Document Detail

Dual approach utilizing self microemulsifying technique and novel P-gp inhibitor for effective delivery of taxanes.
MedLine Citation:
PMID:  22439872     Owner:  NLM     Status:  MEDLINE    
In the present work, concomitant use of self-microemulsifying drug delivery systems (SMEDDS) and a novel third-generation P-gp inhibitor, GF120918 (elacridar), for the effective transport of taxanes (paclitaxel and docetaxel) across an in vitro model of the intestinal epithelium and uptake into tumor cells were investigated. On the basis of solubility studies and ternary phase diagrams, different SMEDDS formulations of taxanes were prepared and characterized. In caco-2 cell permeation study, paclitaxel-loaded SMEDDS along with GF120918 showed a four-fold increase in apparent permeability, while docetaxel-loaded SMEDDS in combination with GF120918 showed a nine-fold increase in permeability, as compared to plain drug solution. Cell uptake studies on A549 cells were performed with microemulsions formed from both SMEDDS formulations loaded with rhodamine 123 dye and showed good uptake than plain dye solution. Confocal laser scanning microscopic images further confirmed the higher uptake of both SMEDDS formulations in the presence of GF120918.
Akash Chaurasiya; Ajeet K Singh; Gaurav K Jain; Musarrat H Warsi; Emmanuelle Sublet; Farhan J Ahmad; Gerrit Borchard; Roop K Khar
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2012-03-22
Journal Detail:
Title:  Journal of microencapsulation     Volume:  29     ISSN:  1464-5246     ISO Abbreviation:  J Microencapsul     Publication Date:  2012  
Date Detail:
Created Date:  2012-08-23     Completed Date:  2012-12-31     Revised Date:  2013-05-28    
Medline Journal Info:
Nlm Unique ID:  8500513     Medline TA:  J Microencapsul     Country:  England    
Other Details:
Languages:  eng     Pagination:  583-95     Citation Subset:  IM    
Faculty of Pharmacy, Hamdard University, New Delhi 110062, India.
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MeSH Terms
Acridines* / chemistry,  pharmacokinetics,  pharmacology
Antineoplastic Agents, Phytogenic* / chemistry,  pharmacokinetics,  pharmacology
Caco-2 Cells
Drug Delivery Systems*
Drug Screening Assays, Antitumor
P-Glycoprotein / antagonists & inhibitors*
Paclitaxel* / chemistry,  pharmacokinetics,  pharmacology
Taxoids* / chemistry,  pharmacokinetics,  pharmacology
Tetrahydroisoquinolines* / chemistry,  pharmacokinetics,  pharmacology
Reg. No./Substance:
0/ABCB1 protein, human; 0/Acridines; 0/Antineoplastic Agents, Phytogenic; 0/P-Glycoprotein; 0/Taxoids; 0/Tetrahydroisoquinolines; 15H5577CQD/docetaxel; 33069-62-4/Paclitaxel; N488540F94/Elacridar

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