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OBJECTIVE: To develop a nonoxynol-9-loaded thermorevesible gel for vaginal administration and evaluate its rheological properties and in vivo retention capacity.
ABSTRACT
Objective: To establish a RP-HPLC method for determining the plasma concentration of nonoxynol-9 and to apply the method in studying the pharmacokinetics of nonoxynol-9 in healthy female rabbits. Methods: A single dose of nonoxynol-9 (64 mg to each animal) was given to 6 healthy female rabbits (weighing 2. 0-2. 2 kg) via vagina. The plasma samples were collected and the concentrations of nonoxynol-9 were determined by RP-1-IPLC method using DiamonsilTM ODS column (200 mm × 4.6 mm,5 μm) and mobile phase of methanol-water (95 : 5) at a flow rate of 1. 0 ml/min. The excitation and emission wavelengths were 226 nm and 300 nm, respectively. The column temperature was 30°C. The pharmacokinetic parameters were calculated. Results: The calibration curve of nonoxynol-9 showed good linearity over the range of 0. 05-5. 00 μg/ml; both the intra- and inter-day precisions were lower than 10%. The recovery rates at three concentrations (0. 10,0. 50, and 2. 00 μg/ml) were (101. 67 ± 8. 12) % ,(100. 84±5. 42) % ,and (100. 29±3. 81) % ,respectively. The main pharmacokinetic parameters of nonoxynol-9 were as following: t1/2 (3. 75 ± 0. 87) h, t max (3. 2 ± 0. 4) h,Cmax (2. 75 ± 0. 32) μg/ml, AUC0-12 (12.72±2.14) μg. h ml-1 ,AUC0-∞(15. 05± 2. 84)ug . h ml-1 ,and MRT (6. 85± 1. 13) h. Conclusion: The established method is convenient, sensitive and specific, and can be used for determination of plasma nonoxynol-9 concentration and for its pharmacokinetic studies in rabbits.
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Objective To establish the mouse model for human papillomavirus types 16, 45 and 58 by the corresponding pseudovirions. Methods The 293FT cells were co-transfected with eodon-modified HPV eapsids genes together with a reporter plasmid containing the luciferase gene. The cells were collected and lysed, then the pseudovirus was collected and the titration was performed. The mouse was subcutaneous-ly injected with Depo-Provera. After 4 d and intravaginally injected with nonoxynol-9, and 6 h later pseud-oviruses were inoculated in intravaginal. After 7 d, the mouse was instilled luciferin substrate intravaginally, and the expression level of the lueiferase gene was detected by the in vivo Imaging System (IVIS). Results Three types (HPV16, HPV45 and HPV58) of pseudoviruses had been produced and the titer was 3.7×108 TU/ml, 1.5×108 TU/ml and 1.2×108 TU/ml, respectively. The luminescent regions could be detected in the mice which were infected with the pseudovirions, the luminescent signal intensity for types 16,45 and 58 was 1.779×106p/s, 5.738×105×p/s and 1.829×106p/s, respectively. Conclusion The mouse models for HPV16, 45 and 58 have been successfully established based on pseudovirions, which will be very useful for the research of HPV infection intervention, the evaluation of HPV vaccines and the screening of the prophylactic agents.
ABSTRACT
Spermicidal effect of Jieze No. 1 (JZ1) in combination with nonoxynol-9 (N-9) was examined in vitro. The minimum spermicidal concentration of JZ1 decoction, N-9 and their mixture solution in 20 s and 3 min were examined by improved spermicidal test of Sander-cramer in vitro.The percentages of progressively moving spermatozoa, moving spermatozoa and viable spermatozoa were also observed 20 s, 3 min and 30 min after the addition of the liquid medicine. Our results showed that sperms did not recover their activities in a revival test when the minimum spermicidal concentration of either JZ1 decoction, or N-9, or the mixed solution of the two agents, was used.N-9 (JZ1 in the mixed group) showed significant differences in the percentages of progressively moving spermatozoa, moving spermatozoa, and visible spermatozoa in 20 s, 3 min, and 30 min,when compared with N-9 alone (P＜0.01). We are led to conclude that JZ1 decoction can improve N-9 spermicidal action in vitro, and when used in combination with N-9, it has synergic effect.