FORMULATION AND EVALUATION OF BILAYERED FELODIPINE TRANSDERMAL PATCHES: IN VITRO AND EX VIVO CHARACTERIZATION

Objective: Felodipine (FD) is an effective Biopharmaceutics Classification System Class II calcium channel blocker mainly used in the management of hypertension and angina pectoris. It has poor solubility and low oral bioavailability (15%). To overcome these disadvantages and to maintain constant plasma concentration for maximum therapeutic activity, there is a need to design an alternative route, that is, transdermal route. The pharmacokinetic parameters make FD a suitable candidate for transdermal delivery. The present investigation consists of the study of in vitro and ex vivo skin flux of FD from bilayered transdermal patches. Methods: The patches were fabricated by solvent casting method using hydrophilic and hydrophobic polymer with different composition. Tween 80 incorporated as solubilizer, polyethylene glycol 600 as plasticizer, menthol, eucalyptus oil, and lemongrass oil used as permeation enhancers, respectively. The prepared transdermal drug delivery system was extensively evaluated for in vitro release, ex vivo permeation through pig ear skin, moisture content, moisture absorption, water vapor transmission, and mechanical properties. The physicochemical interaction between FD and polymers was investigated by Fourier-transform infrared (FTIR) spectroscopy. Results: All the formulations exhibited satisfactory physicochemical and mechanical characteristics. A flux of 35.2 μg/cm2 h, 27.9 μg/cm2 h, and 25.25 μg/cm2 h was achieved for optimized formulations containing lemongrass oil, eucalyptus oil, and menthol, respectively, permeation enhances. Values of tensile strength (0.0652±0.034 kg/mm²) and elongation at break (0.8749±0.0.0029% mm²) revealed that formulation F9 was strong but not brittle. Drug and excipients compatibility studies showed no evidence of interaction between the active ingredient and polymers. Conclusion: Bilayered FD transdermal patches could be prepared with required flux and suitable mechanical properties

EFFECT OF MOMORDICA CHARANTIA AND SYZYGIUM CUMINI EXTRACT ON SERUM ELECTROLYTES IN ALLOXAN INDUCED DIABETIC RATS

Objective: Diabetes is a group of disorders characterized by high blood glucose levels. Disturbances in serum electrolytes like sodium (Na+) and potassium (K+) are found in diabetes. The purpose of the study was to investigate the disturbances in concentrations of serum electrolytes in hyperglycemic crisis and the effect of syzygium cumini and momordica charantia standardized aqueous extracts on serum electrolytes (Na+and K+) in normal and diabetic rats.Methods: Diabetes is induced by intraperitoneal injection of alloxan at a dose of 120 mg/kg b. w in rats. Rats were divided into 5 groups (normal control, disease control, metformin, test 1 and test 2). In test groups 1 and 2, SASESC (standardized aqueous seed extract of syzygium cumini) and SAFEMC (standardized aqueous fruit extract of momordica charantia) were respectively administered orally to alloxan induced diabetic rats, and their serum electrolyte levels were observed at 1st, 4th, 7th and 14th days.Results: By the 14thday, the Na+ and K+ levels in groups 4 and 5 were almost normal. However, in group 3 (standard), Na+levels were relatively lower and K+ levels were relatively higher than groups 4 and 5 (test). In group 2 (disease control) as compared to group 1 (normal control), a decrease in Na+ and increase in K+ levels was observed even on day 14.Conclusion: Treatment with anti diabetic drugs like metformin, syzygium cumini (test-1), momordica charantia (test-2) restored the electrolyte levels almost back to normal over a period of study (14 d). There was significant (**P<0.01, *P<0.05) normalization of electrolyte levels in diabetic rats. It was concluded that syzygium cumini and momordica charantia showed better efficiency in restoring the electrolyte imbalance as compared to metformin during our study