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Objective: To evaluate the pulmonary retention, safety, and local drug concentration of Ranuncoli Ternati Radix extracts- ion sensitive in situ gels (RTRE-ISG). Methods: Sodium alginate as excipient, RTRE (70% ethanol) as solvent, it was swollen at room temperature using magnetic stirring to prepare RTRE-ISG which was administered via endotracheal tube to rats, The levels of inflammatory cytokines and fibrosis factors were detected in BALF to screen the relative safe priscription. Then using CY5.5 as fluorescent dye, the pulmonary retention of RTRE-ISG was evaluated with the aid of the small animal in vivo imaging system. In the end, the lung lavage was performed by using the improved alveolar lavage technique and the local drug concentration was determined. Results: The safety of RTRE-ISG prepared by 1% sodium alginate was better, the retention time in lung was 120-144 h revealed by fluorescence in vivo imaging system. The results showed that the release of drug reached to a peak of 5.24 μg/mL in 5 h after administration and 0.08 μg/mL in 144 h after administration. Conclusion: RTRE-ISG was good safety with the retention time in lung more than 120 h, which is a nevol sustained preparation of Chinese materia medica for the treatment of pulmonary tuberculosis.
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Objective:To prepare N-trimethyl chitosan (TMC)-coated sparfloxacin (SL) nanoliposomes in situ gels(ISG)and in-vestigate the drug release in vitro.Methods:SL liposomes were prepared by a pH gradient method , and then homogenized to nanolipo-somes by high pressure .TMC was used as the coating material to prepare TMC-coated SL nanoliposomes .Poloxamer 407 was used as the gel base, and the optimal amount was selected according to the gelation temperature .TMC-coated SL nanoliposomes ISG was pre-pared using a cold method , and the morphology , size, zeta potential and entrapment efficiency of TMC-coated SL nanoliposomes were studied.A membraneless model was used to study the drug release in vitro, and the result was compared with that of TMC-coated SL nanoliposomes.Results:The optimal amount of poloxamer 407 in the formula was 25%, and the gelation temperature was 23.6℃in the artificial tears and 33 .5℃in the diluted artificial tears .The morphology of TMC-coated SL nanaoliposomes in the ISG was spherical with the mean diameter of (96.8 ±1.5) nm, zeta potential of (46.2 ±1.4) mV and entrapment efficiency of (76.6 ±2.4) %, and the indices had no significant difference when compared with those of TMC-coated SL nanoliposomes .Both the drug release in vitro and gel dissolution profile of TMC-coated SL nanoliposomes ISG exhibited the characteristics of zero-order kinetics, and compared with that of TMC-coated SL nanoliposomes , the sustained release property of the ISG was more significant .Conclusion:TMC-coated SL nanoli-posomes ISG has promising gelation temperature and notable sustained release property .
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Objective:To prepare and evaluate Shenhuang vaginal thermosensitive in situ gels. Methods:Shenhuang vaginal ther-mosensitive in situ gels( SHV-TISG)were prepared with poloxamer 407 and poloxamer 188 as the materials. The viscosity change at different temperatures and the gelation temperature of SHV-TISG and SHV-TISG diluted by stimulant vaginal fluid were measured,the in vitro drug release of the preparation was evaluated by a membraneless diffusion method,and the safety of SHV-TISG was detected by vaginal irritation test. Results:The preparation showed the vaginal injectability and gelationability in vivo without vaginal irritation. Gel erosion was the principal mechanism of the drug release from the gels. Conclusion:The preparation of SHV-TISG is feasible in tech-nique,and the properties meet the requirements of vaginal topical use.
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OBJECTIVE: To optimize the formulation of the lutein thermosensitive in situ gels by using central composite design-response surface methodology, and study the drug release in vitro. METHODS: Gelation temperature was served as the indicator. The influences of the amounts of Poloxamer 407 and Poloxamer 188 on the gelation temperature were investigated. Central composite design-response surface method was used to optimize the prescription. The drug release profile of the preparation was investigated with a membrane-less dissolution model. RESULTS: The amounts of Poloxamer 407 and Poloxamer 188 had quantitative relationships with the gelation temperature. The optimum prescription was as follows: the mass concentration of P407 was 0.21 g · mL-1, and the mass concentration of P188 was 0.03 g · mL-1. The dissolution and drug release of the gels followed zero-order kinetics equation. CONCLUSION: Central composite design-response surface methodology can be applied to optimize the formulation of the lutein thermosensitive in situ gels.