International Journal of Life science and Pharma Reviews (IJLPR)  
   
 
International Journal of Life science and Pharma Research (IJLPR)
Pharmaceutical Sciences
Volume 6 Issue 2, April - June 2016    Pages:26-33
FORMULATION AND EVALUATION OF LOPERAMIDE LOADED POLYSORBATE 80 AND PEG CONJOINED COATED NANO LIPOSOMES

I SARATH CHANDIRAN,PICHANDY MUTHU PRASANNA
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DOI: DOI not available
Abstract:
Loperamide (Lp) cannot pass blood brain barrier but if delivered to brain it produces opiatic activity. Peripherally it produces antidiarheal activity. Its central antinociceptive activity was blocked by Pglyco protein (Pgly) efflux of BBB. Thus a nano sized liposomes for Lp coated with Polysorbate80 and Polyethylene Glycol 20000 (PEG) which favours blood brain barrier (BBB) penetration would be a best carrier for delivering Lp to brain. Thus an approach was made to formulate Lp loaded nano liposomes and conjoined coating the lipid carrier with Polysorbate80 (PS80) which is a Pgly efflux inhibitor and Polyethylene Glycol 20000 (PEG). The formulation were characterised for Entrapment efficiency (EE) , Invitro release study ,zeta potential , particle size distribution ,Scanning electron microscopy (SEM) and Differenctial Scanning calorimetry (DSC) .Entrapment efficiency(EE) of S2G2 was found to be lower (40.51±1.44) . Invitro release study in Artificial Cerebrospinal fluid (ACSF) for 44 hours showed a maximum Lp release for S0G0 (76.8% ± 2.14) and minimum for S0 G2 (33.2% ± 3.27) indicating PEG potential to retard drug release rate. Release kinetic study confirmed the Lp released from CCLs followed Higuchi model of diffusion . Among CCLs, the Zeta potential (ZP) for S2G2 were found to be high (-18.28 mV + 0.31) , low mean particle size (196 nm ± 3.85) and low poly disperse index (PDI) (0.18± 0.31). SEM and DSC ensured the Lp present in the S2G2 as amorphous and as molecular dispersion state. Thus S2G2 CCLs was found to be suitable for BBB penetration and can be further studied for invio performances.
Keywords: loperamide,Blood brain barrier,PGlycoprotein efflux,zeta potential
 
 
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