Preparation of Plga Nanoparticles for Encapsulating Hydrophilic Drug Modifications of Standard Methods

INTRODUCTION Developing strategies for the delivery of hydrophilic drugs and macro molecules such as proteins and peptides is emerging as an important in research field as several new synthesized molecules are hydrophilic in nature. Some of the major problem incurred by the small hydrophilic molecules is low encapsulation, low permeability across barriers, shorter half-life in the circulatory systems, toxicity and poor distribution to the target site. And in order ABSTRACT The effective encapsulation of the drugs that are highly soluble in both aqueous and organic solvent are intricate to attain using standard nanoparticle preparation methods, such as nanoprecipitation (NPC) and double emulsion solvent evaporation method (DESE) due to the rapid partitioning of drug to the external aqueous phase. Modifications of standard methods are required to enhance the encapsulation efficiency. The present work focused on enhancing the encapsulation of highly aqueous and solvent soluble model drug rivastigmine tartrate. The prepared NP was evaluated for its physicochemical properties. The change of aqueous phase pH from 6-9 in NPC method showed encapsulation efficiency from 15 to 35% with the size of 125±12nm and potential ranged from 31±2 to -40±3mv. In DESE method the use of DCM: EA (50:50) as an organic phase resulted in 1 fold increase of encapsulation with the size of 175±15nm. When EA used as an organic phase it results in 2.5 folds increase in encapsulation efficiency. The NP prepared using Pluronic F-127 showed the zeta value (-13±2mv) while DMAB showed the zeta value (+ 40±1mv) with smaller size (105±10nm). In vitro release studies for NPC and DESE method for 24hr was 45.4 ±2.7 and 51.2±3.2 %. The cytotoxicity study using SH-SY-5Y cell line evidenced no toxicity of prepared NP.