Objective The objective of this study was to develop a stable clear ophthalmic nano-micellar formulation of Nepafenac. Significance: The current marketed suspension formulation of nepafenac indicated for post-surgical uveitis is associated with higher manufacturing complexity and cost due to the need for sterile drug substance and specialized aseptic processing inherent to suspension-based ophthalmic products. It also exhibits limitations in patient compliance due to relatively high viscosity, lacrimation, and foreign body sensation following instillation. Methods Pre-formulation study was done to identify the excipients required. Systematic changes in the concentration of surfactant and crystal inhibitor along with other excipients led to the development of stable nano-micellar formulation. Box-behnken method was used for the optimization. The optimized micellar composition was evaluated for physicochemical tests particle size, zeta potential, cloud point, osmolality pH, assay of drug, entrapment efficiency and dynamic viscosity. Further in-vitro cell viability, in-vitro release, ocular tolerance test and stability evaluation were also performed. Results Average particle size of the micelle ranged from 10 to 20 nm, 43.5 mPas dynamic viscosity, osmolality of 319 mOsm/Kg, pH 7.4 and cloud point of 59.7 °C. The optimized formulation demonstrated in-vitro safety as confirmed by MTT cell viability and HET-CAM ocular irritation assays, and exhibited physicochemical stability for up to 6 months under real-time storage conditions. Conclusion The optimized micelle formulation can serve as a better alternative for ophthalmic delivery of nepafenac.

Objective This study aimed to develop and evaluate a dermal gel formulation incorporating the methanolic leaf extract of Guiera senegalensis (GS) for potential topical antimicrobial application. Significance: Dermal gel formulations of GS leaf extracts may offer safe and effective alternatives against bacterial and fungal skin infections, particularly beneficial for paediatric and geriatric individuals who are most susceptible to such conditions. Methods Leaves of GS were extracted by maceration using methanol and fractionated with solvents of increasing polarity. The extract and fractions underwent phytochemical screening, antibacterial evaluation, and spectral characterization (GC–MS and FT–IR). Xanthan gum–based gels were formulated and evaluated for pH, viscosity, spreadability, extrudability, swelling, erosion, and antibacterial activity. Results The methanolic extract (26.36% yield) contained abundant phytochemicals, including flavonoids, phenolics, tannins, and terpenoids. Fractionation revealed the polarity-based distribution of phytochemicals but did not enhance antibacterial potency. The methanolic extract showed the strongest activity against Staphylococcus aureus (22.24 ± 0.12 mm). GC–MS and FT–IR confirmed the presence of bioactive compounds and functional groups linked to antimicrobial effects. The gels exhibited skin-compatible pH (5.95–6.65), appropriate viscosity (11.23–63.23 Pa·s), and desirable spreadability. Among all, formulation F2 showed the best overall characteristics for topical use. Conclusion GS leaf extract–loaded gels demonstrated excellent physicochemical properties and antibacterial activity. Although fractionation provided no added antimicrobial advantage, it offered insights into phytochemical distribution. Formulation F2 represents a promising natural, plant-based topical antimicrobial candidate.

Objectives This study aimed to develop and evaluate rifampicin (RIF) and isoniazid (INH) co-loaded liposome for sustained drug delivery to enhance therapeutic efficacy against tuberculosis (TB) and overcome challenges associated with prolonged treatment and drug resistance. Significance The novel biocompatible liposomal system enables sustained co-delivery of RIF and INH, providing a scalable and stable platform with enhanced antimicrobial efficacy and strong potential to advance tuberculosis therapy. Methods Liposome were prepared using soybean lecithin and cholesterol (L-CH) via rotary evaporator-assisted thin film hydration, optimized by Box-Behnken design, and characterized for size, PDI, entrapment efficiency, and physicochemical properties (FT-IR, DSC, HR-TEM). In vitro release, accelerated stability, antimicrobial efficacy against M. smegmatis and M. tuberculosis H37Rv, and LC-MS/MS-based metabolomic profiling were systematically evaluated. Results The optimized liposome exhibited a mean size of 129.5 ± 2.20 nm, PDI of 0.369 ± 0.06, and entrapment efficiencies of 63.84 ± 1.62% (RIF) and 56.92 ± 1.69% (INH). The release study indicated sustained diffusion-controlled kinetics consistent with the Higuchi model, achieving cumulative releases of approximately 92% for INH and 85% for RIF over a 45-hour period. The accelerated stability studies confirmed negligible drug degradation, while antimicrobial assays demonstrated a twofold reduction in MIC relative to free drugs, and metabolomic profiling indicated modulation of glutathione, citric acid, and tyrosine pathways associated with enhanced redox balance and antimicrobial activity. Conclusions The co-loaded RIF-INH liposomal system offers a promising, clinically translatable approach for sustained drug release and improved tuberculosis therapy.

Objective The aim of this study was to develop a chemotherapy drug paclitaxel (PTX) and a tumor-specific ROS generation agent β-lapachone(LAP) co-loaded human serum albumin (HSA)-based nanoparticles (ANPs) for synergistic anticancer therapy. Significance Albumin-based nanoparticles (ANPs) offer unique advantages for antitumor drug delivery system, including non-immunogenicity and inherent tumor-targeting capacity. In this study, we mimicked the natural fatty acid binding process in vivo to construct ANPs to synergistically elevate ROS with β-lapachone for cooperative cancer therapy. Methods First, a polyethylene glycol monostearate(PGM) modified redox-sensitive paclitaxel prodrug(PTX-SS-PGM) was synthesized and stearic acid capable of binding with HSA was introduced. Further, a LAP/PTX-SS-PGM complex was engineered through the π − π stacking interaction and H-bonding between LAP and PTX. The PTX and LAP co-loaded ANPs (PTX-SS-PGM&LAP@HSA) were obtained through the binding between LAP/PTX-SS-PGM complex and HSA. Results The percentage of apoptosis for PTX, Abraxane®, PTX-SS-PGM@HSA ANPs, and PTX-SS-PGM&LAP@HSA ANPs was 8.17%, 9.53%, 15.17%, and 28.6%, respectively, demonstrating synergistic cytotoxicity effect. The in vivo imaging test confirmed that PTX-SS-PGM&LAP@HSA had targeting ability to tumor tissues. The obtained ANPs exhibited better tumor growth inhibition in vitro and in vivo.

Objective To develop a green and efficient ultrasound-assisted extraction (UAE) process to obtain bioactive resins from Cannabis sativa with potential pharmaceutical applications, optimizing extraction parameters to maximize antioxidant capacity and total polyphenol content. Significance UAE using ethanol under mild temperature and time conditions as a green technique was applied to reduce solvent consumption, energy demand, and extraction time while preserving thermolabile bioactive compounds. Optimizing UAE enables the recovery of cannabinoid- and terpene-rich extracts that may serve as natural active pharmaceutical ingredients or functional excipients for drug development. This study integrates a Doehlert-based optimization of UAE with a functional evaluation of antioxidant efficiency and antimicrobial activity, providing a comprehensive framework for the development of cannabis-derived pharmaceutical ingredients. Methods A Doehlert experimental design combined with response surface methodology was employed to optimize temperature and extraction time. The optimized extract was characterized for its phytochemical composition. Antimicrobial activity was evaluated against Gram-positive and Gram-negative bacterial strains to assess potential therapeutic relevance. Results Under optimal conditions (54.5 °C, 28 min 25 s), the extract showed a total phenolic content of approximately 0.11 mg gallic acid/mg resin and an IC50 value of about 0.24 mg resin/mL extract, indicating enhanced antioxidant performance compared to non-optimized conditions. Also, it showed selective bactericidal activity against Staphylococcus aureus ATCC 25923 and Staphylococcus epidermidis ATCC 12228, while Gram-negative strains remained resistant. Conclusion UAE extraction efficiently recovered antioxidant and selectively antimicrobial compounds from Cannabis sativa resins under mild, eco-friendly conditions, supporting their potential use as bioactive ingredients in pharmaceuticals.

Objective To evaluate the anti-inflammatory activity and mechanism of Panaxadiol saponins (PDS), develop a PDS-based gel for periodontitis treatment, and evaluate its therapeutic efficacy using a rat model of periodontitis. Methods The anti-inflammatory effects of PDS were assessed using LPS-induced RAW264.7 cells. ELISA and RT-qPCR were performed to detect inflammatory factors; Western blotting analyzed MAPK/NF-κB pathway-related proteins. A single-factor experiment was used to examine the effects of the dosages of carbomer 940, propylene glycol, and triethanolamine on the properties of the PDS gel and to evaluate its in vitro release versus in vitro permeation and retention on oral mucosa. A rat periodontitis model was established by ligation plus high-sugar feeding, and the efficacy of PDS gel in ameliorating periodontitis in rats was evaluated using gingival index scoring, micro-CT, HE staining, ELISA, and RT-qPCR to assess the state of periodontal tissues and inflammatory responses, and salivary microbiota analysis using 16S rRNA sequencing. Results PDS significantly reduced NO, IL-6, IL-1β, and TNF-α release, inhibited their mRNA expression, and suppressed MAPK/NF-κB pathway-related proteins in LPS-induced RAW264.7 cells. The PDS gel exhibited good physicochemical properties, release performance, and mucosal permeability. PDS gel decreased gingival index, attenuated alveolar bone loss, reduced inflammatory cell infiltration, and lowered IL-6, IL-1β, TNF-α, and RANKL mRNA levels in serum and periodontal tissue. It also regulated and restored the balance of salivary flora. Conclusion PDS gel can inhibit the MAPK/NF-κB pathway-mediated inflammatory response, reduce bone destruction, and regulate bacterial dysbiosis, demonstrating good therapeutic prospects for periodontitis.

Nanoformulated androgen receptor (AR) antagonists constitute a cutting-edge advancement in the treatment of AR-driven cancers by significantly enhancing the precision and effectiveness of therapy. These nanoparticle-based formulations are uniquely designed to simultaneously inhibit AR-driven transcription and critical signaling pathways involved in tumor progression and drug resistance, including PI3K/AKT and MAPK cascades. The distinctive properties of nanoparticles, such as improved bioavailability, controlled and sustained drug release, and active tumor targeting, enable these AR antagonists to achieve higher intratumoral concentrations and minimize off-target effects. This targeted delivery system not only overcomes common resistance mechanisms seen with conventional AR antagonists but also facilitates the co-delivery of multiple agents for synergistic therapeutic action. This review highlights how nanoformulated AR antagonists hold immense potential to transform cancer management by providing more effective, durable responses and a foundation for personalized, multi-pathway-targeted treatment strategies in advanced and resistant cancers. Their development addresses critical clinical challenges, offering a promising pathway to improve patient outcomes and fill significant gaps in current oncologic therapies.

Objective The main objective of this article was to explore the therapeutic potential of intranasally administered metal/metal oxide nanoparticles (NPs) for treating central nervous system (CNS) disorders. Significance of review Metal/metal oxide NPs offer new possibilities for brain imaging and targeted drug delivery. These NPs can be delivered intranasally with minimal invasiveness, offering a patient-friendly approach for therapeutic applications. The current article synthesizes research studies on the potential of intranasal metal/metal oxide NPs for treating CNS disorders, focusing on their unique features, transport pathways, therapeutic and diagnostic benefits, and neurotoxicological challenges. Key findings The small size and high surface area of metal/metal oxide NPs enable efficient drug encapsulation and direct delivery to the brain via the olfactory and trigeminal pathways, bypassing the blood-brain barrier. These NPs exhibit tunable surface chemistry, allowing functionalization with ligands or coatings to enhance biocompatibility and reduce neurotoxicity. Additionally, these NPs can show inherent therapeutic properties, such as antioxidant or anti-inflammatory effects, which further support neuroprotection. Conclusions Intranasal delivery of metallic NPs is an emerging strategy for drug delivery and imaging, particularly for targeting CNS disorders. However, the development of novel NPs with minimal neurotoxicity is crucial to ensuring their safety and efficacy for clinical applications.

Objective To establish an in vitro release (IVR) method for butenafine hydrochloride cream using Immersion Cells and compare the drug release characteristics of commercial samples. Significance Reevaluating post-listing semisolid drug products based on quality attributes of IVR performance is crucial for guaranteeing clinical efficacy. Methods An in vitro release testing (IVRT) method using Immersion Cells was developed and validated for sensitivity, linearity, and reproducibility. It was adapted for use with Vertical Diffusion Cells (VDCs) to compare two devices. Univariate tests were conducted to assess the effect of excipients on in vitro release rates (IVRRs). Three regulatory guidelines recommended by FDA, NMPA and EMA for IVR performance consistency assessment were compared to evaluate the sameness of marketed samples. Results For IVRT of butenafine hydrochloride cream, Immersion Cells exhibited the same functionality as VDCs. Stearyl alcohol which serves as oil phase matrix and thickener in the cream had a significant impact on IVRRs. Regarding the consistency of marketed samples, FDA guidelines supported a consistent conclusion, while NMPA and EMA guidelines reached the opposite conclusion, which were primarily attributed to different acceptance criteria outlined in the three regulatory guidelines. Conclusions Additional strategies are needed to ensure consistent therapeutic outcomes of butenafine hydrochloride cream throughout its life cycles, such as stricter control of stearyl alcohol dosage during manufacturing. Further research is needed to explore appropriate limits for consistency assessment of it. Immersion Cells offers the advantage of lower cost in routine quality control and its application in IVRT for semisolid formulations merits further expansion.

Objective Silver nanoparticles (AgNPs) are widely utilized in anti-migratory applications due to their beneficial physicochemical and biological properties. This study aimed to evaluate the in vitro cytotoxic and anti-migratory effects of AgNPs synthesized using the above-ground parts (stems, flowers, and leaves) of Onosma mutabilis (O. mutabilis). Significance Green-synthesized AgNPs derived from O. mutabilis exhibit notable cytotoxic and anti-migratory effects on A549 cells, offering dual-functional potential. Their biocompatibility and capacity for targeted release in acidic tumor microenvironments make them promising candidates for sustainable cancer therapies. Methods AgNPs were green-synthesized using aqueous plant extracts and characterized by ultraviolet-visible spectroscopy (UV-Vis spectroscopy), X-ray diffraction (XRD), fourier transform infrared (FTIR), and scanning electron microscopy (SEM). Cytotoxicity against A549 cells was assessed via the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) assay and anti-migratory effects were examined using a scratch assay. Results UV–Vis spectroscopy confirmed the formation of AgNPs synthesized from O. mutabilis extracts by showing a characteristic absorption band around 420–480 nm. XRD analysis revealed their crystalline structure, while SEM demonstrated predominantly spherical morphology. MTT assay indicated that the AgNPs, especially those derived from the flower extract, significantly reduced A549 cell viability in a dose- and time-dependent manner, with an IC50 value of 5.28 µg/mL. In addition, wound healing assays confirmed their strong anti-migratory activity. Conclusion These findings suggest that green-synthesized AgNPs induce cytotoxic and anti-migratory effects, highlighting their potential as therapeutic agents against A549 lung cancer cells.