Document Detail

Development of indinavir submicron lipid emulsions loaded with lipoamino acids-in vivo pharmacokinetics and brain-specific delivery.
MedLine Citation:
PMID:  21360313     Owner:  NLM     Status:  MEDLINE    
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.
Swetha Bollam; Prabhakar Kandadi; Shashank Sridhar Apte; Kishan Veerabrahma
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2011-03-01
Journal Detail:
Title:  AAPS PharmSciTech     Volume:  12     ISSN:  1530-9932     ISO Abbreviation:  AAPS PharmSciTech     Publication Date:  2011 Mar 
Date Detail:
Created Date:  2011-03-30     Completed Date:  2011-11-09     Revised Date:  2013-06-30    
Medline Journal Info:
Nlm Unique ID:  100960111     Medline TA:  AAPS PharmSciTech     Country:  United States    
Other Details:
Languages:  eng     Pagination:  422-30     Citation Subset:  IM    
Copyright Information:
© 2011 American Association of Pharmaceutical Scientists
Nanotechnology Laboratory, Department of Pharmaceutics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Andhra Pradesh, India 506009.
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MeSH Terms
Amino Acids / chemistry
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
Rats, Wistar
Tissue Distribution
Reg. No./Substance:
0/Amino Acids; 0/Drug Carriers; 0/Emulsions; 0/HIV Protease Inhibitors; 0/Lipids; 150378-17-9/Indinavir

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