Cyclodextrin based Nanosponges for the Oral Delivery of Actarit: Physicochemical Characterisation and Dissolution Studies

Abstract

Introduction: The current research aims to formulate a controlled release formulation of Actarit utilizing cyclodextrin based nanosponges as a nanocarriers. β-Cyclodextrin built nanosponges were prepared by condensation reaction using diphenyl carbonate as crosslinking agent. Method: A 3-level, 3-factor Box-Behnken design was used to optimize the reaction conditions. The particle size, zeta potential and solubilization efficiency of prepared nanosponges were determined. Actarit was loaded into nanosponges by freeze drying method. Actarit loaded nanosponges were further evaluated for particle size, zeta potential, surface morphology, FTIR, DSC, XRD and Dissolution characteristics. The cyclodextrin nanosponges prepared under optimum conditions exhibited a particle size range of 143.42 to 152.76 nm with low polydispersity indices. FTIR spectra confirmed the formation of carbonyl bond between the β-Cyclodextrin molecules. Results and Discussion: Actarit loaded nanosponges exhibited a particle size range of 157.13 to 168.34 nm with minimum polydispersity index. The zeta potential value was sufficiently high to maintain the stability of colloidal nanosponges. TEM image exposed the spherical structure of drug loaded nanosponges that could be retained and released gradually over time. The FTIR, DSC and XRPD studies inveterate the interaction between Actarit and nanosponges. The drug loaded nanosponges displayed a significant progress in dissolution of drug when compared to plain Actarit. The initial rapid release of Actarit from nanosponges formulations was observed. After 24 h of study, around 90 % of the drug released from nanoformulation and only around 20 % of the drug from free drug suspension. Conclusion: Cyclodextrin based nanosponges displayed superior complexing capability with increased solubility of poorly soluble Actarit.