Drug delivery amphotericin

Yu, B. G, T. Okano, K. Kataoka, and G Kwon. 1998. Polymeric micelles for drug delivery solubilization and hemolytic activity of amphotericin BJ. Control. Rel.53 131-136. 

Polymeric micelles formed by Pluronics, PEG phospholipid conjugates, PEG-b-polyesters, or PEG-b-poly-L-amino acids were proposed for drug delivery of poorly water-soluble compounds, such as amphotericin B, propofol, paclitaxel, and photosensitizers [77,86,87]. It was also emphasized that using polymeric micelles can significantly increase the drug transport into the brain. 

In pharmaceutical preparations, soybean oil emulsions are primarily used as a fat source in total parenteral nutrition (TPN) regimens. Although other oils, such as peanut oil, have been used for this purpose, soybean oil is now preferred because it is associated with fewer adverse reactions. Emulsions containing soybean oil have also been used as vehicles for the oral and intravenous administration of drugs drug substances that have been incorporated into such emulsions include amphotericin, " diazepam, retinoids, vitamins, poorly water-soluble steroids, fluorocarbons, and insulin. In addition, soybean oil has been used in the formulation of many drug delivery systems such as liposomes, microspheres, dry emulsions, self-emulsifying systems, and nanoemulsions and nanocapsules. ... 

Nephrotoxicity is best minimized by limiting the cumulative dose and avoiding concomitant administration of other nephrotoxins, particularly cyclosporine. Additionally, providing hydration with a high sodium diet and 1 L intravenous 0.9% sodium chloride daily appears to reduce toxicity. Mannitol infusion to induce an osmotic diuresis has not been protective. Lastly, several liposomal amphotericin B formulations are now available and have been reported to reduce nephrotoxicity by enhancing drug delivery to sites of infection and thereby reducing exposure of mammalian cell membranes. ... 

Yu BG, Okano T, Kataoka K, Kwon GS. Pol3uneric micelles for drug delivery Solubilization and haemol3d ic activity of amphotericin B. J Contr Rel 1998 53 131-136. 

Currently, toxic effects of AmB have been largely ameliorated with the advent of lipid formulations, in these formulations, deoxycholate has been replaced by other Upids that mask AmB from susceptible tissues, thus reducing toxicity and facilitating its preferential uptake by reticuloendothelial cells. Thus, this drug delivery results in increasing efficacy and reduced toxicity. Three Upid-associated formulations of amphotericin are commercially available Uposomal amphotericin B (AmBisome), amphotericin B lipid complex (Abelcet), and amphotericin B colloidal dispersimi (Amphocil). These compoimds have been considered between the most striking advances in Leishmania therapy [52],... 

Drug delivery technology - modulating the clinical profile of amphotericin B... 

The delivery of drugs to the RES (also referred to as the mononuclear phagocyte system) is an area where liposomes have a potential for success. They were successfully used in the delivery of antimonial drugs to treat experimental leishmaniasis infection [313], Very good results were obtained in the treatment of systemic fungal infections in cancer patients using liposomal amphotericin B [314, 315]. 

Perlin DS. Amphotericin B cochleates a vehicle for oral delivery. Curr Opin Investig Drugs 2004 5(2) 198. 

A commercial product based on conventional liposomes has been introduced for the parenteral delivery of the anti-fungal drug, amphotericin B, which is poorly tolerated in conventional formulations. AmBisome, a liposomal formulation of amphotericin B, comprises SUV of diameter 50-100 ran. Two other lipid-based formulations of amphotericin B have also recently been commercially introduced ... 

Lee MD, Hess MM, Boucher BA, Apple AM. Stability of amphotericin B in 5% dextrose injection stored at 4 or 25°C for 120 hours. Am J Hosp Pharm 1994 51 394-396. Kowaluk EA, Roberts MS, Polack AE. Interactions between drugs and intravenous delivery systems. Am J Hosp Pharm 1982 39 460 67. 

---