Optimized Formulation F4 Research Articles

Formulation and Evaluation of Gastro Retentive Drug Delivery System for Ofloxacin

The purpose of this investigation was to prepare a gastroretentive drug delivery system of Ofloxacin. Ofloxacin is a fluoroquinolone antibacterial which acts by inhibiting the topoisomerase enzyme which is essential in the reproduction of the bacterial DNA. It is highly soluble in acidic media and precipitates in alkaline media thereby losing its solubility. Hence, a gastroretentive system was developed to enhance the bioavailability by retaining it in the acidic environment of the stomach. Different formulations were formulated using various concentrations of hydroxy propyl methyl cellulose, sodium carboxy methyl cellulose, sodium bicarbonate and citric acid. The formulations were evaluated for quality control tests and all the physical parameters evaluated are within the acceptable limits of Indian Pharmacopoeia. All the formulations were subjected to in-vitro dissolution studies and compared with the marketed formulation. The floating lag time was below 15 seconds for all the formulations except F1 and F2. The floating duration was found to be more than 24 hours in all except F1, F2 and F10. Formulations F7 and F8 were used to study the effect of sodium bicarbonate and formulations F9 and F10 for the effect of hardness on the drug release. Drug release kinetics was studied for prepared formulations and optimized formulation F5 was found to follow zero order kinetics with r2 =0.993. The statistical analysis of the parameters of dissolution data obtained before and after storage for 3 months at 25°C/ 60%RH and 40°C/75%RH showed no significant change indicating the two dissolution profiles were similar.

Investigation of true nanoemulsions for transdermal potential of indomethacin: characterization, rheological characteristics, and ex vivo skin permeation studies

The aim of the present study was to investigate the potential of true nanoemulsions for transdermal delivery of indomethacin. Thermodynamically stable true nanoemulsions were characterized for morphology using transmission electron microscopy (TEM), droplet size, rheological characteristics, and refractive index. The rheological behavior for all true nanoemulsions was found to be Newtonian as viscosity was unchanged by increasing the rate of shear. The ex vivo skin permeation studies were performed using Franz diffusion cell with rat skin as permeation membrane. The ex vivo skin permeation profile of optimized formulation was compared with marketed Indobene gel and nanoemulsion gel. Significant increase in permeability parameters was observed in nanoemulsion formulations (P < 0.05). The steady-state flux (Jss) and permeability coefficient (Kp) for optimized nanoemulsion formulation were found to be 73.96 ± 2.89 μg/cm2/h and 1.479 × 10−2 ± 0.289 × 10− 2 cm/h, respectively, which were significant compared with Indobene gel and nanoemulsion gel (P < 0.05). Enhancement ratio (Er) was found to be 7.88 in optimized formulation F6 compared with other formulations. These results suggested that nanoemulsions can be used as potential vehicles for improved transdermal delivery of indomethacin.

Development and In-Vitro Evaluation of Betahistine Hydrochloride microspheres by Emulsification Solvent Evaporation Method

The formulation of floating microspheres of Betahistine hydrochloride by the o/w emulsification and solvent evaporation method in the presence of tween 80 as an emulsifying agent. The influence of formulation factor Drug: Polymer ratio on particle size, encapsulation efficiency and invitro release characteristics of the microspheres were investigated. The microspheres have been analyzed for their size, drug loading capacity and drug release study. Spherical and smooth surfaced microspheres with desired encapsulation efficiencies were obtained. Slow drug release from microspheres observed up to 12 h. for formulation F4, F5. Optimized formulation F4 was evaluated for FTIR, DSC, SEM. DSC and FTIR studies showed that the nature of pure drug Betahistine hydrochloride remains unaffected till the completion of process of microspheres formation. SEM photographs showed that the Floating microspheres were spherical in nature with smooth surface and uniform distribution of the drug within the microsphere.&#x0D; Keywords: