Protein transduction domain-containing microemulsions as cutaneous delivery systems for an anticancer agent.
Loading...
Issue Date
2013-05
Authors
Pepe, Dominique*
McCall, Melissa*
Zheng, HaiAn
Lopes, Luciana B
Degree
Advisor
Committee Members
Journal Title
Journal ISSN
Volume Title
Abstract
In this study, we developed cationic microemulsions containing a protein transduction domain (penetratin) for optimizing paclitaxel localization within the skin. Microemulsions were prepared by mixing a surfactant blend (BRIJ:ethanol:propylene glycol 2:1:1, w/w/w) with monocaprylin (oil phase) at 1.3:1 ratio, and adding water at 30% (ME-30), 43% (ME-43), and 50% (ME-50). Electrical conductivity and viscosity measurements indicated that ME-30 is most likely a bicontinuous system, whereas ME-43 and ME-50 are water continuous. Their irritation potential, studied in bioengineered skin equivalents, decreased as aqueous content increased. Because ME-50 was not stable in the presence of paclitaxel (0.5%), ME-43 was selected for penetratin incorporation (0.4%). The microemulsion containing penetratin (ME-P) displayed zeta potential of +5.2 mV, and promoted a 1.8-fold increase in paclitaxel cutaneous (but not transdermal) delivery compared with the plain ME-43, whereas the enhancement promoted by another cationic microemulsion containing phytosphingosine was 1.3-fold. Compared with myvacet oil, ME-P promoted a larger increase on transepidermal water loss (twofold) than the plain or the phytosphingosine-containing microemulsions (1.5-fold), suggesting that penetratin addition increases the barrier-disrupting and penetration-enhancing effects of microemulsions. The ratio Δcutaneous/Δtransdermal delivery promoted by ME-P was the highest among the formulations, suggesting its potential for drug localization within cutaneous tumor lesions.
Citation
Pepe D, McCall M, Zheng H, Lopes LB. Protein transduction domain-containing microemulsions as cutaneous delivery systems for an anticancer agent. J Pharm Sci. 2013 May;102(5):1476-87. doi: 10.1002/jps.23482. Epub 2013 Feb 21. PMID: 23436680.
ACPHS Research Commons URI
Description
Click on the Resource Link to access the article (may not be free).