Journal of microencapsulation最新文献

The aim is to prepare, characterise, and evaluate the biological activities and key molecular interactions of L-ascorbic acid and phosphatidylcholine (PC-AA) complex vesicles. PC-AA complexes were prepared and characterised using DLS, TEM, FTIR, UV-Vis, in-vitro release, bioactivities, and cytotoxicity. The key interactions of the AA with the PC were studied with MD simulations. PC-AA complex provides improved stability towards the degradation of AA in aqueous solutions while also slowing its release profile. The PC-AA complexes with an optimal molar ratio of PC: AA = 2.5:1 was shown to have a hydrodynamic diameter of 368.67 ± 4.65 nm and an EE of 68.16 ± 0.23%. At low concentration, the PC-AA complexes have no toxicity towards human dermal fibroblast cells over 48 h. Importantly, MD suggests that AA only forms the PC-AA complex when in its neutral form which is the desired active form. PC-AA complex could be a potential active to use in medicinal and cosmeceutical applications.

This study aims to fabricate core-shell clarithromycin (CAM) microcapsules to cover up the bitter taste of CAM by spray drying with aqueous polymer dispersion. Water dispersion of Eudragit EPO and Surelease^® were innovatively used to encapsulate CAM into microcapsules via a one-step spray-drying method. The inlet air temperature, airflow rate, CAM-polymer ratio, and particle size of CAM were optimised based on drug content and T_6% (the time taken for the drug to release equal to 6% w/w). The powder properties were assessed by measuring particle size and microstructure using SEM, FT-IR, and PXRD. Furthermore, selected batch was assessed for their drug content, encapsulation efficiency, in vitro release, bitterness, and stability studies. EPO-Surelease^® (1: 4) microcapsules had an average diameter (D50) of 37.69 ± 3.61 μm with a span of 2.395. The drug contents and encapsulation efficiency of EPO-Surelease^®(1:4) were 10.89% and 63.7%, respectively. EPO-Surelease^® (1:4) microcapsules prepared by spray drying with aqueous polymer dispersion can effectively mask the bitter taste of CAM.

Aim: The present study aimed to develop topical combinatorial therapy of nisin and 5-fluorouracil in a single nanosized formulation against skin cancer.

Methods: Nisin and 5-fluorouracil were encapsulated in an organogel system (NF-OG) and investigated for morphology, physicochemical properties, cytotoxicity, encapsulation and release. NF-OG was evaluated against DMBA/TPA murine skin cancer in terms of tumour statistics, histoarchitecture, TUNEL and M1/M2 macrophages.

Results: The optimised NF-OG formulation exhibited particle size of 185.1 ± 11.24 nm, zeta potential of -7.93 ± 0.60 mV, offered substantial drug loading and temporal release. NF-OG therapy led to improved cytotoxicity of nisin and 5-FU against B16-F10 cells, significant decrease in tumour volume (84.983 mm³) in treated group as compared to untreated group (490.482 mm³) accompanied by restoration of histoarchitecture and repolarization of macrophages.

Conclusion: The study yielded a promising delivery system exhibiting potent anticancer activity and forms the bases for further applications in clinical settings.

Solid lipid nanoparticles (SLNs) containing rutin were prepared to enhance their photochemopreventive effect on the skin. SLNs were produced by the hot melt microemulsion technique. Two 3D skin models: ex vivo skin explants and 3D tissue engineering skin were used to evaluate the photochemopreventive effect of topical formulations containing rutin SLNs, against ultraviolet B (UVB) radiation, inducing sunburn cells, caspase-3, cyclobutane pyrimidine dimers, lipid peroxidation, and metalloproteinase formation. The rutin SLNs presented average size of 74.22 ± 2.77 nm, polydispersion index of 0.16 ± 0.04, encapsulation efficiency of 98.90 ± 0.25%, and zeta potential of -53.0 ± 1.61 mV. The rutin SLNs were able to efficiently protect against UVB induced in the analysed parameters in both skin models. Furthermore, the rutin SLNs inhibited lipid peroxidation and metalloproteinase formation. These results support the use of rutin SLNs as skin photochemopreventive agents for topical application to the skin.

Microcapsules of Lactobacillus plantarum LN66 were prepared to improve the cell viability in simulated gastrointestinal and different packaging conditions. Microcapsules containing Lactobacillus plantarum LN66 were produced by complex coacervation followed by freeze drying and characterised by water activity, moisture content, size, encapsulation efficiency, SEM, FTIR, XRD, as well as the resistance of probiotics to the simulated gastrointestinal tract and storage under different packaging conditions. The microcapsules presented the particle size of 196.57 ± 1.46 μm and the encapsulation efficiency of 75.26 ± 1.95% (w/w). After simulated gastrointestinal conditions, viability of encapsulated cells was 71.33 ± 0.99% (w/w) and 70.39 ± 0.86% (w/w), separately, while that of free cells was only 45.45 ± 0.5% (w/w) and 8.59 ± 0.67% (w/w). Compared with aluminium foil, the viable cells in glass bottles at 4 °C and 25 °C was increased 1.1-fold and 1.4-fold, respectively. Complex coacervation could be considered an appropriate alternative to increase the viability of probiotics.

This study aimed to formulate the green, sustainable, and ecofriendly nanobiopesticides of Azadirachta indica with enhanced pest control efficacy. Nanoprecipitation method was used for the development of nanobiopesticides. Optimisation was done by response surface methodology. Nanoformulations were characterised by zetasizer, scanning electron microscopy, energy dispersive x-ray spectroscopy, atomic force microscopy, and Fourier transform infrared spectroscopy. Pesticidal potential of nanosuspensions was evaluated by insecticide impregnated filter paper method. Optimised nanobiopesticide showed an average particle size of 275.8 ± 0.95 nm, polydispersity index (PDI) 0.351 ± 0.002, and zeta potential of -33 ± 0.90 mV. Nanobiopesticides exhibited significantly higher mortality rates of 86.81 ± 3.04 and 84.97 ± 2.83% against Tribolium castaneum and Ryzopertha dominica, respectively, as compared to their crude extract. Minor change in particle size from 275.8 ± 0.95 to 298.8 ± 1.00 nm and PDI from 0.351 ± 0.002 to 0.445 ± 0.02 were observed after 3 months of storage at 4 °C. Pesticidal efficacy of A. indica was significantly enhanced by the formulation of its nanobiopesticides.

Anacardium occidentale (AO) possesses potent anti-diabetic properties, owing to its high phytochemicals content. This study attempted to maximise the efficacy of AO by encapsulating it in a solid lipid microparticle (SLMs) formulation. Leaves of AO were extracted with water and formulated into SLMs using a lipid matrix composed of P90H and Dika fat. Characterisation of the SLMs include morphology, particle size, pH, encapsulation efficiency percentage, in vitro release and anti-diabetic properties. SLMs were spherical with sizes ranging from 16.7 ± 0.8 µm to 40.12 ± 2.34 µm and had a fairly stable pH over time. Highest drug entrapment was 87%_. Batch A₂ exhibited an even release of 89%, sustained over time, and a mean percentage reduction in glucose of 25.9% at 12 h after oral administration to study animals. Anacardium occidentale-loaded SLMs exhibited a good hypoglycaemic effect and can be used in the management of diabetes.

To study the effects of nanocrystallisation technology on the intestinal absorption properties and antibacterial activity of florfenicol (FF). The florfenicol nanocrystals (FF-NC) were prepared by wet grinding and spray drying. Additionally, changes in particle size, charge, morphology, and dissolution of FF-NC in the long-term stability were monitored by laser particle sizer, TEM, SEM, paddle method, and the structure of FF-NC powder was characterised by nuclear magnetic resonance (NMR) test. The antibacterial activity, intestinal absorption and intestinal histocompatibility of FF-NC were investigated by the stiletto, mini broth dilution susceptibility test, in situ single-pass intestinal perfusion (SPIP) and haematoxylin-eosin (H-E) staining. After 12 months of storage, the particle size and zeta potential of FF-NC were 280.43 ± 8.21 nm and -19.64 ± 3.45 mV, and the electron microscopy results showed that FF-NC were nearly circular with no adhesion between particles. In addition, the drug loading, encapsulation efficiency, and dissolution of FF-NC did not change significantly during storage. The inhibition zone of FF-NC against Escherichia coli and Staphylococcus aureus was 21.37 ± 1.70 mm and 25.17 ± 2.47 mm, respectively. Compared with the FF, the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of FF-NC are reduced, and the absorption rate constant (K_a) and efficient permeability coefficient (P_eff) of FF-NC in the three intestinal segments were increased by 1.28, 0.25, and 9.10 times and 0.59, 0.17, and 6.0 times, respectively. The results of tissue sections showed that FF-NC had little damage to the small intestinal. Nanocrystallisation technology is an effective method to increase the intestinal absorption and antibacterial activity of FF.

This study aimed the development of fluorescent melamine-formaldehyde (MF)/polyamine coatings for labelling of prefabricated microcapsules and their tracking in composites. The composition of the fluorescent MF coatings was studied by FTIR spectroscopy, thermogravimetric analysis, and elemental analysis. The characteristics of the coatings and its deposition on different surfaces were investigated using optical and fluorescence microscopy and fluorescence spectroscopy. MF prepolymers were polymerised with tri- and polyamines yielding in fluorescent coatings without addition of fluorescent dyes. Both, MF/poly(ethylene imine) and MF/poly(vinyl amine) (PVAm) coated glass beads showed maximum fluorescence at an excitation wavelength of λ_max = 360 nm with the emission maxima at λ_max = 490 nm and λ_max = 410 nm, correspondingly. The MF/PVAm polymer was coated on diuron-poly(methyl methacrylate) microcapsules and tracked in highly filled composites (water-based plaster/paint) to show its applicability. MF/polyamine coatings were identified as promising materials for the fluorescent labelling of prefabricated microcapsules.

Background and aim: The study was to extend systemic circulation and biological half-life (t_1/2) of trans-resveratrol (RSV) using solid lipid nanoparticles (RSV-SLN) to improve its anti-cancer potential.

Methods: RSV-SLN was prepared by solvent emulsification evaporation technique and proceeded for evaluation like particle size, PDI, zeta potential, in vitro release, in vitro cytotoxicity, cellular internalisation, haemolysis and erythrocyte membrane integrity, platelet aggregation and pharmacokinetic studies in rats. Moreover, cancer cells accumulation of RSV-SLN also needs to be evaluated for proving their targeting ability.

Result: Prepared SLN showed 126.85 ± 12.09 nm particle size, -24.23 ± 3.27 mV Zeta potential and 74.67 ± 4.76%. release at 48 h and haemocompatible. The cellular internalisation image showed the SLN reach in a cytoplasm and nucleus of PC3 prostate cells. RSV-SLN exhibited high t_1/2 (8.22 ± 1.36 h) and 7.19 ± 0.69 h MRT (Mean residence time) and lower clearance i.e. 286.42 ± 13.64 mL/min/kg. The bio-distribution of RSV-SLN was found to be extremely high in prostate cells and accumulate 7.56 times greater than that of RSV solution.

Conclusion: The developed RSV-SLN can be applied as potential carrier for delivery of drug of chemotherapeutics at an extend systemic circulation and targeting efficiency at tumour site.