Abstract
The efficiency of water-in-oil (W/O) and gelatin-microsphere-in-oil (W/O-G) emulsions as drug delivery systems for achieving specificity into lymphatics was evaluated in the rat stomach. Following injection into the stomach wall, radioactivities of131I-labeled o-iodohippuric acid (IH, watersoluble model compound) and [14C]tripalmitin (TP, tracer of oil) in blood, regional lymph nodes, thoracic lymph, and stomach were determined. Since increased transfer of TP indicated the facilitation of lymphatic transport of IH following injection of W/O and W/O-G emulsions, the existence of a special transport mechanism through which drug and oil are delivered together was confirmed for this injection site. W/O and W/O-G emulsions increased the concentration-time curve (AUC) of IH in the regional lymph nodes (1.7 and 5.5 times that of aqueous solution injection, respectively), so the improvement of bioavailability was accomplished. In addition, a prolonged release of IH and decrease of its maximum blood concentration were obtained following injection of W/O-G emulsion. These results suggest that W/O and W/O-G emulsions satisfy many of the criteria of an ideal drug delivery system for cancer chemotherapy. An abundant supply of lymphatic vessels in the stomach wall exhibited the efficiency of these delivery systems more clearly than did thigh muscle.
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Hashida, M., Takahashi, Y., Muranishi, S. et al. An application of water-in-oil and gelatin-microsphere-in-oil emulsions to specific delivery of anticancer agent into stomach lymphatics. Journal of Pharmacokinetics and Biopharmaceutics 5, 241–255 (1977). https://doi.org/10.1007/BF01065398
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DOI: https://doi.org/10.1007/BF01065398