Exploring dendrimer towards dual drug delivery: pH responsive simultaneous drug-release kinetics

Tekade, Rakesh Kumar, Dutta, Tathagata, Gajbhiye, Virendra and Jain, Narendra Kumar (2009) Exploring dendrimer towards dual drug delivery: pH responsive simultaneous drug-release kinetics. Journal of Microencapsulation, 26 4: 287-296. doi:10.1080/02652040802312572

Author Tekade, Rakesh Kumar
Dutta, Tathagata
Gajbhiye, Virendra
Jain, Narendra Kumar
Title Exploring dendrimer towards dual drug delivery: pH responsive simultaneous drug-release kinetics
Journal name Journal of Microencapsulation   Check publisher's open access policy
ISSN 0265-2048
Publication date 2009-06
Sub-type Article (original research)
DOI 10.1080/02652040802312572
Volume 26
Issue 4
Start page 287
End page 296
Total pages 10
Editor T. L. Whateley
O. Alpar
Place of publication London, U.K.
Publisher Taylor & Francis
Collection year 2010
Language eng
Subject C1
860899 Human Pharmaceutical Products not elsewhere classified
111599 Pharmacology and Pharmaceutical Sciences not elsewhere classified
1115 Pharmacology and Pharmaceutical Sciences
111504 Pharmaceutical Sciences
100703 Nanobiotechnology
Formatted abstract
A major problem associated with conventional leukaemia chemotherapy is the development of resistance that can be surmounted well by combination chemotherapy. The objective of the present investigation is to reaport a novel technology to load two anti-leukaemic drugs of choice simultaneously inside the PAMAM dendrimer. Under optimized conditions of pH and dialysis time, one molecule of PAMAM dendrimer was found to be capable of entrapping 27.02 ± 0.51 and 8.00 ± 0.46 molecules of Methotrexate and all-trans Retinoic acid (ATRA), respectively. The simultaneous in-vitro release profiling of the loaded drugs was studied at pH 4, 7.4 and 10. The release kinetics was found to be governed by degree of dendrimer protonation, with more sustained and controlled behaviour at pH 7.4. Terminal loading of dendrimer with less haemolytic bioactive (ATRA) reduced the haemolytic toxicity of the dendrimer formulation. A cytotoxicity study was performed on HeLa cell lines by MTT assay, wherein after 72 h, the dual-drug loaded dendrimer was found to be more efficient (IC50 0.5 µM) as compared to that of the free drug combination (IC50 0.75 µM).
© 2009 Informa UK Ltd
Keyword Dendrimer
Dual-drug loading strategy
Simultaneous release study
pH dependent protonation
MTT cytotoxicity assay
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
School of Pharmacy Publications
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Citation counts: TR Web of Science Citation Count  Cited 57 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 65 times in Scopus Article | Citations
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Created: Wed, 08 Apr 2009, 10:27:04 EST by Elizabeth Pyke on behalf of School of Pharmacy