blaschke, K D Kramer, J Plendl, G Weindl, H C Korting, D Hoeller Obrigkeit, H-F Merk, M Schäfer-Korting
JournalSkin pharmacology and physiology (Skin Pharmacol Physiol) Vol. 27 Issue 4 Pg. 173 ( 2014) ISSN: 1660-5535 [Electronic] Switzerland
PMID24503861 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Organophosphonates
  • Guanosine
Topics
  • Administration, Topical
  • Animals
  • Drug Delivery Systems
  • Guanosine (analogs & derivatives)
  • Humans
  • Nanoparticles (administration & dosage)
  • Organophosphonates (administration & dosage)
  • Skin Neoplasms (drug therapy)
  • Tissue Engineering

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