Pharmaceutica Analytica Acta

QbD based design and development of surface modified polymeric nanoparticulate systems of Antipsychotic drug for brain targeting

5^th International Conference and Exhibition on Pharmaceutics & Novel Drug Delivery Systems

March 16-18, 2015 Crowne Plaza, Dubai, UAE

Emil Joseph, Garima Balwani, Vibhu Nagpal, Satish Reddi and R N Saha

Posters & Accepted Abstracts: Pharm Anal Acta

Abstract:

The main objective of the present study was to design and develop novel nanoparticulate delivery systems (NPDS) of widely prescribed anti-psychotic drug, Olanzapine (OLN) for controlled release and better distribution to brain. This paper presents effect of few variables on in-vitro characters of NPDS. Nanoparticulate systems have been prepared using biodegradable polymer polycaprolactone utilizing nanoprecipitation method. A QbD based design was used for formulation development, where amount of surfactant (poloxomer 188) and polymer concentration were selected as significant variables affecting the desired outputs such as particle size and encapsulation efficiency. Surface plots have been made using design expert software and it was found that both the selected variables have significant impact on both the desired outputs. The optimized formulations were further surface modified using tween 80 in order to achieve better brain targeting characteristics since this would inhibit P-glycoprotein and augment endocytosis across blood-brain-barrier. The size and zeta-potential of obtained nanoparticles were found to be <200nm and >20mV (better physical stability) respectively. Drug content and encapsulation efficiency of the optimized formulations, determined using in-house developed HPLC analytical technique were found to be 5.44?0.04%w/w and 82.64?1.41% respectively. Further, in vitro release studies using dialysis bag technique demonstrated controlled release of OLN from these delivery systems up to 60hr. These results would help to achieve optimum dopamine-D2 receptor occupancy (60-80%), thereby, better anti-psychotic action with least extra-pyramidal adverse effects and decreased weight gain. Designed formulations are to be further studied for pharmacokinetics and bio-distribution in suitable animal model..

Biography :

Emil Joseph is a Senior Research Fellow in Industrial Research Lab, Department of Pharmacy, BITS Pilani, India with UGC-Government of India fellowship for pursuing Doctoral research. He has qualified national level competitive exam, GATE twice and received numerous awards including prestigious Department of Science and Technology-Government of India international travel award for young scientist. He has published numerous articles in reputed journals and presented as well as reviewed posters in international conferences. He also has diverse research experience in central labs such as Central Drug Research Institute of India and Formulation & Development division of reputed pharmaceutical industries.