ABSTRACT
Olanzapine is an atypical antipsychotic drug shows low bioavailability due to extensive first pass metabolism and results in numerous side effects due to non targeted delivery. The present study was aimed to prepare and characterize olanzapine loaded chitosan nanoparticles for nose to brain targeting. The olanzapine loaded chitosan nanoparticles were prepared by ionic gelation of chitosan with tripolyphosphate anions. The formulated nanoparticles showed mean particle size, polydispersity index and zeta potential to be 183.1±8.42 nm, 0.122±0.08, +52.1±2.4 mV respectively. The entrapment efficiency and drug loading was found to be 72.42 ±3.65% and 26 .04± 2.12. In vitro drug release was showed a biphasic release pattern with initial burst release followed by sustained release of formulated nanoparticles. In vitro toxicity studies were carried out on RPMI 2650 human nasal epithelial cell line by MTT assay. The obtained result shows lower toxicity (high IC50 value) of nanoformulation as compared to free drug. Ex vivo histopathological studies were carried out by using excised goat nasal mucosa and the microscopic structure of nasal mucosa shows no significant harmful effects of formulated nanoparticles. These results illustrate that olanzapine loaded chitosan nanoparticles is a potential new delivery system for treatment of depressant when transported via olfactory nasal pathway to the brain.
ABSTRACT
Objective: To study the optimal preparation process of glycyrrhetinic acid-chitosan nanoparticles (GA-CS-NPs) and to evaluate the quality. Methods: The GA-CS-NPs were prepared by ionic cross-linking. The particle size, drug loading, and encapsulation efficiency were as evaluation indexes. The prescription and preparation process were optimized through single factor and orthogonal design. The quality of GA-CS-NPs was evaluated by morphology, particle size, drug loading, and encapsulation efficiency. Results: The optimal prescription was as follows: concentration of GA and CS was 0.2 and 2 mg/mL, ratio of CS and TPP (1.0 mg/mL) solutions was 20∶3. The mean diameter of GA-CS-NPs was (310.27 ± 10.02) nm, the entrapment efficiency and drug-loading efficiency were (51.42 ± 0.43)% and (6.87 ± 0.47)%. The evaluation showed that the appearance of GA-CS-NPs was round and uniform. It had a certain stability under lower temperature. Conclusion: The ionic cross-linking method used to prepare GA-CS-NPs is simple, rational, and stable.