Cutibacterium acnes (C. acnes) is involved in the pathogenesis of acne by inducing inflammation and biofilm formation, along with other virulence factors. A Camellia sinensis (C. sinensis) callus lysate is proposed to reduce these effects. The aim of the present work is to study the anti-inflammatory properties of a callus extract from C. sinensis on C. acnes-stimulated human keratinocytes and the quorum-quenching activities. Keratinocytes were stimulated with thermo-inactivated pathogenic C. acnes and were treated with the herbal lysate (0.25% w/w) to evaluate its anti-inflammatory effect. C. acnes biofilm was developed in vitro and treated with 2.5 and 5% w/w of the lysate to evaluate quorum sensing and the lipase activity. The results showed that the lysate was able to reduce the production of interleukin-6 (IL-6), interleukin-8 (IL-8), tumor necrosis factor-α (TNF-α), and C-X-C motif chemokine ligand 1 (CXCL1), and decrease the nuclear translocation of nuclear factor kappa light chain enhancer of activated B cells (NF-κB). The lysate did not show bactericidal activity but showed diminished biofilm formation, the lipase activity, and the production of autoinducer 2 (AI-2), a member of a family of signaling molecules used in quorum sensing. Therefore, the proposed callus lysate could have the potential to reduce acne-related symptoms without the eradication of C. acnes, which is part of the natural skin microbiome.

Helicobacter pylori is the main pathogen responsible for gastric ulcers and a predisposing factor of stomach cancer. Although current treatment is usually successful, it requires high doses and frequent administration. An innovative mucoadhesive system (Mucolast^®) loaded with amoxicillin and clarithromycin is proposed to improve the efficacy of treatment against H. pylori. The drug product was optimized based on its viscoelastic properties to obtain long-term stability of the vehicle. The drug release mechanisms were different for both antibiotics based on their solubilization status. A systemic and stomach pharmacokinetic profile was obtained after three different doses were administered to mice, obtaining similar systemic exposure levels but an increase in drug concentration in the stomach. The efficacy results in mice infected with H. pylori also demonstrated the superiority of the antibiotics when administered in Mucolast^®, as shown by the bacterial count in stomach tissue and under histopathological and biochemical evaluation. The proposed treatment was efficacious and safe and is presented as a realistic alternative to current treatment options to improve patient compliance and to reduce bacterial resistance.

Antimicrobial drugs applied topically offer several advantages. However, the widespread use of antibiotics has led to increasing antimicrobial resistance. One interesting approach in the drug discovery process is drug repurposing. Disulfiram, which was originally approved as an anti-alcoholism drug, offers an attractive alternative to treat topical multidrug resistance bacteria in skin human infections. This study aimed to evaluate the biopharmaceutical characteristics of the drug and the effects arising from its topical application in detail. Microdilution susceptibility testing showed antibacterial activity against Gram-positive bacteria Staphylococcus aureus and Streptococcus pyogenes. Dermal absorption revealed no permeation in pig skin. The quantification of the drug retained in pig skin demonstrated concentrations in the stratum corneum and epidermis, enough to treat skin infections. Moreover, in vitro cytotoxicity and micro-array analyses were performed to better understand the mechanism of action and revealed the importance of the drug as a metal ion chelator. Together, our findings suggest that disulfiram has the potential to be repurposed as an effective antibiotic to treat superficial human skin infections.

Background: The encapsulation of hydrophilic drugs within microparticles has gained significant interest in drug delivery systems due to their potential to improve stability, bioavailability, and controlled release of therapeutic agents. Biotin, a water-soluble vitamin, presents challenges such as rapid degradation and limited membrane permeability, which constrain its therapeutic effectiveness. Objectives: This study aims to develop and characterize biotin-loaded microparticles formulated with alginate, Eudragit^® E100, and CaCl₂, and to evaluate their characterization and potential applications. Methods: The microparticles were produced using the external ionic gelation method, where alginate and CaCl₂ solutions were mixed under probe sonication. Eudragit^® E100 was added as a complexing agent. The optimized formulation was used to encapsulate biotin, and various experimental variables were screened to study their influence on the properties of the microparticles. Results: Biotin was encapsulated in alginate microparticles (size: 634 nm; polydispersity index: 0.26; zeta potential: −45 mV) with an encapsulation efficiency of 90.5%. In vitro release studies using vertical diffusion Franz cells demonstrated a controlled release profile following the Weibull kinetic model. Conclusions: Encapsulation techniques offer a promising approach to overcome the limitations of hydrophilic drug delivery. The biotin-loaded microparticles developed in this study have potential applications in both topical and oral formulations, providing controlled release and improved therapeutic efficacy, and illustrate the broader applicability of polymeric encapsulation systems for improving the delivery of labile, hydrophilic bioactives.

Background: Liposomes are attractive topical carriers, yet translating laboratory fabrication to scalable, well-controlled processes remains challenging. Objectives: We compared three manufacturing methods for diclofenac-loaded liposomes: probe sonication, microfluidic mixing, and a high-turbulence microreactor, under a Quality-by-Design framework. Methods: Differential scanning calorimetry (DSC) was used to define a processing-relevant liquid-crystalline temperature window for the lipid excipients. For sonication scale-up, a Plackett-Burman screening design identified key process factors and supported an energy-density (W·s·L⁻¹) control approach. For microfluidics, the effects of flow-rate ratio (FRR) and total flow rate (TFR) were mapped and optimized using a desirability function. Microreactor trials were performed at elevated throughput. Residual ethanol during post-processing was monitored at-line by Raman spectroscopy calibrated against gas chromatography (GC). Particle size and dispersity were measured by DLS and morphology assessed by cryo-TEM. Results: DSC supported a 70–85 °C processing window. Sonication scale-up using an energy-density target (~11,000 W·s·L⁻¹) reproduced lab-scale quality at 8 L (Z-average ~87–92 nm; PDI 0.16–0.23; %EE 86–94%). Microfluidics optimization selected FRR 3:1/TFR 4 mL·min⁻¹, yielding ~64 nm liposomes with PDI ~0.13 and %EE ~93%. The microreactor achieved ~50 nm liposomes with %EE ~95% at 50 mL·min⁻¹. Cryo-TEM corroborated size trends and showed no evident aggregates. Conclusions: All three routes met topical CQAs (~50–100 nm; PDI ≤ 0.30; high %EE). Method selection should be guided by target size/dispersity and operational constraints: sonication enables energy-based scale-up, microfluidics offers precise size control, and microreactors provide higher throughput.

Background/Objectives: The question addressed in the current work is to develop a simulation of a pharmaceutical process (DNA encapsulation within lipid nanoparticles using a microfluidic micromixer) which will be of utility to the end users (laboratory-scale formulation development). The simulation and the microfluidic approach also address sustainability issues, such as reducing the environmental impact of the process itself, and reducing the need for physical testing. The paper details the implementation and validation, taking into account key performance indicators and control parameters. Methods: The main method applied for simulation development is a novel multi-agent approach to incorporate stochastic probabilistic behavior, combined with theoretical definitions from the process experts and relevant literature, and data/results from laboratory-scale experiments with different parameter configurations. Results: The simulation was implemented as a representation of the real physical process, reproducing the relationships between process parameters (flow rates) and experimental key performance indicators (capsule diameter, poly dispersion index, encapsulation efficiency). The simulation results demonstrated a general agreement with the empirical results and provided useful predictive insights for the laboratory experiments. Conclusions: The simulation has potential as a support tool for laboratory experiments to reduce physical testing and indicate the most promising configurations on which to focus, with potential savings in time, resources and other costs.