PREPARATION AND EVALUATION OF NANOSPONGES BASED TRAMADOL HCL C/R TABLETS USING DESIGN OF EXPERIMENT

Abstract

Objective: The goal was to develop a controlled release formulation of tramadol utilizing the cyclodextrin-based nanosponges as a nanocarrier. Methods: Based on the preliminary trials a 3-factor, 3-level Box-Behnken design was employed. Five types of nanosponges from β-cyclodextrin (NS1-NS5) were purposely designed. Tramadol was loaded into nanosponges by the freeze-drying method. The prepared nanosponges were characterized and formulated into tablets and evaluated. Results: The particle sizes of tramadol-loaded nanosponges are in between 34.38 to 134.26 nm, encapsulation efficiency of 41.13-86.72% and drug release% at 6h of 52.34-81.12%. In vitro release studies showed that more than 90 % of the drug were released from nanosponge formulations as compared to only around 20% from free drug suspension after 24 h. The FTIR, DSC and XRPD studies confirmed the interaction of Tramadol with nanosponges. TEM image revealed the spherical structure of drug-loaded nanosponges. The drug-loaded in the nanosponge structure can be retained and released slowly over time. The nanosponges were formulated into tablets and evaluated for weight variation, hardness, friability and disintegration studies and obtained satisfactory results. In vitro release of drug from tablet showed controlled release behavior for a period of 12 h. The percentage of tramadol released from nanosponges tablets after was 87.48 percent and stability studies indicated no significant changes within 6 months. Conclusion: Cyclodextrin-based nanosponges showed superior complexing ability with increased solubility of poorly soluble Tramadol tablets made for controlled drug delivery, which can reduce dosing frequency.