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AAPS PharmSci

, Volume 5, Issue 4, pp 1–12 | Cite as

Amphiphilic star-like macromolecules as novel carriers for topical delivery of nonsteroidal anti-inflammatory drugs

  • Jelena Djordjevic
  • Bozena Michniak
  • Kathryn E. UhrichEmail author
Article

Abstract

The objective of this study was to evaluate amphiphilic star-like macromolecules (ASMs) as a topical drug delivery system. Indomethacin, piroxicam, and ketoprofen were individually encapsulated into the ASMs using coprecipitation. The effects of the ASMs on percutaneous permeation of nonsteroidal anti-inflammatory drugs (NSAIDs) across full thickness, hairless mouse skin were evaluated in vitro using modified Franz diffusion cells. In addition, solubility and in vitro release experiments were performed to characterize ASMs behavior in aqueous media. Poly(ethylene glycol) (PEG) and Pluronic P-85 were used as polymer controls to compare the role of PEG and amphiphilic behavior in the ASMs. In vitro release experiments indicated that ASMs can delay drug release (P⋖05), whereas solubility measurements showed that ASMs can increase NSAIDs aqueous solubility (P⋖05). Percutaneous permeation studies revealed that ASMs decreased both flux and Q24 of drugs compared with the control (P⋖10). Skin pretreatment studies with ASM-containing solution before drug application demonstrated that pretreatment similarly influenced NSAID percutaneous permeation. In conclusion, ASMs likely slow drug permeation through 2 mechanisms, delayed drug diffusion from its core and skin dehydration by its shell. Thus, ASMs may be useful for delayed dermal delivery or prevention of compound permeation through the skin (eg, sunscreens, N,N-diethyl-m-toluamide [DEET]) from aqueous formulations.

Keywords

topical drug delivery NSAIDs polymeric micelle permeation drug release 

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Copyright information

© American Association of Pharmaceutical Scientists 2003

Authors and Affiliations

  • Jelena Djordjevic
    • 1
    • 2
  • Bozena Michniak
    • 3
  • Kathryn E. Uhrich
    • 1
    Email author
  1. 1.Department of Chemistry and Chemical BiologyRutgers UniversityPiscataway
  2. 2.Department of Pharmaceutics, Ernest Mario School of PharmacyRutgers UniversityPiscataway
  3. 3.Department of Pharmacology and PhysiologyUMDNJ-New Jersey Medical SchoolNewark

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