Formulation and evaluation of polymeric nanoparticles of an antihypetensive drug for gastroretention

Abstract

The aim of present study was to formulate and evaluate nanoparticles of carvedilol by using different hydrophilic polymers. Carvedilol was selected as a suitable drug for gastro- retentive nanoparticles due to its short half life, low bioavailability, high frequency of administration, and narrow absorption window in stomach and upper part of GIT. The nano-precipitation method was used to prepare nanoparticles so as to avoid both chlorinated solvents and surfactants to prevent their toxic effect on the body. Nanoparticles of  carvedilol were prepared by using hydrophilic polymers such as HPMC K100M, chitosan, and gelatin. The prepared formulations were then characterized for particle size, polydispersity index, zeta potential, loading efficiency, encapsulation efficiency and drug-excipient compatibility. The prepared nanoparticulate formulations of carvedilol  with different polymers in 1:1 ratio have shown particle size in the range of 250.12-743.07 nm, polydispersity index (PDI) in the range of 0.681-1.0, zeta potential in the range of -14.2 to +33.2 mV, loading efficiency in the range of 8.74-17.54%, and entrapment efficiency in the range of 55.7%-74.2%. Nanoparticulate formulation prepared with chitosan in 1:1 ratio showed satisfactory results i.e. average particle size 312.04 nm, polydispersity index 0.681, zeta potential 33.2 mV, loading efficiency 17.54%, and entrapment efficiency 73.4%. FTIR study concluded that no major interaction occurred between  the drug and polymers used in the present study. Keywords: Nanoparticles; gastro-retentive; nano-precipitation, polydispersity index, zeta potential; entrapment efficiency.