Abstract
BGP-15 is a Hungarian-developed drug candidate with numerous beneficial effects. Its potential anti-inflammatory effect is a common assumption, but it has not been investigated in topical formulations yet. The aim of our study was to formulate 10% BGP-15 creams with different penetration enhancers to ensure good drug delivery, improve bioavailability of the drug and investigate the potential anti-inflammatory effect of BGP-15 creams in vivo. Since the exact mechanism of the effect is still unknown, the antioxidant effect (tested with UVB radiation) and the ability of BGP-15 to decrease macrophage activation were evaluated. Biocompatibility investigations were carried out on HaCaT cells to make sure that the formulations and the selected excipients can be safely used. Dosage form studies were also completed with texture analysis and in vitro release with Franz diffusion chamber apparatus. Our results show that the ointments were able to reduce the extent of local inflammation in mice, but the exact mechanism of the effect remains unknown since BGP-15 did not show any antioxidant effect, nor was it able to decrease LPS-induced macrophage activation. Our results support the hypothesis that BGP-15 has a potential anti-inflammatory effect, even if it is topically applied, but the mechanism of the effect remains unclear and requires further pharmacological studies.
Highlights
BGP-15 is a nicotinic amidoxime derivative, a Hungarian-developed drug candidate, which was originally intended to alleviate neuro, nephro- and myelotoxic effects of different cytostatic preparations [1,2,3,4,5]
Since the exact mechanism of effect is still unknown of BGP-15, we aimed to evaluate the antioxidant effect and ability of BGP-15 to decrease macrophage activation
Texture analysis revealed that the compositions have different surfactants were formulated of BGP-15, and these compositions were adequate consistency; those formulations that contain sucrose esters have a slightly harder investigated from different aspects, such as texture analysis and in vitro release
Summary
BGP-15 is a nicotinic amidoxime derivative, a Hungarian-developed drug candidate, which was originally intended to alleviate neuro-, nephro- and myelotoxic effects of different cytostatic preparations [1,2,3,4,5]. BGP-15 has entered into clinical phase II in the indication of diabetes [1,7,8], but the determination of the proper indication is still ongoing as we still have little knowledge about the drug. As for this matter, the exact mechanism of the effect is still unknown, though many research groups are studying BGP-15. Farkas et al have formulated creams of BGP-15, though the indication was slightly different They investigated the photoprotective effect of the ointments by pretreating mice with the preparations, exposed the animals to direct UV radiation
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