In this study, we investigated the formulation of stable solid dispersions to enhance the bioavailability of olaparib (OLA), a therapeutic agent for ovarian cancer and breast cancer characterized as a BCS class IV drug with low solubility and low permeability. Various polymers were screened based on solubility tests, and OLA-loaded solid dispersions were prepared using spray drying. The physicochemical properties of these dispersions were investigated via scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier Transform Infrared Spectroscopy (FT-IR). Subsequent dissolution tests, along with assessments of morphological and crystallinity changes in aqueous solutions, led to the selection of a hypromellose (HPMC)-based OLA solid dispersion as the optimal formulation. HPMC was effective at maintaining the supersaturation of OLA in aqueous solutions and exhibited a stable amorphous state without recrystallization. In an in vivo study, this HPMC-based OLA solid dispersion significantly enhanced bioavailability, increasing AUC_0–24 by 4.19-fold and C_max by more than 10.68-fold compared to OLA drug powder (crystalline OLA). Our results highlight the effectiveness of HPMC-based solid dispersions in enhancing the oral bioavailability of OLA and suggest that they could be an effective tool for the development of oral drug formulations.

Objectives: In this study, Quality by Design (QbD) was used to develop an optimized self-nanoemulsifying drug delivery system (SNEDDS) as an ophthalmic formulation of flurbiprofen (FLU). Using a Box–Behnken design (BBD), an optimal SNEDDS composition was crafted, targeting enhanced corneal permeability and increased bioavailability of the drug. Methods: The levels of each factor(X) were established using a pseudo-ternary diagram, and the Box-Behnken design (BBD) was used to evaluate the components of oil (18.9 mg), surfactant (70.7 mg), and co-surfactant (10.0 mg) to optimize the SNEDDS formulation. The response(Y) considered were particle size, polydispersity index (PDI), transmittance, and stability. Transmission electron microscopy (TEM) and dynamic light scattering (DLS) were used to analyze the particle size and morphology. In vitro and ex vivo diffusion tests were conducted to assess drug flux and permeability. Result: Using a response optimization tool, the values of each X factor were optimized to achieve a small particle size (nm), a low polydispersity index (PDI), and high transmittance (%), resulting in a formulation prepared with 18.9 mg of oil, 70.7 mg of surfactant, and 10.0 mg of co-surfactant. The optimized SNEDDS exhibited a small particle size of 24.89 nm, a minimal PDI of 0.068, and a high transmittance of 74.85%. A transmission electron microscopy (TEM) analysis confirmed the presence of uniform spherical nanoemulsion droplets with an observed mean diameter of less than 25 nm, corroborating the dynamic light scattering (DLS) measurements. Furthermore, the SNEDDS demonstrated improved stability under the stress conditions of heating–cooling cycles, with no phase separation, creaming, or caking observed and no differences in its particle size, PDI, or transmittance. In vitro and ex vivo diffusion tests demonstrated that the flux of the optimized SNEDDS (2.723 ± 0.133 mg/cm², 5.446 ± 0.390 μg/cm²) was about 2.5 and 4 times higher than that of the drug dispersion, and the initial diffusion was faster, which is suitable for the characteristics of eye drops. Conclusions: Therefore, the formulation of a flurbiprofen-loaded SNEDDS (FLU-SNE) was successfully optimized using the QbD approach. The optimized FLU-SNE exhibited excellent stability and enhanced permeability, suggesting its potential effectiveness in treating various ocular inflammations, including uveitis and cystoid macular edema.

The aim of this study was to develop a long-acting injectable formulation of risperidone using polylactic acid (PLA) or poly (lactic-co-glycolic acid) (PLGA), a biodegradable and biocompatible polymer. Risperidone microspheres (RMs) were prepared by creating an O/W emulsion using dichloromethane (DCM) as a solvent and then employing the solvent evaporation method. The RMs were prepared with four different risperidone-to-PLGA ratios (1:1, 1:1.3, 1:2, and 1:3 (w/w)), and each ratio was subjected to the same manufacturing process. The physicochemical properties of the prepared RMs, such as their shape, particle size, drug loading ratio, encapsulation efficiency, and in vitro degradation profile, were evaluated. The particle size of the RMs ranged from 30 to 100 μm, with larger PLGA ratios resulting in larger RM sizes. The drug loading ratio was inversely proportional to the increase in the PLGA ratio in the RMs, and all the formulations showed improved release profiles compared to the reference drug, Risperdal Consta^®. The release data modeling results showed that the RM-3 formulation with a 1:1 (w/w) ratio of risperidone and PLGA exhibited a release pattern close to zero-order kinetics. The manufactured RMs were confirmed to have the potential to be used as a long-acting risperidone injection with sustained and stable release as well as an extended dosing interval.

The purpose of this study was to enhance the stability of montelukast and levocetirizine for the development of a fixed-dose combination (FDC) monolayer tablet. To evaluate the compatibility of montelukast and levocetirizine, a mixture of the two drugs was prepared, and changes in the appearance characteristics and impurity content were observed in a dry oven at 60 °C. Excipients that contributed minimally to impurity increases were selected to minimize drug interactions. Mannitol, microcrystalline cellulose, croscarmellose sodium, hypromellose, and sodium citrate were chosen as excipients, and montelukast–levocetirizine FDC monolayer tablets were prepared by wet granulating the two drugs separately. A separate granulation of montelukast and levocetirizine, along with the addition of sodium citrate as a pH stabilizer, minimized the changes in tablet appearance and impurity levels. The prepared tablets demonstrated release profiles equivalent to those of commercial products in comparative dissolution tests. Subsequent stability testing at 40 ± 2 °C and 75 ± 5% RH for 6 months confirmed that the drug content, dissolution rate, and impurity content met the specified acceptance criteria. In conclusion, the montelukast–levocetirizine FDC monolayer tablet developed in this study offers a potential alternative to commercial products.

To improve the low solubility of poorly water soluble olaparib, in the following study, we prepared olaparib-loaded quaternary solid dispersions with hypromellose, Tween 20 or Labrasol, and colloidal silica. The solubility of olaparib with various types of surfactants was evaluated to select the most suitable surfactant to effectively enhance its solubility, and subsequently, olaparib-loaded quaternary solid dispersions were prepared through spray drying. The physicochemical properties of the prepared olaparib-loaded quaternary solid dispersions were investigated using scanning electron microscopy, flowability, powder X-ray diffraction, and Fourier-transform infrared spectroscopy. The particle size of the olaparib-loaded quaternary solid dispersions was smaller and more spherical compared to the olaparib drug powder and maintained an amorphous state, and olaparib exhibited no intermolecular interactions with other excipients within the solid dispersion. Additionally, they exhibited enhanced flow properties compared to the olaparib drug powder. The results of subsequent kinetic solubility tests and dissolution tests demonstrated that the surfactant influenced the enhancement of the solubility and drug release of olaparib. Therefore, olaparib-loaded quaternary solid dispersions, characterized by enhanced solubility, will be beneficial for the oral delivery of poorly soluble olaparib.

This study aimed to identify novel antimicrobial peptides (AMPs) from Lactiplantibacillus plantarum K9, isolated from Protaetia brevitarsis seulensis larvae, using genome and transcriptome analyses. L. plantarum K9, among the isolated lactic acid bacteria from P. brevitarsis larvae, showed the strongest antimicrobial activity, with MIC₉₀ values of 22 μL against E. coli and 21 μL against S. aureus. Approximately 54% of the antimicrobial activity was attributed to peptides or proteins. Genome analysis revealed a 3 Mb chromosome and three plasmids. Screening of hypothetical proteins using CAMP_R4 identified 18 AMP candidates. Transcriptomic analysis showed that most AMP genes were more highly expressed in the stationary phase and were upregulated under low-pH conditions. Antimicrobial assays using synthetic peptides demonstrated that AMP4, 6, 7, 12-2, 14, and 18 exhibited strong activity against S. aureus, whereas AMP16 and 18 were effective against E. coli. After cloning each AMP and assessing its antimicrobial activity, the cloned AMPs exhibited overall greater antimicrobial activity against S. aureus than against E. coli. Among all candidates, AMP12 displayed the strongest antimicrobial activity and high specificity toward S. aureus. Structural analysis revealed a conserved α-helical region that is likely responsible for membrane-targeting antimicrobial activity. Collectively, these findings suggest that L. plantarum K9 AMP12 is a novel antimicrobial peptide that contributes to the strain’s antimicrobial properties.