Journal of microencapsulation最新文献

The present study aimed to develop and optimise Ranolazine-loaded Nanostructured Lipid Carriers (RNZ-NLCs) to overcome the poor oral bioavailability and rapid clearance associated with Ranolazine, thereby improving its therapeutic efficacy. RNZ-NLCs were prepared using the hot high-pressure homogenisation technique and optimised using a 2³ factorial design. Characterisation techniques included dynamic light scattering (DLS), differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier-transform infra-red spectroscopy (FTIR), in vitro drug release profiling, and pharmacokinetic analysis in rats. The optimised RNZ-NLCs exhibited a mean diameter of 205.8 nm, a polydispersity index (PDI) of 0.318, a surface charge (Zeta potential) of -22.4 mV and drug loading of 8.01% w/w. DSC and XRD studies confirmed the transformation of Ranolazine into an amorphous state, and FTIR indicated no chemical interaction with excipients. In vitro release studies showed a sustained release profile, with 65% drug release at 12 hours and 90% at 24 hours, fitting the Korsmeyer-Peppas model. Long-term storage stability studies over 90 days revealed no significant changes in particle characteristics. Pharmacokinetic evaluation in rats showed that RNZ-NLCs increased the Cmax to 18.621 µg/mL (from 9.413 µg/mL for free RNZ), delayed Tmax to 4 h (from 2 h), and enhanced AUC₀-∞ to 217.02 µg·h/mL (from 32.06 µg·h/mL). Additionally, mean residence time (MRT) and elimination half-life (t₁/₂) were extended to 11.83 h and 6.81 h, respectively. RNZ-NLCs significantly improved the pharmacokinetic profile and storage stability of Ranolazine, indicating their potential as a promising delivery system for enhancing oral bioavailability and therapeutic efficacy.

This study was to prepare the esculin-loaded chitosan microspheres for intravitreal injection and explore the feasibility of the treatment of macular degeneration. The microspheres were fabricated using an emulsification crosslinking technique. The drug loading, encapsulation efficiency, and mean particle diameter of the optimised esculin-loaded chitosan microspheres were 8.03 ± 1.30%, 93.03 ± 2.16%, and 4.81 ± 1.60 μm, respectively. The thermal stability evaluation at 25 °C demonstrated consistent particle diameter maintenance, with microspheres retaining sizes of 4.73 ± 1.75 μm and 4.89 ± 1.55 μm after 15 and 30 days' storage periods, respectively. The in vitro release profile demonstrated 80% cumulative drug release from the microspheres over a 72 h period. Subsequent pharmacokinetic analysis revealed significantly enhanced parameters in the vitreous humour following intravitreal administration, with the half-life (t_1/2) reaching 879.88 ± 44.00 min and the area under curve (AUC) attaining 150.18 ± 2.28 × 10³ mg·min/mL. Intravitreal injection of esculin-loaded chitosan microspheres offers a promising drug delivery system for the treatment of macular degeneration.

Context: Gastric cancer (GC) remains a major health concern with limited effective therapies. Nanotechnology-based drug delivery systems offer targeted and efficient treatment strategies.

Objective: This study aimed to develop chitosan-coated gold nanoparticles loaded with Nobiletin (Ch-AuNPs-NB) and evaluate their anticancer potential by targeting the PI3K/AKT/mTOR signaling pathway in GC.Materials and MethodsCh-AuNPs were synthesized by NaBH₄ reduction and loaded with Nobiletin using nanoprecipitation. Characterization was done using UV-Vis, FTIR, XRD, DLS, and TEM. Drug loading, encapsulation efficiency, and pH-responsive release were assessed.

Results: Ch-AuNPs-NB (∼120 nm, PDI 0.247, +51 mV) showed enhanced drug loading (15%) and encapsulation efficiency (90.4%) at higher NB concentrations. The formulation demonstrated pH-responsive release over 72 hours and stability for 60 days.

Discussion and conclusion: Ch-AuNPs-NB inhibited the PI3K/AKT/mTOR pathway, induced apoptosis, and arrested the cell cycle in AGS cells, highlighting its potential as a targeted GC therapy.

Aim: Linagliptin (LGP) has poor oral bioavailability due to P-gp efflux and first-pass metabolism. This study aimed to develop LGP-loaded novasomes (LGP-NVS) for intranasal brain delivery.

Methods: LGP-NVS were prepared via thin film hydration and optimised using a Box-Behnken design, varying cholesterol, stearic acid, and span-80 levels. Fifteen formulations were evaluated for particle size, entrapment efficiency, zeta potential, and drug release. The optimised formula underwent further surface, compatibility, permeability, and stability studies.

Results: The optimised formula showed high entrapment (84.22% ± 1.68%), small particle size (239.35 ± 15.20 nm), plausible zeta potential (-30.25 ± 1.23 mV), polydispersity index (0.32 ± 0.058), and controlled release (66.85 ± 2.25% after 8 h). Transmission electron microscopy demonstrated uniform size. Stability was maintained over three months. Ex-vivo permeation studies showed 1.39-fold higher permeation through camel nasal mucosa compared to drug solution.

Conclusion: Intranasal LGP-NVS might be an auspicious therapeutic avenue for the combat of Alzheimer's disease.

Solid Lipid Nanoparticles (SLNs) are versatile nano-carriers for wide range of applications. The advantages of SLNs include ease of preparation, low toxicity, high active compound bioavailability, flexibility of incorporating hydrophilic and lipophilic drugs, and feasibility of large-scale production. This review provides an overview on the preparation methods of the SLNs, the micro and nanostructure characteristics of the SLNs, and the different factors influencing sustained release and targeted drug delivery. The applications in agriculture and environment, cosmetics, wound healing, malarial treatment, gene therapy and nano-vaccines, and cancer therapy, are elaborated. The mechanisms such as passive, active, and co-delivery are discussed. The issues, challenges and the way forward with ionisable SLNs for delivery of gene and vaccines, RAS-targeted therapy, and bioactive compounds, are highlighted. In combination with multiple compounds and the potential for integration with nature/bio-based solutions, SLNs are proven to be effective, and practical for diverse applications.

The study aimed to prepare nanoembedded microparticles for pulmonary delivery of montelukast. The nanoparticles were synthesised by ionic gelation method and characterised for physicochemical properties. The nanoembedded microparticles fabricated via freeze drying method were evaluated for their physicochemical properties, drug release, aerodynamic performance and pharmacokinetic parameters in male Sprague Dawley rats. The hyaluronic-coated chitosan nanoparticles with particle size of 276.221 ± 08.232 nm, PDI of 0.397 ± 0.007, zeta potential of 14.101 ± 0.107 mV, drug content of 22.781 ± 1.002 µg/mg, and a triangular structure were embedded within microparticles. The sustained release of montelukast from nanoembedded microparticles was attributed to slow dissolution of chitosan at lung pH. The lactose-embedded nanoparticles had higher fine particle fraction (FPF: 31.37 ± 1.29) as compared to mannitol-embedded nanoparticles (FPF: 25.053 ± 0.93) due to spherical compact structure. The microparticles have lower AUC_0-t (835-856 µg.h/ml) compared to montelukast solution (1488 µg.h/ml), confirming preferential accumulation of microparticles in the lung.

A spray-dried DPI formulation was developed to enhance solubility, stability, and pulmonary delivery of curcumin-loaded CS-HA dual-coated micelles for lung cancer therapy. Curcumin was encapsulated in Pluronic F68 micelles via thin-film hydration and coated with CS-HA to improve colloidal stability and cellular interaction. The micellar suspension was spray-dried using lactose and L-leucine as dispersibility enhancers. Formulation characterisation was conducted using DLS to determine mean diameter and PDI, zeta potential analysis, and HPLC for drug loading and encapsulation efficiency, along with TEM. Spray-dried formulations were further characterised by SEM, laser diffraction (Sympatec), FTIR, and XRPD. In vitro aerosol characterisation was performed using NGI. The micelles exhibited a mean diameter of 209 nm, PDI of 0.21, zeta potential of -14 mV, encapsulation efficiency of 50-90%, and loading capacity of 5.6% (w/w). XRPD and FTIR confirmed amorphous conversion and stability. The optimized DPI showed favourable aerodynamic properties for targeted pulmonary delivery in NSCLC.

Aim: The current therapeutic approaches for rheumatoid arthritis (RA) have limited effectiveness; the present study focused on the formulation of hyalurosomes co-encapsulating dexamethasone and berberine (BER-DEX hyalurosomes).

Methods: Different formulations were developed and in-vitro characterized. The optimized formulation was transdermally applied in rats with AIA model. At the end of the experiment, histopathological examination and evaluation of inflammatory biomarkers were conducted.

Results: Entrapment efficiency of 81.14 ± 2.36% for DEX and 92.69 ± 1.58% for BER was achieved with a sustained release for 24h for both drugs. TNF-α, IL7, MMP9, and HO levels decreased by 2.7, 2.4, 2.24, and 3.6 folds in BER-DEX hyalurosomes compared to the positive control group. Histopathological assessment revealed that BER-DEX hyalurosomes showed normal joint structure comparable to the negative control.

Conclusion: The BER-DEX hyalurosomes offered a synergistic, non-invasive nanoplatform that actively targeted CD44 receptors, provided a novel and effective strategy for localized management of RA..

Aims: This study aimed to develop a thermoplastic polyurethane-oleic acid-based nanosystem (TPU-Ole NPs) incorporating siRNA and curcumin (CUR) to overcome multidrug resistance in breast cancer by silencing the c-myc gene.

Methods: TPU-Ole and CUR-loaded NPs were prepared via solvent evaporation and coated with poly-L-lysine (PLL) for siRNA attachment. NPs were characterised by dynamic light scattering (DLS) for mean diameter, polydispersity index (PDI), and zeta potential (ZP). Encapsulation (EE) and loading efficiencies (LE) were measured by NanoDrop. Release (pH 5.0; 7.4) and storage stability (pH 7.4) were evaluated using the eppendorf method. siRNA binding was confirmed by agarose gel electrophoresis. Gene silencing and apoptosis were assessed by RT-PCR and flow cytometry.

Results: Mean diameter, PDI, and ZP of NPs were 170 ± 2 nm, 0.011 ± 0.080, and -27.5 ± 0.11 mV. EE and LE were 75 ± 0.12 and 14.2 ± 0.06%. Sustained release and good stability were observed.

Conclusion: siRNA-CUR-NPs efficiently silenced c-myc and induced apoptosis in MCF-7 cells.

Aims: Doxorubicin (DOX), a potent chemotherapeutic, is a commonly prescribed treatment for breast cancer, but is limited by severe organ toxicity. Therefore, more effective therapies are required. This study developed a novel DOX-liposomes (LipDOX-ALA-AA) co-loaded with alpha-lipoic-acid (ALA) and ascorbic-acid (AA) to enhance antineoplastic effect.

Methods: Liposomes were fabricated using a microfluidic-system with a DSPClipid:Cholesterol ratio of 1:1 and a flow rate ratio of 5:1. Liposomes were investigated using various-techniques such-as dynamic light scattering to measure liposomes' size and charge; and UV-spectroscopy to determine DOX-encapsulation-efficiency, EE. Cytotoxicity assays used various cell-lines.

Results: Data revealed that LipDOX-ALA-AA had diameter of 79.0 ± 0.3 nm, with narrow size distribution, and zeta-potential of -4.0 ± 1.2. DOX-EE exceeded 95%, drug load was 0.5 mg/105.5 mg total content, drug release followed a biphasic pattern. Cytotoxicity assay showed activity (p < 0.05) against breast cancer cell-lines with reduced nephrotoxicity compared to Doxosome.

Conclusion: This novel formulation (LipDOX-ALA-AA) offers a promise in breast cancer therapy.