Targeting of efavirenz loaded tuftsin conjugated poly(propyleneimine) dendrimers to HIV infected macrophages in vitro

Dutta, Tathagata, Garg, Minakshi, Jain, Narendra K., Dubey, Vaibhav, Mishra, Dinesh, Singh, Kanhaiya, Pandita, Deepti, Singh, Ajeet K., Ravi, Alok K. and Velpandian, Thirumurthy (2008) Targeting of efavirenz loaded tuftsin conjugated poly(propyleneimine) dendrimers to HIV infected macrophages in vitro. European Journal of Pharmaceutical Sciences, 34 2-3: 181-189. doi:10.1016/j.ejps.2008.04.002


Author Dutta, Tathagata
Garg, Minakshi
Jain, Narendra K.
Dubey, Vaibhav
Mishra, Dinesh
Singh, Kanhaiya
Pandita, Deepti
Singh, Ajeet K.
Ravi, Alok K.
Velpandian, Thirumurthy
Title Targeting of efavirenz loaded tuftsin conjugated poly(propyleneimine) dendrimers to HIV infected macrophages in vitro
Journal name European Journal of Pharmaceutical Sciences   Check publisher's open access policy
ISSN 0928-0987
1879-0720
Publication date 2008-07-03
Sub-type Article (original research)
DOI 10.1016/j.ejps.2008.04.002
Open Access Status Not yet assessed
Volume 34
Issue 2-3
Start page 181
End page 189
Total pages 9
Editor A. Urtti
Place of publication Amsterdam, Netherlands
Publisher Elsevier BV
Language eng
Subject C1
860899 Human Pharmaceutical Products not elsewhere classified
111599 Pharmacology and Pharmaceutical Sciences not elsewhere classified
Abstract HIV infected macrophages are considered as reservoirs for spreading the virus in AIDS patients. Tuftsin not only binds specifically to the mononuclear phagocytic cells but also enhances their natural killer activity. The purpose of this study is to explore the targeting potential and anti-HIV activity of efavirenz (EFV) loaded, tuftsin conjugated 5th generation poly(propyleneimine) dendrimers (TuPPI) in vitro. Tuftsin was chemically conjugated to 5th generation poly(propyleneimine) dendrimers (PPI). The entrapment efficiency of PPI and TuPPI were found to be 37.43 ± 0.3% and 49.31 ± 0.33%, respectively. TuPPI was found to slow down and prolong the in vitro release of EFV upto 144 h against PPI, which releases the drug completely within 24 h. TuPPI possessed negligible cytotoxicity as compared to that of PPI. The cellular uptake of TuPPI was found to be 34.5 times higher than that of the free drug in first 1 h and was significantly higher in HIV infected macrophages than that of uninfected cells. TuPPI was found to reduce the viral load by 99% at a concentration of 0.625 ng/ml, which is due to the enhanced cellular uptake, reduced toxicity and the inherent anti-HIV activity of TuPPI. © 2008 Published by Elsevier B.V.
Keyword Tuftsin
Dendrimer
Poly(propyleneimine) dendrimers
Antiretroviral drug targeting
Macrophages
Anti-HIV activity
Phagocytic uptake
Q-Index Code C1
Q-Index Status Confirmed Code

Document type: Journal Article
Sub-type: Article (original research)
Collections: 2009 Higher Education Research Data Collection
Excellence in Research Australia (ERA) - Collection
School of Pharmacy Publications
 
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Created: Wed, 08 Apr 2009, 20:01:17 EST by Elizabeth Pyke on behalf of School of Pharmacy