| Development of indinavir submicron lipid emulsions loaded with lipoamino acids-in vivo pharmacokinetics and brain-specific delivery. | |
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MedLine Citation:
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PMID: 21360313 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The aim of our present work was to develop indinavir O/W submicron lipid emulsions (SLEs) loaded with lipoamino acids for specific delivery to brain. Tetradecyl aspartic acid (A) and decyl glutamic acid (G) loaded stable SLEs of indinavir having a mean size range of 210-220 nm and average zeta potential of -23.54±1.2 mV were developed using homogenization and ultrasonication. The cumulative % drug release from different SLEs varied in between 26% and 85%. The formulations, SLE, SLE-A3, and SLE-G3 were stable to the centrifugal stress, dilution stress, and storage at RT. The total drug content and entrapment efficiency were determined by HPLC method. During pharmacokinetic studies in male Wistar rats there was no significant difference in the serum levels of indinavir for SLE, SLE-A3 and SLE-G3 formulations at all time points. In tissue distribution studies, the therapeutic availability (TA) of indinavir in brain and kidneys for SLE-A3 were 4.27- and 2.66-fold whereas for SLE-G3 were 2.94 and 2.12 times, respectively, higher than that of indinavir solution. But when compared with that of SLE, in brain tissue the levels of indinavir from SLE-G3 and SLE-A3 varied in between 2.5- and 3.38-fold. While in case of the kidney, it was between 1.23- and 1.54-fold only. However, the TA is not significantly different in tissues like the heart, liver, and spleen. Thus, brain-specific delivery of indinavir was improved by including tetradecyl aspartic acid and decyl glutamic acid in submicron lipid emulsions. |
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Authors:
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Swetha Bollam; Prabhakar Kandadi; Shashank Sridhar Apte; Kishan Veerabrahma |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2011-03-01 |
Journal Detail:
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Title: AAPS PharmSciTech Volume: 12 ISSN: 1530-9932 ISO Abbreviation: AAPS PharmSciTech Publication Date: 2011 Mar |
Date Detail:
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Created Date: 2011-03-30 Completed Date: 2011-11-09 Revised Date: 2012-09-20 |
Medline Journal Info:
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Nlm Unique ID: 100960111 Medline TA: AAPS PharmSciTech Country: United States |
Other Details:
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Languages: eng Pagination: 422-30 Citation Subset: IM |
Copyright Information:
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© 2011 American Association of Pharmaceutical Scientists |
Affiliation:
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Nanotechnology Laboratory, Department of Pharmaceutics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Andhra Pradesh, India 506009. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Amino Acids
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chemistry Animals Brain / drug effects* Drug Carriers Drug Delivery Systems* Drug Stability Emulsions / chemistry HIV Protease Inhibitors / administration & dosage*, blood, chemistry, pharmacokinetics* Indinavir / administration & dosage*, blood, chemistry, pharmacokinetics* Lipids / chemistry Male Rats Rats, Wistar Solubility Tissue Distribution |
| Chemical | |
Reg. No./Substance:
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0/Amino Acids; 0/Drug Carriers; 0/Emulsions; 0/HIV Protease Inhibitors; 0/Lipids; 150378-17-9/Indinavir |
| Comments/Corrections | |
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