DEVELOPMENT AND INVESTIGATION OF EUDRAGIT S-100 ENCAPSULATED CHITOSAN COATED LIPOSOMES OF PREDNISOLONE FOR COLON TARGETINGAbstract
The objective of the study was to formulate coated liposomes containing Prednisolone for colon targeting and localization of the therapy to the inflamed colon mucosa. Liposomes were prepared using thin film hydration method. Liposomal formulations were optimized using 32 factorial design using varying concentrations of SPC and cholesterol as independent variables and % EE as the dependent variable. Optimized formulation F5 (60:30) was selected for successive coating with chitosan and eudragit S-100. Chitosan concentration of 1% w/v was taken as optimal based on ZP values. The coated liposomes were encapsulated in eudragit S-100 shell using a solvent-free method. The size if liposomes increased upon addition of the coatings. Fluorescent microscopy aided in clear visualization of chitosan coating around the vesicles. SEM images showed a transition surface appearance in the order smooth-rough-smooth for F5 and the coated liposomes. Eudragit S-100 coated liposomes were subjected to in-vitro drug release studies using simulated fluids for 16 h. ECL5 with 2% w/v eudragit showed sufficient lag time of 6 h. The formulation was able to protect the liposomes in gastric as well as small intestinal conditions, i.e., up to 5 h. Drug release of ECL5 followed zero order kinetics and fitted to Hixon-Crowell release model. The findings of the study conducted indicate a promising approach of the coated liposomes in the targeted release of the drugs.
S. B. Mascarenhas *, M. Koland and H. Kumar
Department of Pharmaceutics, N. G. S. M. Institute of Pharmaceutical Sciences, NITTE Deemed to be University, Paneer, Deralakatte, Mangalore, Dakshina Kannada, Karnataka, India.
28 August 2018
29 October 2018
31 October 2018
01 May 2019