We have previously shown that Trapa japonica fruit extract (TJE) as well as its fermented extract (FTJ) can be potentially used to treat alopecia. In the current study, a newly synthesized peptide (PEP) was detected in an active compound isolated from FTJ. Several biological assays were conducted to verify the antiaging effects of TJE, FTJ, and PEP on the skin. We examined the effects of TJE, FTJ, and PEP on cell viability, collagen synthesis, and inhibition of mRNA expression of matrix metalloproteinases (MMPs), induced by tumor necrosis factor alpha (TNF-α), in human dermal fibroblasts (HDFs). In addition, a wound-healing assay of the human keratinocyte cell line (HaCaT) and a clinical study of antiaging activity were conducted. The findings confirmed that PEP exerted an effect on cell proliferation in a dose-dependent manner. Treatment with TJE, FTJ, and PEP increased collagen synthesis but inhibited TNF-α-induced mRNA expression of MMPs. Compared with TJE and FTJ, PEP promoted a significant level of wound recovery in HaCaT cells and also exhibited antiaging effect, as demonstrated by a clinical study. These results suggest that PEP shows potential as a skin antiaging cosmetic product.

This study aims to examine the contribution of nanoporous silica entrapped lipid-drug complexes (NSCs) in improving the solubility and bioavailability of dutasteride (DUT). An NSC was loaded with DUT (dissolved in lipids) and dispersed at a nanoscale level using an entrapment technique. NSC microemulsion formation was confirmed using a ternary phase diagram, while the presence of DUT and lipid entrapment in NSC was confirmed using scanning electron microscopy. Differential scanning calorimetry and X-ray diffraction revealed the amorphous properties of NSC. The prepared all NSC had excellent flowability and enhanced DUT solubility but showed no significant difference in drug content homogeneity. An increase in the lipid content of NSC led to an increase in the DUT solubility. Further the NSC were formulated as tablets using D-α tocopheryl polyethylene glycol 1000 succinate, glyceryl caprylate/caprate, and Neusilin®. The NSC tablets showed a high dissolution rate of 99.6% at 30 min. Furthermore, NSC stored for 4 weeks at 60 °C was stable during dissolution testing. Pharmacokinetic studies performed in beagle dogs revealed enhanced DUT bioavailability when administered as NSC tablets. NSC can be used as a platform to develop methods to overcome the technical and commercial limitations of lipid-based preparations of poorly soluble drugs.

Background Owing to the limited amount of research, there are no nanoparticle-based anticancer agents that use hydrophilic drugs. Therefore, we developed irinotecan-loaded self-agglomerating hyaluronan nanoparticles (ISHNs). While irinotecan has high hydrophilicity, the resulting nanoparticle should possess high anticancer drug-loading capacity and allow selective targeting of the cluster of differentiation 44 (CD44) protein, which is overexpressed on the surface of tumor cells. Results The ISHNs were successfully made with hyaluronan (HA) as a targeting moiety, FeCl3 as a binder, and D-glutamic acid (GA) as a stabilizer. The ISHNs self-agglomerated via chelating bonding and were lyophilized using a freeze dryer. The particle diameter and zeta potential of the ISHNs were 93.8 ± 4.48 nm and − 36.3 ± 0.28 mV, respectively; a relatively narrow size distribution was observed. The drug fixation yield and drug-loading concentration were 58.3% and 1.75 mg/mL, respectively. Affinity studies revealed a tenfold stronger targeting to H23 (CD44+) non-small-cell lung cancer (NSCLC) cells, than of A549 (CD44−) cells. Conclusion We developed irinotecan-loaded ISHNs, which comprised irinotecan hydrochloride as a water-soluble anticancer agent, HA as a targeting moiety, FeCl3 as a binder for self-agglomeration, and GA as a stabilizer; HA is a binding material for CD44 in NSCLC cells. Owing to their ease of manufacture, excellent stability, non-cell toxicity and CD44-targeting ability, ISHNs are potential nanocarriers for passive and active tumor targeting.

The aim of this study was to develop a single-layered version of commercially available Twynstar® (Telmisartan + Amlodipine) double-layered tablets to improve the dosing convenience. A quality-by-design approach was applied to develop the single-layered version. To evaluate the range and cause of risks for a single-layered tablet in the formulation design research, we used the tools of the risk assessment, initial risk assessment of preliminary hazard analysis and main risk assessment of failure mode and effect analysis to determine the parameters affecting formulation, drug dissolution, and impurities. The critical material attributes were the stabilizer and disintegrant, and the critical process parameters were the wet granulation and tableting process. The optimal range of the design space was determined using the central composite design in the wet granulation and tablet compression processes. The stabilizer, kneading time, and disintegrant of the wet granulation were identified as X values affecting Y values. The compression force and turret speed in the tablet compression were identified as X values affecting Y values. After deciding on the design space with the deduced Y values, the single-layered tablets were formulated, and their dissolution patterns were compared with that of the double-layered tablet. The selected quality-by-design (QbD) approach single-layered tablet formulated using design space were found to be bioequivalent to the Twynstar® double-layered tablets. Hence, the development of single-layered tablets with two API using the QbD approach could improve the medication compliance of patients and could be used as a platform to overcome time-consuming and excessive costs and the technical and commercial limitations related to various multi-layered tablets.

This study aimed to optimize and evaluate self-assembled liquid crystalline nanoparticles (SALCs) prepared from phospholipids and oleic acid for enhancing the absorption of ω-3s. We explored the structure and optimal formulation of SALCs, which are composed of ω-3 ethyl ester (ω-3 EE), phospholipids, and oleic acid, using a ternary diagram and evaluated the improvement in ω-3 dissolution, permeation, and oral bioavailability. The in vitro dissolution and pharmacokinetics of ω-3 SALCs were compared with those of Omacor soft capsules (as the reference). The shape of the liquid crystal was determined according to the composition of phospholipids, oleic acids, and ω-3s and was found to be in cubic, lamellar, and hexagonal forms. The dissolution rates of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) obtained from ω-3 SALCs were 1.7 to 2.3-fold higher than those of the Omacor soft capsules. Furthermore, a pharmacokinetic study in male beagle dogs revealed that ω-3 SALCs increased the oral bioavailability of ω-3 EE by 2.5-fold for EPA and 3.1-fold for DHA compared with the reference. We found an optimal formulation that spontaneously forms liquid crystal-based nanoparticles, improving the bioavailability of EPA and DHA, not found in the existing literature. Our findings offer insight into the impact of nanoparticle phase on the oral delivery of oil-soluble drugs and provide a novel ω-3 EE formulation that improves the bioavailability of EPA and DHA.