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Casein-based micelles: a novel vector for delivery of the poorly soluble anticancer drug, flutamide? “Casein polymeric micelles are desirable nanobiotechnology materials for future applications in genomics, proteomics, biomedical and bioanalytical areas together with being nanovehicles for hydrophobic bioactives.” Keywords: casein micelles n flutamide nanoparticles n polymeric micelles

Polymeric micelles Polymeric micelles (PMs) are nanoscopic delivery systems (15–100 nm) formed through self assembly of amphiphilic copolymers. Since their hydrophilic shell sterically suppress opsonization by blood components, PMs are capable of evading non-specific capture by the reticulo­ endothelial system (RES) resulting in prolonged circulation times [1]. PM size should be large enough for extravasation from normal vessel walls and renal excretion. Moreover, this size should be small for extravasation from tumor blood vessels. In solid tumors, the enhanced permeability and retention effect may be due to increased vascularity and absence of effective lymphatic drainage. All these factors warrant the passive targeting of PM, while passive targeting is also the basis of active targeting [1,2]. PMs intended for use as drug-delivery systems should be stable to withstand early dissociation and release after entry into the bloodstream. They should provide sufficient time for drug-delivery and hence accumulation in the target zone. Their stability depends on critical micelle concentration values of micelle forming compounds [3,4]. Most micelles only exist above their critical micelle concentration. The large dilution in the bloodstream will tend to dissociate these nanoparticles after administration. Thus, their stability is a serious problem when used as drug carriers that requires cross-linking of their shells or cores [3].

and hydrophilic domains. The aS1‑CAS has a strongly acidic peptide bond together with the highly charged N-terminal region of b-CAS. CAS micelles are composed of four phosphoproteins held by hydrophobic interactions and by bridging of the nano-calcium phosphates that are bound to phosphorylated serine residues of CAS side chains. The CAS micellular surface is covered with k-CAS, which provides a charged surface layer stabilizing the micelles through electrostatic and steric repulsion [5]. In a recent study, CAS nanoparticles were used to encapsulate the anticancer drug, flutamide (FLT).

Casein micelles Caseins (CAS), the famous milk proteins, are amphiphilic proteins that self-assemble into stable micelles in aqueous solutions [5,6]. Casein proteins have distinct hydrophobic

CAS-flutamide nanoparticles FLT is an effective antitumor drug used in androgen-dependent prostate cancer, with a poor aqueous solubility and low oral bioavailability [7,8]. FLT was selected to prepare prolonged release nanoparticles owing to its fast clearance rate and the significant fluctuation in its bioavailability. The obtained CAS–FLT micelles were spherical with a particle size of

Casein-based micelles: a novel vector for delivery of the poorly soluble anticancer drug, flutamide?

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