Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers.

Mutalik, Srinivas, Shetty, Pallavi K., Kumar, Aravind, Kalra, Rohit and Parekh, Harendra S. (2014) Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers.. Drug Delivery, 21 1: 44-54. doi:10.3109/10717544.2013.845861


Author Mutalik, Srinivas
Shetty, Pallavi K.
Kumar, Aravind
Kalra, Rohit
Parekh, Harendra S.
Title Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers.
Journal name Drug Delivery   Check publisher's open access policy
ISSN 1071-7544
1521-0464
Publication date 2014-02-17
Sub-type Article (original research)
DOI 10.3109/10717544.2013.845861
Open Access Status
Volume 21
Issue 1
Start page 44
End page 54
Total pages 11
Place of publication New York, NY, United States
Publisher Informa Healthcare
Collection year 2015
Language eng
Formatted abstract
Enhancing the deposition and permeation of 5-fluorouracil across human epidermis assisted by appropriately charged and well-defined peptide dendrimers was investigated. Peptide dendrimers with arginine as the terminal amino acid and having a range of terminal positive charges (4+, 8+ and 16+) were synthesized by solid phase peptide synthesis. Various parameters including effect of peptide dendrimers on the solubility and partition coefficient of 5-FU, degradation of drug in skin as well as deposition and permeation of 5-FU in/through skin were studied. All the tested dendrimers increased the aqueous solubility and partition coefficient of 5-FU with each also significantly (p < 0.05) enhancing the deposition and permeation of 5-FU in/across human epidermis in a concentration-dependent manner. Of the three peptide dendrimers examined, R8 dendrimer (bearing 8+ charge derived from four terminal arginines and MW of ≈1000 Da) showed greatest values for flux, Q48 (cumulative amount of drug permeated at the end of 48 h) and amount of drug retained in human skin. Furthermore, this study also scrutinized and reports on the likely mechanisms by which peptide dendrimers act as transdermal permeation enhancers.
Keyword 5-Fluorouracil
Human skin
Peptide dendrimers
Skin permeation
Transdermal
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2015 Collection
School of Pharmacy Publications
 
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Created: Tue, 28 Jan 2014, 19:46:52 EST by Harendra Parekh on behalf of School of Pharmacy