The use of amorphous drug delivery systems is an attractive approach to improve the\nbioavailability of low molecular weight drug candidates that suffer from poor aqueous solubility.\nHowever, the pharmaceutical performance of many neat amorphous drugs is compromised by their\ntendency for recrystallization during storage and lumping upon dissolution, which may be improved\nby the application of coatings on amorphous surfaces. In this study, hot melt coating (HMC) as a\nsolvent-free coating method was utilized to coat amorphous carvedilol (CRV) particles with tripalmitin\ncontaining 10% (w/w) and 20% (w/w) of polysorbate 65 (PS65) in a fluid bed coater. Lipid coated\namorphous particles were assessed in terms of their physical stability during storage and their drug\nrelease during dynamic in vitro lipolysis. The release of CRV during in vitro lipolysis was shown to\nbe mainly dependent on the PS65 concentration in the coating layer, with a PS65 concentration of 20%\n(w/w) resulting in an immediate release profile. The physical stability of the amorphous CRV core,\nhowever, was negatively affected by the lipid coating, resulting in the recrystallization of CRV at the\ninterface between the crystalline lipid layer and the amorphous drug core. Our study demonstrated\nthe feasibility of lipid spray coating of amorphous CRV as a strategy to modify the drug release from\namorphous systems but at the same time highlights the importance of surface-mediated processes for\nthe physical stability of the amorphous form.
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