A high-payload ascorbyl palmitate (AP) nanosuspension (NS) was designed to improve skin delivery following topical application. The AP-loaded NS systems were prepared using the bead-milling technique, and softly thickened into NS-loaded gel (NS-G) using hydrophilic polymers. The optimized NS-G system consisted of up to 75 mg/mL of AP, 0.5% w/v of polyoxyl-40 hydrogenated castor oil (Kolliphor^® RH40) as the suspending agent, and 1.0% w/v of sodium carboxymethyl cellulose (Na.CMC 700 K) as the thickening agent, in citrate buffer (pH 4.5). The NS-G system was embodied as follows: long and flaky nanocrystals, 493.2 nm in size, −48.7 mV in zeta potential, and 2.3 cP of viscosity with a shear rate of 100 s⁻¹. Both NS and NS-G provided rapid dissolution of the poorly water-soluble antioxidant, which was comparable to that of the microemulsion gel (ME-G) containing AP in solubilized form. In an ex vivo skin absorption study using the Franz diffusion cell mounted on porcine skin, NS-G exhibited faster absorption in skin, providing approximately 4, 3, and 1.4 times larger accumulation than that of ME-G at 3, 6, and 12 h, respectively. Therefore, the high-payload NS makes it a promising platform for skin delivery of the lipid derivative of ascorbic acid.

The aim of this study was to design a poorly water-soluble electrostatic nanocomplex of semaglutide (SMG) with protamine sulfate (PS) and zinc ions (Zn) for prolonged subcutaneous delivery. Complexation of SMG with the cationic peptide PS increased the lipophilicity (logP) proportionally from −4.7 to 0.3, particularly in the presence of Zn. The optimized nanocomplex exhibited spherical morphology, an amorphous state, a particle size of 196.0 nm, and a zeta potential of −45.7 mV. In an in vitro dissolution test under sink conditions, native SMG showed rapid drug release with 98% dissolution within 24 h. In contrast, the nanocomplexes showed markedly delayed release, with a concentration-dependent relationship between PS/Zn contents and SMG release rate, exhibiting 19% drug release over 7 days in the optimized formula. These findings suggest that the proposed nanocomplex is a promising system for long-acting injectable delivery of SMG, potentially enhancing patient compliance in patients with obesity or type 2 diabetes.

This study designs stable fast-disintegrating oral granules (FDGs) of volatile liquid essential oils (cinnamon, lemon, rose, and peppermint oils) for olfactory rehabilitation. By adsorbing liquid-type essential oils onto colloidal silicon dioxide (1:1 w/w) and incorporating olive oil (1:1:0.25 w/w) as a volatile restrainer, the retention of major odorants—cinnamaldehyde, citral, phenethyl alcohol, and menthol—in cinnamon, lemon, rose, and peppermint oils, respectively, was markedly improved after 12 h of exposure at 40 °C. Then, free-flowing FDG system was formulated with sugar alcohols (mannitol, xylitol, and sorbitol), low substituted hydroxypropyl cellulose, and magnesium stearate, exhibiting rapid spreading and disintegration (82% of cinnamaldehyde, citral, phenethyl alcohol, and menthol for 8 weeks under 25 °C/65% relative humidity (RH) conditions. In an in vitro volatilization test, major odorants were effectively volatilized from artificial saliva-wetted FDGs within 90 min depending on the volatility of each constituent. Therefore, this novel oral FDG system is expected to be a promising alternative for olfactory training for neurogenic smell dysfunction, providing enhanced storage stability, precise dosing, and patient compliance.

Tegoprazan (TPZ) is a promising potassium-competitive acid blocker, but its pH-dependent low solubility often leads to erratic oral absorption. Although several hydrophilic polymer-based amorphous solid dispersions have been attempted to enhance dissolution, they often suffer from thermodynamic instability or rely on complex, solvent-mediated manufacturing processes. Herein, to enhance dissolution and oral absorption, a crystalline drug-loaded melt granulation (MG) system using D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) was fabricated while maintaining stable physicochemical properties. MGs were prepared via a solvent-free, hot-melt process by optimizing the type of solid surfactant carrier, the ratio of drug to solid surfactant, and the type and ratio of flow-enhancing excipients. The optimized composition was TPZ:TPGS:microcrystalline cellulose = 1:2:4 (w/w/w). Solid-state analyses revealed that TPZ was uniformly dispersed within the granules while retaining its crystalline form. Compared to the raw drug, the MG showed remarkably faster and higher dissolution across both acidic and neutral media. Under long-term (25 °C/60% RH) and accelerated storage conditions (40 °C/75% RH) for 24 weeks, MG exhibited robust physicochemical stability, showing no drug degradation, changes in dissolution behavior, or crystalline alterations. Moreover, in a pharmacokinetic evaluation in Sprague–Dawley rats, MG provided marked absorption enhancement, yielding over 1.8-fold increases in exposure compared to the raw material. Consequently, the crystalline drug-loaded TPGS-based MG represents a promising strategy for improving the oral delivery of TPZ.

This study investigated the antimicrobial potential of Coptis chinensis rhizome extract against key oral pathogens and evaluated the safety and clinical efficacy of a CCE-loaded mouthwash. CCE exhibited broad-spectrum bactericidal activity, with low minimum inhibitory concentrations (0.002–0.008%) and minimum bactericidal concentrations (0.004–0.016%) against Streptococcus mutans, Aggregatibacter actinomycetemcomitans, and Porphyromonas gingivalis. Time-kill kinetics revealed that CCE promptly eradicated Porphyromonas gingivalis. To balance antimicrobial potency and sensory acceptability, specifically the extract’s bitterness, we established the CCE concentrations in the mouthwash at 0.01% and 0.02% (w/v). Preclinical safety evaluations in animal models, including oral mucosal irritation and skin sensitization tests, confirmed the biocompatibility of 0.02% CCE, yielding “None” and “Non-sensitizer” ratings, respectively. Furthermore, a four-week, randomized, double-blind clinical trial (n = 73) revealed that 0.02% CCE mouthwash substantially reduced halitosis-inducing volatile sulfur compounds (hydrogen sulfide by 59.5% and methyl mercaptan by 50.0%). Significant improvements were also observed in the Plaque Index (55.2% reduction), Gingival Index (52.0% reduction), and Bleeding on Probing (77.3% reduction), with no adverse effects. These findings provide preliminary evidence that CCE mouthwash improves halitosis-related parameters and gingival indices in adults with self-reported halitosis, though further research is required to evaluate its long-term impact on broader periodontal disease states.