Preparation and fabrication of nanosponges nifedipine and study of its in vitro characterization

Background and aim: 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 molecules. Nifedipine is a class II drug substance with poor bioavailability due to its low aqueous solubility (5.9 mg/l). The aim of this research work was to synthesize the nifedipine-cyclodextrin nanosponge complex and investigate its physiochemical 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 efficiency, sample was dissolved in methanol and analysed by UV spectrophotometer at 243 nm.The release study of nifedipine from nanosponge complex was performed using a dyalise cell in a medium of SLS 1.25% (W/V) with pH= 6.8 (phosphate buffer). Results: The particle sizes of nanosponges (1: 2 and 1: 4) was 31 and 64 nm with a zeta potential of -27 and -16 respectively. Loading efficiency of nifedipine was 47.25% and 57.46 for NS (1: 2) and (1: 4). In vitro release study of nifedipine showed a rapid and complete release pattern (100% release in 4 hours). while 25% of pure nifedipine was passed from dialysis membrane in 4 hours. Discussion and conclusion: It can be concluded from these findings that nifedipine-loaded NS have appropriate colloidal particle size with acceptable loading efficiency. DSC and FTIR studies corroborated the encapsulation of nifedipine in CDNS. There is marked enhancement in in vitro release parameters of with nifedipine formulation as compared to plain nifedipine.