DEVELOPMENT OF β-CYCLODEXTRIN CROSSLINKED NANOSPONGES FOR ENHANCED ENCAPSULATION AND CONTROLLED DELIVERY OF RABEPRAZOLE

Awinish Kumar Shrivastaw*, Manju Makhija

Rabeprazole belongs to a group of drugs called proton pump inhibitors (PPIs) which are commonly used to treat stomach ulcers and other stomach acid conditions. However, there is a problem with low aqueous solubility and rapid degradation at acidic pH that hinders its therapeutic performance. The objective of the present study was to prepare β-cyclodextrin crosslinked nanosponges for better drug encapsulation for a controlled oral drug delivery. Preformulation studies such as Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), solubility analysis, partition coefficient determination, UV spectrophotometric calibration and drug–excipient compatibility studies were performed to extract Rabeprazole from the enteric coated pellets. Six nanosponge formulations (F1–F6) were obtained from the use of β-cyclodextrin and diphenyl carbonate with different ratios of polymer to crosslinker. The formulations were assessed in terms of particle size, polydispersity index, zeta potential, surface morphology, drug loading, entrapment efficiency, production yield, in vitro drug release, release kinetics and stability. F5 had the best performance among the developed formulations with particle size of 228.7 nm ± 4.6 nm, polydispersity index of 0.241 ± 0.007 and the entrapment efficiency of 88.91 ± 1.11%. The FTIR and DSC analyses revealed that there were no noticeable significant physicochemical interactions between rabeprazole and the selected formulation components. The optimized formulation showed controlled drug release with suitable stability during the investigated storage conditions. The present findings demonstrate that the crosslinked nanosponges of β-cyclodextrin are an effective carrier system for rabeprazole and can be used as an effective method to enhance the encapsulation efficiency, formulation stability and controlled oral drug delivery.