الفهرس | Only 14 pages are availabe for public view |
Abstract Tetracycline Hcl loaded nanoemulsion (TC-NE) was prepared, characterized and stability was assessed. MDS from 32.33±3.81 to 101.5±9.86 nm.; size has 3 S/CoS ratios were 1:1, 1:2 and 2:1. PDI value (0.11± 0.01: 0.41± 0.07). ZP values ( -25.45±3.43 to -33.47±2.11 mV.) TEM showed spherical globules with uniform droplet size. Pharmacokinetics and pharmacodynamics of TC-Hcl powder and TC-NE were studied in rabbits following a single iv and oral dose (50 mg/kg b.wt). TC-NE had higher distribution volume V2 and slowly cleared Cl2 than TC- Hcl. Significant longer half-life for TC-NE than for TC-Hcl powder with calculated Cmax, achieved at prolonged calculated tmax in TC-NE than in TC-Hcl oral treated rabbits, respectively. A Significant higher AUC0-inf. (20.377 ± 1.4841 μg/ml.h and 11.056 ± 0.5835 μg/ml.h) at prolonged MRT (3.926 ± 0.4712 h. and 2.771 ± 0.2932 h.) and higher bioavailability in TC-NE than TC-Hcl, respectively. Some changes in histopathology, liver and kidneys function were observed with the two formulas. No difference in antibacterial and MIC between TC-NE than TC-Hcl. Conclusion: The nanoemulsion formulation improves both pharmacokinetis and pharmacodynamics and not affect the antibacterial efficacy as compared with TC-Hcl formula. This formulation can be useful for reduce the used dose to obtain the same serum concentration, reduce tissue effect and save cost of medication. Further studies are needed for clinical evaluation of the TC-Hcl formula. |