In vivo disposition characteristics of succinylated (Suc-) proteins were studied after intravenous injection in mice in relation to their molecular characteristics as negatively charged macromolecules. Recombinant superoxide dismutase (SOD; molecular mass, 32 kDa), bovine serum albumin (BSA; molecular mass, 67 kDa), and bovine IgG (molecular mass, 150 kDa) were used to produce succinylated derivatives with different degrees of modification.111 In-labeled Suc-SODs were rapidly excreted into the urine with no significant hepatic uptake. In contrast, 111 In-Suc-BSA and Suc-IgG were significantly taken up by liver nonparenchymal cells via scavenger receptors (SRs) according to the degree of succinylation and the dose injected. Interestingly, highly succinylated BSAs exhibited significant accumulation in the kidney at higher doses when the hepatic uptake was saturated. Pharmacokinetic analysis demonstrated that the hepatic uptake of succinylated proteins depended on the molecular size and the estimated surface density of succinylated amino residues. Further analysis based on a physiological pharmacokinetic model, involving a saturable process with Michaelis-Menten kinetics, revealed that the surface density of negative charges was correlated with the affinity of larger succinylated proteins for the hepatic SRs. Thus, the present study has provided useful basic information for a therapeutic strategy and the molecular design of succinylated proteins for use as drug carriers and therapeutic agents per se for SR-mediated targeting in vivo.

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Leaves of an obscure plant “oxalis deppei” are so hydrophobic that showered water droplets are almost completely repelled and hardly remained on their surfaces. For this reason, surface configurations were investigated. On the live leaves, there formed protrusions somewhat similar to those observed on lotus leaves which are well known as super hydrophobic leaves. However, in winter, it was found that even dead leaves were hydrophobic also. Because leaf tissues were shriveled and dried half, heights of protrusions with sizes of 20-50 μm were low, and undulations of surfaces were gentle and smooth, and pitches of undulations were as large as 30-70 μm. It was thought that such gentle lens-like protrusions would be probably formed on versatile stainless-steel plates using lithography and wet chemical etching. For this reason, arrays of protrusions with a size of 20 μm, a pitch of 35 μm, and heights of 6-7 μm were formed, and change of hydrophobic properties were investigated. As a result, the hydrophobic properties were effectively improved by forming even such gentle and smooth protrusions. It was also clarified that contact angles were improved almost in proportion to etched depths.

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