Background/Objectives: Trans-resveratrol (Res) has been reported to possess many biological activities, including neuroprotective effects, owing to its anti-inflammatory and antioxidant properties. However, Res has very low water solubility, which limits its therapeutic application. In this work, we formulated water-soluble micellar formulations incorporating Res using polyethylene glycol monostearate (stPEG). Methods: These formulations (stPEG/Res) were developed using five types of stPEG containing 10, 25, 40, 55 and 140 PEG repeat units. The formulations were characterized for Res content, water solubility, particle size, zeta potential, precipitation, biodistribution, and efficacy against neuronal and motor dysfunction in intracerebral hemorrhage (ICH). Results: Intravenous administration of stPEG40/Res, which demonstrated particle size, water solubility, and biodistribution properties suitable for intravenous administration, suppressed neurological and motor dysfunction following in a collagenase-induced ICH mouse model. These effects were inhibited by zinc protoporphyrin-9, an inhibitor of the antioxidant enzyme heme oxygenase-1, suggesting that Res contributes to antioxidant enzyme expression and anti-inflammatory activity. Conclusions: The stPEG/Res micellar formulation developed in this study may offer a promising therapeutic approach for ICH treatment.

Background/Objectives: Boron neutron capture therapy requires the efficient delivery of sufficient amounts of ¹⁰B to tumor cells. In this study, we evaluated a liposomal boron-delivery system based on the B5-TAT-lipopeptide, which contains five boronophenylalanine (BPA) residues within its peptide portion and is anchored to the liposomal membrane through a hydrophobic lipid moiety. Methods: B5-TAT-lipopeptide 5% liposomes with a particle size of approximately 100 nm were prepared, and boron delivery to CT26 murine colon carcinoma cells was evaluated. Results: At an exposure concentration of 25 ppm boron, B5-TAT-lipopeptide 5% liposomes achieved a cell-associated boron level of approximately 4.5 µg B per 1 × 10⁶ cells. Separately, sodium mercaptoundecahydro-closo-dodecaborate (BSH)-encapsulated B5-TAT-lipopeptide 5% liposomes achieved approximately 11 µg B per 1 × 10⁶ cells when evaluated at an exposure concentration of 50 ppm. Following thermal neutron irradiation, B5-TAT-lipopeptide 5% liposome-treated cells showed marked loss of clonogenic survival, with surviving fractions of approximately 0.12 and 0.01 after 15 and 45 min of irradiation, respectively. In the preliminary in vivo tolerability study, rapid intravenous administration of B5-TAT-lipopeptide 5% liposomes without encapsulated BSH at 10 mg B/kg resulted in the death of all treated mice within 5–10 min, whereas no mortality occurred following the administration of phosphate-buffered saline (PBS), free BSH, or BSH-encapsulated PEGylated liposomes. Conclusions: These findings demonstrate substantial cell-associated boron delivery and neutron-induced clonogenic cell killing by B5-TAT-lipopeptide-modified liposomes while revealing a critical limitation in acute in vivo tolerability under the examined administration conditions.