Open AccessSelf Nanoemulsifying Drug Delivery System of Candesartan Cilexetil with Improved Bioavailability
Author(s) -
J. Venkateswara Rao,
T. Rama Mohan Reddy
Publication year - 2018
Publication title -
international journal of pharmaceutical sciences and drug research
Language(s) - English
Resource type - Journals
ISSN - 0975-248X
DOI - 10.25004/ijpsdr.2018.100501
Subject(s) - bioavailability , candesartan , pulmonary surfactant , drug delivery , chemistry , chromatography , cmax , zeta potential , pharmacology , drug , materials science , angiotensin ii , nanoparticle , nanotechnology , medicine , organic chemistry , receptor , biochemistry
Candesartan is an angiotensin II receptor blocker with inherent low bioavailability. The present studies entail the optimization and evaluation of self- nanoemulsifying drug delivery system (SNEDDS) of Candesartan in order to enhance its oralbioavailability. For this Capryol 90, Captex 500, Labrasol were used as oil, surfactant and co surfactant respectively. FTIR studies revealed no interaction among the drug and polymers used in the formulation. Based on the physicochemical parametersand in-vitro dissolution studies, F17 prepared with Smix (Surfactant: Co-surfactant) of 3:1 and Oil:Smix of 6:4, was found to be an optimum one. The formulation F17 was found to release 99.12 ± 5.10% drug at the end of one hour and scanning electronmicroscopic analysis showed nanosized particles. The droplet size of the optimized formulation was found to be 51.7 nm and Z-Average of 59.2 nm. The zeta potential of the optimized formulation (F17) was found to be -15.5 mV. The formulations werealso found to be stable over a period of 6 months of testing. From in vivo bioavailability studies Cmax of the SNEDDS 35.2 ± 0.02 ng/ml was significant (p less than 0.05) as compared to the pure drug suspension formulation 25.1 ± 0.03ng/ml. Tmax ofboth SNEDDS formulation and pure drug suspension was 1.00 ± 0.03 h and 2.00 ± 0.01 h, respectively. AUC is an important parameter in evaluating bioavailability of drug from dosage form, AUC0-∞ infinity for SNEDDS formulation was higher (160.1±1.04ng.h/ml) than the pure drug suspension formulation 135.3 ± 2.02 ng.h/ml. Statistically, AUC0-t of the SNEDDS formulation was significantly higher (p less than 0.05) as compared to pure drug suspension formulation. Higher amount of drug concentration inblood indicated better systemic absorption of Candesartan from SNEDDS formulation as compared to the pure drug suspension formulation. The results from this study suggest the requirement for potential use of candesartan as self-nanoemulsifying drugdelivery systems.