In this study, we developed a lipid-coated hollow calcium phosphate (LCP) nanoparticle for the combined application of two chemotherapeutic drugs to human lung cancer A549 cells. Hydrophilic doxorubicin (DOX) was incorporated into the hollow structure of hollow calcium phosphate (HCP), and a lipid bilayer containing hydrophobic paclitaxel (PTX) was subsequently coated on the surface of HCP. The study on combinational effects demonstrated that the combination of DOX and PTX at a mass ratio of 12:1 showed a synergistic effect against A549 cells. The particle size, zeta potential, and encapsulation efficiency were measured to obtain optimal values: particle size was 335.0 3.2 nm, zeta potential -41.1 mV, and encapsulation efficiency 80.40%±2.24%. An in vitro release study indicated that LCP produced a sustained drug release. A549 cells had a better uptake of LCP with good biocompatibility. Furthermore, in vitro cytotoxicity experiment, apoptosis analysis, in vivo anti-tumor efficacy and protein expression analysis of Bax, Bcl-2, and Caspase-3 demonstrated that the co-delivery system based on LCP had significant synergistic anti-tumor activity. All conclusions suggested that LCP is a promising platform for co-delivery of multiple anti-tumor drugs.

Three novel monoterpenoid indole alkaloids gardflorine A (1), gardflorine B (2), and gardflorine C (3) were isolated from the leaves of Gardneria multiflora. Their structures, including absolute configurations, were established on the basis of spectroscopic methods (MS, UV, IR, 1D and 2D NMR) and circular dichroism experiments. All the compounds were evaluated for their vasorelaxant and acetylcholinesterase (AChE) inhibitory activities. Compound 1 exhibited potent vasorelaxant activity, with an EC₅₀ value of 8.7 μM, and compounds 2 and 3 showed moderate acetylcholinesterase (AChE) inhibitory activities, with IC₅₀ values of 26.8 and 29.2 μM, respectively.

Objectives: To address the critical limitations of current formulations that fail to simultaneously resolve indomethacin’s poor water solubility, susceptibility to gastric acid hydrolysis, and difficulty in balancing rapid onset with long-term sustained release, this study prepared solid dispersions via anti-solvent freeze-drying to improve drug dissolution, constructed oral buccoadhesive bilayer controlled-release tablets using direct powder compression, and elucidated the intrinsic relationships among polymer gel properties, swelling-erosion behavior, tablet integrity maintenance, and drug release mechanisms. Methods: Solid dispersions (SDs) were prepared by anti-solvent freeze-drying. Bilayer tablets (25 mg IND/tablet, 12.5 mg/layer) were fabricated via direct powder compression after optimizing disintegrants and polymer matrices. In vitro dissolution, surface pH, adhesion time, and adhesion strength were evaluated. Results: SDs enhanced dissolution by at least 30-fold in water and 2.4-fold at pH 6.8 within 2 h versus pure drug. Optimized bilayer tablets achieved 45% drug release at 20 min and 80% sustained release over 8 h, with surface pH of 6.8 ± 0.1, adhesion time of 8.3 ± 0.1 h, and adhesion strength of 57 ± 0.13 g. Conclusions: The physicochemical properties of polymeric excipients are critical for balancing drug release and mucoadhesion in buccal tablets. To achieve ideal controlled-release effects, in addition to focusing on the swelling and erosion characteristics of matrix-based tablets, the ability to maintain tablet integrity during dynamic dissolution must be further investigated, which is an essential factor for ensuring precisely modulated drug release. Meanwhile, when employing solid dispersions as solubilizing intermediates to prepare controlled-release formulations, the gelling properties of polymers in each formulation component should be fully considered to avoid incomplete disintegration and insufficient release at the initial dissolution stage.