production of cyclodextrin nanosponge flutamide and study of its in vitro characterizations

Abstract

Introduction and Background: Cyclodextrin-based nanosponge is a three dimensional sponge-like structure of cyclodextrins that are bonded together with carbonate bonds. These structures have a high capacity to encapsulate, increase solubility, modify release and protect drug moleculs. Flutamide is a class II drug substance with a poor bioavalability due to it´s low aqueous solubility (9.45 mg/l). Aim: The aim of this research work was to synthesis flutamide-cyclodextrin nanosponge complex and investigate it's phisyochemical properties. Methods:In this study, two types of nanosponges (1:2and1:4/ carbonyldiimidazole: cyclodextrin) were prepared and the characteristics of each were studied. Solvent method was used to prepare nanosponges and freeze drying method was used to drug loading. Particle size and zeta potential studied by Dynamic Light Scattering method. To get the loading efficency ,sample was dissolved in methanol and analysed by UV spectrophotometer at 295 nm.The release study of flutamide from nanosponge complex was performed using a microdyalise cell with dialysis membrane (cut-off 12,000 Da) in a medium of SLS 2% (W/V) with pH= 7.4 (phosphate buffer). Results: The particle sizes of nanosponges (1:2 and 1:4) was 24 and 99 nm with a zeta potential of -19.3 and -42 respectively . Loading efficiency of flutamide was 36.05% and 56.55 for NS ( 1:2 ) and (1:4). In vitro release study of flutmide showed a rapid and complete release pattern ( 100% release in 3 hours). while 25% of pure flutamide was passed from dialysis membrane in 3 hours. Discussion and conclusion: It can be concluded from these findings that flutamide-loaded NS have appropriate colloidal particle size with acceptable loading efficiency . DSC and FTIR studies corroborated encapsulation of flutamide in CDNS. There is marked enhancement in in vitro release parameters of with flutamide formulation as compared to plain flutamide.