Document Detail

Drug Release and Skin Penetration from Solid Lipid Nanoparticles and a Base Cream: A Systematic Approach from a Comparison of Three Glucocorticoids.
MedLine Citation:
PMID:  21346400     Owner:  NLM     Status:  Publisher    
Solid lipid nanoparticles (SLNs) can enhance drug penetration into the skin, yet the mechanism of the improved transport is not known in full. To unravel the influence of the drug-particle interaction on penetration enhancement, 3 glucocorticoids (GCs), prednisolone (PD), the diester prednicarbate (PC) and the monoester betamethasone 17-valerate (BMV), varying in structure and lipophilicity, were loaded onto SLNs. Theoretical permeability coefficients (cm/s) of the agents rank BMV (-6.38) ≥ PC (-6.57) > PD (-7.30). GC-particle interaction, drug release and skin penetration were investigated including a conventional oil-in-water cream for reference. Both with SLN and cream, PD release was clearly superior to PC release which exceeded BMV release. With the cream, the rank order did not change when studying skin penetration, and skin penetration is thus predominantly influenced by drug release. Yet, the penetration profile for the GCs loaded onto SLNs completely changed, and differences between the steroids were almost lost. Thus, SLNs influence skin penetration by an intrinsic mechanism linked to a specific interaction of the drug-carrier complex and the skin surface, which becomes possible by the lipid nature and nanosize of the carrier and appears not to be derived by testing drug release. Interestingly, PC and PD uptake from SLN even resulted in epidermal targeting. Thus, SLNs are not only able to improve skin penetration of topically applied drugs, but may also be of particular interest when specifically aiming to influence epidermal dysfunction.
P Schlupp; T Blaschke; K D Kramer; H-D Höltje; W Mehnert; M Schäfer-Korting
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-2-24
Journal Detail:
Title:  Skin pharmacology and physiology     Volume:  24     ISSN:  1660-5535     ISO Abbreviation:  -     Publication Date:  2011 Feb 
Date Detail:
Created Date:  2011-2-24     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101188418     Medline TA:  Skin Pharmacol Physiol     Country:  -    
Other Details:
Languages:  ENG     Pagination:  199-209     Citation Subset:  -    
Copyright Information:
Copyright © 2011 S. Karger AG, Basel.
Institut für Pharmazie, Freie Universität Berlin, Berlin, Deutschland.
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