The aim of our study was to formulate a stable multiple emulsions containing two nitroimidazole derivates, metronidazole (MT) and ornidazole (OR), for vaginal therapy. MT and OR were located internal and external phases of multiple emulsion, respectively, and the in vitro release studies were realized in phosphate (pH 7) and lactate buffer (pH 4.5) solutions to investigate better the effect of pH and location of active substance on the release. The imaging studies were realized in rabbits following labeling MT and OR with Technethium-99m ( 99m Tc) to evaluate the in vivo absorption characteristics. The percentage of MT and OR released from the multiple emulsions in alkaline media were 3.2-and 2.8-fold greater than that observed in acidic media, respectively, when they were introduced in the internal phase of the multiple emulsions. The absorption rate of MT from vaginal epithelium was faster than OR. We observed that especially in alkaline medium a high release was found that was convenient for the vaginal infections seen in the alkaline pH. We concluded that W/O/W multiple emulsions were locally effective in vagina and they could be introduced as a new drug carrier system for vaginal delivery.

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The unique properties like rich blood supply and the large surface area makes vagina an important area for systemic drug delivery (15). The advan-ABSTRACT: The aim of this study was to compare the bone uptake of alendronate sodium (ALD) from vaginal suppositories prepared with massa estarinum AB (ME) and polyethylene glycol 1500 (PEG) bases. For this purpose, ALD was radiolabeled with 99m Tecnetium Pertechnetate ( 99m Tc) by direct method. Radiochemical purity and stability of 99m Tc-ALD was performed with chromatographic studies. 99m Tc-ALD containing suppositories were prepared with ME and PEG bases. Physical properties of suppositories were evaluated. The physicochemical diffusion study was carried out to compare the release of ALD from different suppository bases. The bone uptake of 99m Tc-ALD was observed by gamma scintigraphy studies. 99m Tc-ALD containing suppositories were administrated to rabbits via vaginal route. The scintigraphic images were obtained with a gamma camera at different time intervals up to 240 minutes. According to our studies, radiochemical purity of 99m Tc-ALD was observed more than 95% up to 6 hours. At 240 minutes of physicochemical diffusion studies, released ALD has 0.620 ± 0.091 mm and 10.465 ± 0.651 mm diameter zone from ME and PEG base suppositories respectively. According to the gamma scintigraphy studies, although no bone uptake observed after ME suppositories application, rabbit's bones were clearly visible after PEG suppositories applied. The results of physicochemical diffusion and gamma scintigraphy studies were found compatible in each other.