Formulation of sustained release bioadhesive minitablets containing solid dispersion of levofloxacin for once daily ocular use

AbstractThis study aimed to increase ocular residence time of levofloxacin by formulation into zero order controlled release mucoadhesive minitablets for once daily administration using a hydrophobic-hydrophilic polymeric matrix. Levofloxacin was first formulated into solid dispersion with different ratios of Eudragit® RS then the resulting solid dispersion was mixed with different concentrations of Carbopol® and other excipients to be finally compressed into minitablets.A 2^4 full factorial design was employed to estimate the effects and interactions of two formulation factors, and to establish their relationships with selected responses in the developed minitablets. The studied factors were: drug to Eudragit® RS ratio, and percent of Carbopol® in the minitablets. Sixteen ocular minitablets formulations were prepared and evaluated for the cumulative percentages drug release at 6, 12 and 24 h, as well as mucoadhesion time, mucoadhesive strength, and swelling index as response variables. After optimizing t...