Journal article
Development and characterization of site specific target sensitive liposomes for the delivery of thrombolytic agents
International journal of pharmaceutics, Vol.403(1-2), pp.254-261
01/17/2011
DOI: 10.1016/j.ijpharm.2010.10.028
PMID: 20971175
Abstract
In recent times, search for potent and highly selective thrombolytic agents with minimal side effects has become a major area of research. The aim of the present study was to develop and characterize target sensitive (TS) liposomes encapsulating streptokinase, a thrombolytic agent. The developed TS liposomes were composed of dioleylphophatidyl ethanolamine (DOPE) and dipalmityl-c(RGDfK) (10:1 mol/mol). Dipalmityl-c(RGDfK) was synthesized using typical carbodiimide chemistry using palmitic acid and c(RGDfK), while lysine was used as a spacer. Liposomes were of 100-120 nm size. In vitro drug release study showed that nearly 40% drug of the entrapped drug was released in 12 h in the PBS (pH 7.4), however on incubation with activated platelet about 90% of drug was released within 45 min. The results suggested target sensitivity of the liposomes. Further, targeting potential was confirmed using fluorescent microscopy and flow cytometry. Clot lysis study revealed that TS liposomes could not only reduce the clot lysis time but also increase the extent of clot lysis as compared to non-liposomal streptokinase solution. In conclusion, the present liposomal formulation will target the thrombolytic agent to the activated platelets in the thrombus and hence will improve the therapeutic efficacy of the drug. (C) 2010 Elsevier B.V. All rights reserved.
Details
- Title: Subtitle
- Development and characterization of site specific target sensitive liposomes for the delivery of thrombolytic agents
- Creators
- Bhuvaneshwar Vaidya - Dr. Hari Singh Gour UniversityManasa K. Nayak - Banaras Hindu UniversityDebabrata Dash - Banaras Hindu UniversityG. P. Agrawal - Dr. Hari Singh Gour UniversitySuresh P. Vyas - Dr. Hari Singh Gour University
- Resource Type
- Journal article
- Publication Details
- International journal of pharmaceutics, Vol.403(1-2), pp.254-261
- Publisher
- Elsevier
- DOI
- 10.1016/j.ijpharm.2010.10.028
- PMID
- 20971175
- ISSN
- 0378-5173
- eISSN
- 1873-3476
- Number of pages
- 8
- Grant note
- All India Council of Technical Education (AICTE), New Delhi
- Language
- English
- Date published
- 01/17/2011
- Academic Unit
- Hematology, Oncology, and Blood & Marrow Transplantation; Internal Medicine
- Record Identifier
- 9984359833402771
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