Journal of Nanomedicine & Nanotechnology

Optimized positively charged self-nanoemulsifying systems of candesartan cilexetil with enhanced bioavailability potential

3^rd International Conference on Nanotek & Expo

December 02-04, 2013 Hampton Inn Tropicana, Las Vegas, NV, USA

Sarwar Beg, Gajanand Sharma, O. P. Katare and Bhupinder Singh

Accepted Abstracts: J Nanomed Nanotechnol

Abstract:

Nanostructured drug delivery systems have recently gained higher potential in drug delivery with special on bioavailability enhancement of poorly water soluble drugs. Such systems include liposomes, nanoparticles, nanoemulsions, nanotubes, nanocomposites and many more. Positively charged self-nanoemulsifying drug delivery systems (P-SNEDDS) are newer and innovative drug delivery innovations which have proved significant potential to augment the oral bioavailability of lipophilic drugs. Due to the cationic charge, such systems have enhanced interaction with mucosal surface and subsequently increased cellular uptake of drugs, leading to enhanced dissolution and permeation, bypassing hepatic first-pass effect (HPE) and P-gp efflux. The current research work entails formulation development and evaluation of P-SNEDDS of candesartan cilexetil, a BCS class II drug exhibiting extensive HPE and low oral bioavailability (15%), using Formulation by Design (FbD). Pseudo- ternary phase diagrams and FT-IR studies facilitated selection of constituents for P-SNEDDS viz., lauroglycol 90 (oil), tween 40 (surfactant), transcutol HP (co-surfactant) and oleylamine (cationic charge inducer). A D-optimal mixture design (three factors and two levels) was employed for optimizing P-SNEDDS employing Design Expert? software. Globule size, percent dissolution efficiency, MDT, amount permeated through intestine and emulsification time were employed as response variables to optimize the formulation. The optimized formulation was studied for ex vivo permeability using everted sac technique, in vivo pharmacokinetics studies and in situ single pass perfusion (SPIP) studies in Wistar rats. The curvilinear 3-D response surface and 2-D contour plots construed remarkable diminution in globule size and consequent improvement in drug release (>90% in 15 min) with decreasing oil and increasing surfactant and co-surfactant levels. Pharmacokinetic and SPIP studies on the optimized positively charged system revealed 3-4 fold bioavailability enhancement vis-?-vis the marketed formulation (CANDESARTM) and significant improvement as compared to conventional SEDDS. In a nutshell, the P-SNEDDS have immense potential to significantly enhance bioavailability of poorly soluble drugs

Biography :

Sarwar Beg is a Doctoral Research Fellow in Pharmaceutics from Panjab University, Chandigarh, India. Currently, he is also a recipient of UGC- Research Fellowship in Science for Meritorious Students (RFSMS), Ministry of HRD, Govt. of India. He worked as a Trainee Research Associate from Ranbaxy Laboratories Limited, India. Also, he has worked as Assistant Professor for one in Roland Institute of Pharmaceutical Sciences, Berhampur, India. His major area of research interests include Self-emulsifying Drug Delivery, Oral Controlled Release Drug Delivery, Nanotechnology Based Drug Delivery using Microspheres, Nanoparticles, Dendrimers, Carbon nanotubes and Nanocomposites. Till date he has more than 20 publications in drug delivery in various high impact International journals, 2 book chapters, 2 Indian patents and attended 5 national and International conferences to his credit.