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Please use this identifier to cite or link to this item: http://repository.iitr.ac.in/handle/123456789/1538
Title: Anti-cancer, pharmacokinetic and biodistribution studies of cremophor EL free alternative paclitaxel formulation
Authors: Jain S.K.
Utreja P.
Tiwary A.K.
Mahajan M.
Kumar N.
Roy P.
Published in: Current Drug Safety
Abstract: Purpose: The aim of the present investigation is to determine the in vivo potential of previously developed and optimized Cremophor EL free paclitaxel (CF-PTX) formulation consisting of soya phosphatidylcholine and biosurfactant sodium deoxycholate. CF-PTX was found to have drug loading of 6 mg/ml similar to Cremophor EL based marketed paclitaxel formulation. In the present study, intracellular uptake, repeated dose 28 days sub-acute toxicity, anti-cancer activity, biodistribution and pharmacokinetic studies were conducted to determine in vivo performance of CF-PTX formulation in comparison to marketed paclitaxel formulation. Methods: Intracellular uptake of CF-PTX was studied using A549 cells by fluorescence activated cell sorting assay (FACS) and fluorescence microscopy. In vivo anti-cancer activity of CF-PTX was evaluated using Ehrlich ascites carcinoma (EAC) model in mice followed by biodistribution and pharmacokinetic studies. Results: FACS investigation showed that fluorescence marker acridine orange (AO) solution showed only 19.8±1.1% intracellular uptake where as significantly higher uptake was observed in the case of AO loaded CF-PTX formulation (85.4±2.3%). The percentage reduction in tumor volume for CF-PTX (72.5±2.3%) in EAC bearing mice was found to be significantly (p<0.05) higher than marketed formulation (58.6±2.8%) on 14th day of treatment. Pharmacokinetic and biodistribution studies showed sustained plasma concentration of paclitaxel depicted by higher mean residence time (MRT; 18.2±1.8 h) and elimination half life (12.8±0.6 h) with CF-PTX formulation as compared to marketed formulation which showed 4.4±0.2 h MRT and 3.6±0.4 h half life. The results of the present study demonstrated better in vivo performance of CF-PTX and this formulation appears to be a promising carrier for sustained and targeted delivery of paclitaxel. © 2014 Bentham Science Publishers.
Citation: Current Drug Safety (2014), 9(2): 145-155
URI: https://doi.org/10.2174/1574886308666131223123218
http://repository.iitr.ac.in/handle/123456789/1538
Issue Date: 2014
Publisher: Bentham Science Publishers
Keywords: Alternative paclitaxel formulation
Anti-cancer activity
Biodistribution study
Fluorescence microscopy
Intracellular uptake
Pharmacokinetic study
ISSN: 15748863
Author Scopus IDs: 55712554200
26536851600
7004094730
55649961700
57192281884
35509207200
Author Affiliations: Jain, S.K., Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, 143005, India
Utreja, P., Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala 147002, India
Tiwary, A.K., Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala 147002, India
Mahajan, M., Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, 143005, India
Kumar, N., Department of Biotechnology, IIT, Roorkee, India
Roy, P., Department of Biotechnology, IIT, Roorkee, India
Corresponding Author: Jain, S. K.; Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab, 143 005, India; email: subheetjain@rediffmail.com
Appears in Collections:Journal Publications [BT]

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