Journal of microencapsulation最新文献

Aim: Plant-derived extracellular vesicles (EVs) are natural nanovesicles for drug delivery. This study isolated and characterised EVs from medicinal plants as delivery vehicles.

Methods: Precipitation method was employed for the isolation and characterised using DLS, SEM, and TEM. The encapsulation efficiency (EE) and antioxidant activity of ascorbic acid (AA)-EVs were evaluated.

Results: The total yields of lyophilised vesicles per weight of the sample were 6.0, 8.6 and 9.2 mg/g for garlic, turmeric and ginger, respectively. Mean size of garlic-derived EVs, ginger-derived EVs, and turmeric-derived EVs were 101.0 ± 6.7, 226.4 ± 62.2 and 90.7 ± 2.5 nm, respectively. The zeta potential of the EVs was between -33.2 ± 10.9 and -28.8 ± 8.43 mV. Spherical morphology of the nanovesicles was confirmed by SEM and TEM. The EE of the EVs was between 78.1 ± 2.8% and 87.2 ± 1.4%.

Conclusion: Overall, the antioxidant activity of AA-loaded EVs was better compared to free AA. This study provides evidence that these medicinal plants are rich sources for developing nanotherapeutics.

This study aimed to encapsulate an anti-VEGF nanobody (Nb) within niosome nanoparticles (NNPs) to enhance its circulation half life. Key parameters such as encapsulation efficiency, stability, Nb release, cytotoxicity, and cell migration inhibition in HUVEC cells were evaluated, along with pharmacokinetic studies in mice. Nb-loaded NNPs (Nb-NNPs) were successfully prepared with an encapsulation efficiency of 78.3 ± 3.2% and demonstrated stability over one month. In vitro assays revealed that Nb-NNPs enhanced cytotoxicity and significantly reduced cell migration in HUVEC cells compared to free Nb (P < 0.05). Pharmacokinetic studies in mice demonstrated a dramatically reduced elimination rate constant (0.025 h^-1 vs. 0.843 h^-1) and an extended terminal half life (27.721 h vs. 0.822 h), indicating slower clearance and prolonged systemic presence. In conclusion, these findings underscore the potential of Nb-NNPs to provide sustained and potent therapeutic effects, contributing valuable insights for advancing targeted therapeutic strategies.

Microneedle technology is a pivotal component of third-generation transdermal drug delivery systems featuring tiny needles that create temporary microscopic channels in the stratum corneum which facilitate drug penetration in the dermis. This review offers a detailed examination of the current types of microneedles, including solid, coated, dissolving, hollow, and swelling microneedles, along with their preparation techniques as well as their benefits and challenges. Use of 3D printing technology is especially gaining significant attention due to its ability to achieve the high dimensional accuracy required for precise fabrication. Additionally, its customisability presents significant potential for exploring new designs and creating personalised microneedles products. Furthermore, this review explores next generation microneedles, especially stimuli-responsive microneedle, bioinspired microneedle and microneedles combined with other transdermal technology like sonophoresis, electroporation and iontophoresis. Regulatory aspects, characterisation techniques, safety considerations, and cost factors have also been addressed which are crucial for translation from lab to the market.

Aim: To enhance cefixime's effectiveness and address drug delivery challenges like concentration at the site, dose, and time, present study investigated the impact of polymer blends on cefixime's in vitro release profile.

Methods: Cefixime-loaded nanoparticles were prepared via a modified solvent evaporation method, forming a W/O/W double emulsion. Characterisation included FT-IR, zeta potential, TGA, TEM, and XRD, with in vitro studies and kinetic models used to analyse the release mechanism.

Results: The PH-4 nanoparticle formulation (80:20 PCL/HPMC, 0.5% PVA) achieved an 81% loading rate, no adverse effects, and a controlled release of 84.66%±2.53 over 30 days. It showed stable physicochemical properties, with in vitro antibacterial tests revealing inhibition zones of 27.4 ± 2.12 mm for E. coli and 17.2 ± 2.23 mm for S. aureus at 12 hours.

Conclusion: Based on the findings, developed nanoparticulate system containing PCL/HPMC demonstrates its efficacy and safety as a controlled drug delivery method for antibiotics like cefixime.

Aim: The study aimed to enhance phloretin's oral absorption and systemic availability through nanoencapsulation within biodegradable polymers, improving its anti-oxidant and cardioprotective potential.

Methods: Phloretin-loaded polymeric nanocomposites were prepared using ionic gelation and optimised for yield, encapsulation, loading, particle size, PdI and zeta potential. The formulation was characterised by FTIR, XRD, FESEM and MS. In-vitro drug release, stability, pharmacokinetics, biodistribution, anti-oxidant capacity, haemolysis and both in-vitro and in-vivo assessments were conducted in an ischaemia-induced rat model.

Results: The average particle size, zeta potential, encapsulation and drug loading of the optimised nanoparticles were 105.8 ± 1.92 nm, -41.5 ± 1.10 mV, 92.36 ± 0.01% and 18.47 ± 0.38%, respectively. Nano-phloretin enhanced oral bioavailability, anti-oxidant capacity. In-vivo, it reduced myocardial infarct size by ∼46% versus ∼13% for free phloretin, showing significant cardiomyocyte protection and ROS suppression.

Conclusion: The study demonstrates polymer-based nanoparticles as effective oral drug delivery systems capable of enhancing both systemic bioavailability and therapeutic efficacy of the encapsulated drug.

Study was to develop a nanostructured-lipid-careers (NLCs) of paliperidone (PLP) for nose-to-brain targeting. NLCs was prepared by sonication, high-shear homogenisation method, and characterised their mean diameter, PDI, zeta-potential, morphology (by SEM, TEM and AFM), entrapment efficiency, drug loading, in vitro release, interaction study (by FTIR), and stability. Further, ex vivo permeation and ciliotoxicity performed in sheep nasal mucosa, and in vivo biodistribution/pharmacokinetic was performed in rats for schizophernia. Developed NLCs showed spherical and clearly 3-dimentinal structure with 129 ± 2.7 nm mean diameter, 0.304 ± 0.003 PDI, -7.61 ± 0.56 mV zeta-potential, 58.16 ± 0.17% entrapment efficiency, 65.8 ± 2% drug loading and 74.32 ± 0.003% release in 12 h, followed by Higuchi model. Ex vivo study showed NLCs have three times higher permeation, compare to pure drug (around 71.50.32% in 6 h) and 3.98 g/cm²/h steady sate flux. The blood/brain ratio given by intranasally have higher compare to IV route, and 94.53 ± 21.45% drug targeting efficiency in brain. In conclusion, NLCs have easily crossed BBB, higher drug delivery and effective for schizophrenia in given by intranasal.

This study aims to investigate Polylactic Acid (PLA) and Polycaprolactone (PCL) polymers for microencapsulation of hydrophilic and hydrophobic anti-glaucoma drugs using an emulsion-based solvent evaporation technique. Microparticle size was analysed using optical microscopy, while drug-polymer interactions through Dynamic-Light-Scattering (DLS) and Fourier-Transform-Infra-red/Attenuated-Total-Reflection spectroscopy (FTIR/ATR). In vitro, drug release studies were performed to investigate drug encapsulation and release profiles. Spherical microparticles, with particle size 94 ± 6.9 μm for PCL-based and 100 ± 3.74 μm for PLA-based formulation, were obtained. Drug release studies showed 100% release over about 32 days, with encapsulation efficiency (%EE) and drug loading (%w/w) reaching up to 95 and 2.84% for PLA-based and 97 and 2.91% for PCL-based microparticles, respectively. DLS studies reveal an increase in hydrodynamic radius (R_H), which correlates to enhanced drug encapsulation. So, the nature of the drug and polymer significantly impacts drug encapsulation and release, with drug-polymer interactions playing a crucial role alongside experimental parameters.

This study aims to evaluated the impact of poly(ε-caprolactone) (PCL) microspheres on the pharmacokinetics and pharmacodynamics (PopPK/PD) of 6-methylcoumarin (6MC). For this, PCL microspheres loaded with 6MC were prepared using the emulsification-evaporation method. Particle size, zeta potential, drug loading, and entrapment efficiency were characterised by dynamic light scattering and UV spectrophotometry. In vitro release and pharmacokinetics in Wistar rats were assessed for free and encapsulated 6MC. Anti-inflammatory activity was evaluated using the carrageenan-induced paw edoema model, with PopPK and PopPK/PD models developed. Microspheres showed diameters between 2.9 and 7.1 µm, zeta potentials of -10 to -15 mV, and drug loading of 0.24 mg/mg. Encapsulation efficiency was 45.5% to 75.9%. PopPK models showed enhanced absorption and distribution, with increased anti-inflammatory potency of encapsulated 6MC. PCL microspheres significantly improved the pharmacokinetic and pharmacodynamic profiles of 6MC, enhancing its therapeutic potential for lipophilic drugs.

Aim: The present study was conducted to produce a new carrier containing whey protein isolate-basil seed gum (WPI-BSG) conjugate to achieve superior physicochemical stability of emulsions containing vitamin D₃ (Vit-D₃).

Methods: Zeta-potential and particle size analysis, spectrophotometric method, encapsulation efficiency, loading capacity and dialysis bag method were used to examined physicochemical stability and Vit-D₃ release from the emulsions.

Results: The conjugate-stabilised emulsion showed maximum encapsulation efficiency (87.05 ± 3.37% (w/w)) and loading capacity (5.43 ± 0.08% (w/w)) at the Vit-D3 concentration of 200 and 300 mg/kg. This emulsion also demonstrated good physical stability after 30 days of storage with the zeta potential and mean droplet size of -79.60 ± 0.62 mV and 1346.82 ± 5.95 nm, respectively. Additionally, the conjugate-stabilised emulsion had a maximum Vit-D₃ retention (chemical stability) of 72.79 ± 3.58% after a 15-day storage period.

Conclusion: Our findings suggest that the conjugate-stabilised emulsion has a good stabilising capacity as a carrier for hydrophobic compounds such as Vit-D₃.

The dermal route is commonly used to deliver the drugs at the targeted site and achieve maximum therapeutic efficacy. The stratum corneum, the uppermost layer of the skin, presents a significant diffusional barrier for most drugs. Various nanoformulations face challenges such as limited drug absorption and inadequate retention at the targeted site, frequently hindering therapeutic efficacy. Researchers are increasingly exploring innovative strategies that leverage nanotechnology and specialized carriers to address these challenges and enhance the outcomes of dermal medications. A novel drug delivery system, bilosomes, has been designed as a potential vesicular carrier system for the dermal route. Bilosomes are colloidal, lipid-based vesicles stabilized with bile salts, offering greater stability during storage and transportation. The lipid bilayer of bilosomes imparts ultra-flexibility, facilitating penetration through the stratum corneum. This review explores the use of bilosomes in dermal formulations for treating diverse diseases, their developmental techniques, and characterization, and it sheds light on their advantages over traditional lipid nanocarriers.