PMID- 19833178 OWN - NLM STAT- MEDLINE DCOM- 20100927 LR - 20220409 IS - 1873-3476 (Electronic) IS - 0378-5173 (Linking) VI - 390 IP - 1 DP - 2010 May 5 TI - The evidence for solid lipid nanoparticles mediated cell uptake of resveratrol. PG - 61-9 LID - 10.1016/j.ijpharm.2009.10.011 [doi] AB - The potential for colloidal carriers to increase drug bioavailability has spurred a renewed interest in their uptake mechanisms and movement within cells. Solid lipid nanoparticles (SLN) were used as a carrier for a promising chemopreventive drug, resveratrol (RSV). The effects of SLN, empty or loaded with RSV (SLN-RSV), on the internalization, growth, morphology, metabolic activity and genetic material of keratinocytes were compared to those of RSV in solution. Fluorescence images clearly showed that SLN with a size below 180 nm move promptly through the cell membrane, distribute throughout the cytosol, move successively among different cellular levels and localize in the perinuclear region without inducing cytotoxicity. RSV solubility, stability and intracellular delivery were all increased by loading into SLN. The release profile of RSV showed a biphasic pattern, reflecting its distribution in SLN. RSV in solution was slightly cytotoxic. That was prevented by loading it into solid lipid nanoparticles, which preserved cell morphology. The cytostatic effect of SLN-RSV was much more expressed than that of RSV in solution. Delivery of RSV by SLN contributes to effectiveness of RSV on decreasing cell proliferation, with potential benefits for prevention of skin cancer. CI - Copyright 2009 Elsevier B.V. All rights reserved. FAU - Teskac, K AU - Teskac K AD - University of Ljubljana, Faculty of Pharmacy, Askerceva 7, Ljubljana, Slovenia. FAU - Kristl, J AU - Kristl J LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20091013 PL - Netherlands TA - Int J Pharm JT - International journal of pharmaceutics JID - 7804127 RN - 0 (Anticarcinogenic Agents) RN - 0 (Delayed-Action Preparations) RN - 0 (Drug Carriers) RN - 0 (Lecithins) RN - 0 (Lipids) RN - 0 (Stilbenes) RN - 106392-12-5 (Poloxamer) RN - Q369O8926L (Resveratrol) SB - IM MH - Anticarcinogenic Agents/administration & dosage/metabolism/pharmacokinetics/pharmacology MH - Biological Availability MH - Cell Cycle/drug effects MH - Cell Line, Transformed MH - Cell Nucleus/drug effects MH - Cell Proliferation/drug effects MH - Cell Shape/drug effects MH - Cell Size/drug effects MH - Delayed-Action Preparations/chemistry/metabolism/pharmacology MH - Drug Carriers/chemistry/*metabolism/pharmacology MH - Humans MH - Hydrophobic and Hydrophilic Interactions MH - Intracellular Space/metabolism MH - Keratinocytes/cytology/drug effects/*metabolism MH - Lecithins/chemistry MH - Lipids/*chemistry MH - Metabolism/drug effects MH - Microscopy, Fluorescence MH - Nanoparticles/*chemistry MH - Necrosis/chemically induced MH - Particle Size MH - Poloxamer/chemistry MH - Resveratrol MH - Static Electricity MH - Stilbenes/*administration & dosage/*metabolism/pharmacokinetics/pharmacology EDAT- 2009/10/17 06:00 MHDA- 2010/09/29 06:00 CRDT- 2009/10/17 06:00 PHST- 2009/02/18 00:00 [received] PHST- 2009/09/18 00:00 [revised] PHST- 2009/10/03 00:00 [accepted] PHST- 2009/10/17 06:00 [entrez] PHST- 2009/10/17 06:00 [pubmed] PHST- 2010/09/29 06:00 [medline] AID - S0378-5173(09)00720-0 [pii] AID - 10.1016/j.ijpharm.2009.10.011 [doi] PST - ppublish SO - Int J Pharm. 2010 May 5;390(1):61-9. doi: 10.1016/j.ijpharm.2009.10.011. Epub 2009 Oct 13.