Journal of microencapsulation最新文献

Aims: This study aimed to improve rivaroxaban delivery by optimising solid lipid nanoparticles (SLN) for minimal mean diameter and maximal entrapment efficiency (EE), enhancing solubility, bioavailability, and the ability to cross the blood-brain barrier.

Methods: A central composite design was employed to synthesise 32 SLN formulations. Response surface methodology (RSM) and artificial neural networks (ANN) models predicted mean diameter and EE based on five independent variables.

Results: The optimised SLN formulation achieved a mean particle diameter of 159.8 ± 15.2 nm, with a Polydispersity index of 0.46, a zeta potential of -28.8 mV, and an EE of 74.3% ± 5.6%. The ANN model showed superior accuracy for both mean diameter and EE, outperforming the RSM model. Structural integrity and stability were confirmed by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier-transform infrared spectroscopy (FTIR).

Conclusion: The high accuracy of the ANN model highlights its potential in optimising pharmaceutical formulations and improving SLN-based drug delivery systems.

Phytochemicals as dietary components are being extensively explored in order to prevent and treat a wide range of diseases. Apigenin is among the most studied flavonoids found in significant amount in fruits (oranges), vegetables (celery, parsley, onions), plant-based beverages (beer, tea, wine) and herbs (thyme, chamomile, basil, oregano) that has recently gained interest due to its promising pharmacological effects. However, the poor solubility and extended first pass metabolism of apigenin limits its clinical use. Various advantages have been demonstrated by nanocarrier-based platforms in the delivery of hydrophobic drugs like apigenin to diseased tissues. Apigenin nanoformulations have been reported to have better stability, high encapsulation efficiency, prolonged circulation time, sustained release, enhanced accumulation at targeted sites and better therapeutic efficacy. An overview of the major nanocarriers based delivery including liposomes, niosomes, solid lipid nanoparticles, micelles, dendrimers etc., is described. This review sheds insight into the therapeutic effects and advanced drug delivery strategies for the delivery of apigenin.

Present study reports analgesic and anti-inflammatory potential of Piper betel (L.) leaf oil loaded lipid nanocarrier (BLNs)-embedded bigel. BLNs were developed by solvent evaporation technique and were characterised by FESEM, Cryo-TEM, mean diameter, zeta potential, loading efficiency, etc. BLNs embedded bigel (BLNs-G) was evaluated for analgesic and anti-inflammatory efficacy in rat model. Data showed spherical BLNs with intact lamellarity, 138.2 ± 1.08 nm mean diameter, 0.182 PDI, -46.6 ± 0.61 mV zeta potential, 76.2 ± 2.1% (w/w) loading efficiency and a sustained release in vitro. BLNs-G was homogenous with satisfied viscosity (40 734 ± 1.7 cps), spreadability (8.3 ± 1.5 g.cm sec^-1), extrudability (91.33 ± 1.3% w/w) along with a sustained permeation ex vivo. Significant analgesic and anti-inflammatory action were depicted by BLNs-G (1% w/w) in rat model (p ˂ 0.05) within 30 minutes post topical application. In silico docking study revealed high affinity of major phytoactive components with key analgesic/inflammatory mediators. Further pre-clinical investigations are warranted for futuristic clinical application of BLNs-G.

The aim of research is to enhance the solubility of crystalline gefitinib (GF), a poorly water-soluble drug, by developing drug delivery systems using chitosan oligosaccharide (COS) particle engineering. Fabrication utilizes ionic gelation followed by spray drying. The preliminary evaluations such as Uv-Vis, FTIR, DSC followed by advanced techniques like SEM and invitro drug release characteristics was performed along with solubility study. The spray-dried particles measured a mean diameter of 3.18 ± 0.5 microns, %EE as well as load w/w improved from 63.25 ± 2.1% and 37.98 ± 1.5% w/w (COS nanoparticles) to 78.15 ± 2.6% and 45.34 ± 1.6% w/w (engineered microparticles), respectively. The zeta potential and in vitro studies demonstrated 41 ± 3.5 mV and 92 ± 2.1% (w/w) release suggest long-term stability and prolonged release. This novel engineering approach effectively enhances GF solubility and surface characteristics, offering promising potential for improving delivery characteristics.

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.

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.

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.

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.

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.