Journal of microencapsulation最新文献

Osteoarthritis is considered a degenerative joint disease that is characterised by inflammation, chronic pain, and functional limitation. The increasing development of nanotechnology in drug delivery systems has provided new ideas and methods for osteoarthritis therapy. This review aimed to evaluate patents that have developed innovations, therapeutic strategies, and alternatives using nanotechnology in osteoarthritis treatment. The results show patents deposited from 2015 to November 2021 in the online databases European Patent Office and World Intellectual Property Organisation. A total of 651 patents were identified for preliminary assessment and 16 were selected for full reading and discussion. The evaluated patents are focused on the intraarticular route, oral route, and topical route for osteoarthritis treatment. The intraarticular route presented a higher patent number, followed by the oral and topical routes, respectively. The development of new technologies allows us to envision a promising and positive future in osteoarthritis treatment.

The aims of this study were to systematically optimise a formula for eugenol emulsions via face-centered central composite design and to assess the activity against two-different bacterial strains (Staphylococcus aureus and Propionibacterium acnes) present at planktonic and biofilm forms. The molecular interaction of excipients, mean particle size (MPS) including zeta potential (ZP), drug entrapment efficiency (DEE) and in vitro drug release of optimised emulsions was done using FT-IR, Malvern Zetasizer, ultracentrifugation technique and membrane-free dissolution model, respectively. The emulsions consisted of 151.3 ± 1.45 nm MPS, -21.3 ± 1.25 mV ZP and 93.98 ± 1.41% DEE values. On storage of emulsions at 25 °C for 3 months, the value of DEE was found to be 72.12 ± 2.82%. The Tween 80 emulsifier film coverage onto the dispersed eugenol droplets of emulsions delayed significantly the drug release (12%-19%) compared to the drug release occurred from pure eugenol. The treatment of planktonic S. aureus and P. acnes with diluted eugenol emulsions showed the minimum inhibitory concentration and minimum bactericidal concentration values at 1.25-2.5 mg/ml whereas it occurred at 10 mg/ml for pure eugenol. Treating the biofilms with eugenol emulsions (1-2 mg/ml) yielded 59-70% minimum biofilm eradication concentration but 10 mg/ml pure eugenol showed 60%. Hence, the eugenol emulsions displayed antibacterial activity and could be projected as an antibiofilm or biofilm disruption agent.

To improve survival during storage and exposure to adverse conditions, Bacillus subtilis was microencapsulated with oat β-glucan by spray-drying technology. The characterisation of the microcapsules was designed to compare free and microencapsulated cells through exposure to simulated gastric fluids (SGF) throughout storage for 90 days at different temperatures. The characterisation included analysis of efficiency, morphology, moisture, water activity, hygroscopicity, particle size, and zeta potential. The microcapsules presented a particle size of 1.5 ± 0.34 μm and an encapsulation efficiency of 77.9 ± 3.06%. After SGF, the survival of microencapsulated cells was 8.4 ± 0.07 log CFU mL^-1 while that of free cells was 7.6 ± 0.06 log CFU mL^-1. After 90 days of storage, only microencapsulated cells remained above 6 log-unit of viability. In conclusion, spray-drying technique combined with the addition of oat β-glucan proved to be an efficient method to protect B. subtilis under storage and SGF with potential application in fish feed.

The proposed research aims to develop Tacrolimus-loaded nanostructured lipid carriers (TAC-loaded NLCs) to overcome poor aqueous solubility and dissolution rate to enhance its oral absorption. A central composite design was used to optimise the amount of Poloxamer 188 and D-α-Tocopherol-polyethylene-glycol-succinate (TPGS). The optimised TAC-loaded NLCs contain stearic acid (250 mg), Moringa oleifera (MO) seed oil (50 mg), TAC (Tacrolimus: 10 mg), TPGS (60 mg), and Poloxamer 188 (1% w/v) with a mean diameter of 393.3 ± 29.68 nm, a zeta potential of -18.3 ± 6.19 mV, high entrapment efficiency (92.12 ± 1.14% w/w), and desirability (0.989). TAC-loaded NLCs showed ∼12 times higher drug dissolution efficiency, while in-vitro anti-inflammatory studies showed ∼1.8 times lower IC₅₀ (half-maximal inhibitory concentration) than TAC suspension. The lyophilised TAC-loaded NLCs were found to be stable after 3 months. Thus, the present study concludes the successful encapsulation of TAC in NLCs made of stearic acid and MO seed oil.

The aim of this work was to investigate novel formulations containing diruthenium(II-III)-ibuprofen (RuIbp) metallodrug encapsulated into the chitosan (CT) biopolymer. Microparticles (RuIbp/CT MPs, ∼ 1 µm) were prepared by spray-drying, and RuIbp/CT-crosslinked nanoparticles (NPs) by ionic gelation (RuIbp/CT-TPP, TPP = tripolyphosphate (1), RuIbp/CT-TPP-PEG, PEG = poly(ethyleneglycol (2)) or pre-gel/polyelectrolyte complex method (RuIbp/CT-ALG, ALG = alginate (3)). Ru analysis was conducted by energy dispersive x-ray fluorescence or inductively coupled plasma atomic emission spectroscopy, and physicochemical characterisation by powder x-ray diffraction, electronic absorption and FTIR spectroscopies, electrospray ionisation mass spectrometry, thermal analysis, scanning electron, transition electron and atomic force microscopies, and dynamic light scattering. The RuIbp-loaded nanosystems exhibited encapsulation efficiency ∼ 20-37%, drug loading∼ 10-20% (w/w), hydrodynamic diameter (nm): 103.2 ± 7.9 (1), 91.7 ± 12.6 (2), 270.2 ± 58.4 (3), zeta potential (mV): +(47.7 ± 2.8) (1), +(49.2 ± 3.6) (2), -(28.2 ± 2.0) (3). Nanoformulation (1) showed the highest cytotoxicity with increased efficacy in relation to the RuIbp free metallodrug against U87MG human glioma cells.

The present study was aimed to prepare and examine in vitro novel dual-drug loaded delivery systems. Biodegradable nanoparticles based on poly(L-glutamic acid-co-D-phenylalanine) were used as nanocarriers for encapsulation of two drugs from the paclitaxel, irinotecan, and doxorubicin series. The developed delivery systems were characterised with hydrodynamic diameters less than 300 nm (PDI < 0.3). High encapsulation efficiencies (≥75%) were achieved for all single- and dual-drug formulations. The release studies showed faster release at acidic pH, with the release rate decreasing over time. The release patterns of the co-encapsulated forms of substances differed from those of the separately encapsulated drugs, suggesting differences in drug-polymer interactions. The joint action of encapsulated drugs was analysed using the colon cancer cells, both for the dual-drug delivery sytems and a mixture of single-drug formulations. The encapsulated forms of the drug combinations demonstrated comparable efficacy to the free forms, with the encapsulation enhancing solubility of the hydrophobic drug paclitaxel.

Objective: Encapsulation of esculetin into DSPE-MPEG2000 carrier was performed to improve its water solubility and oral bioavailability, as well as enhance its anti-inflammatory effect on a mouse model of ulcerative colitis that was induced with dextran sulphate sodium (DSS).

Methods: We determined the in-vitro and in-vivo high-performance liquid chromatographic (HPLC) analysis method of esculetin; Esculetin-loaded nanostructure lipid carrier (Esc-NLC) was prepared using a thin-film dispersion method, wherein a particle size analyser was used to measure the particle size (PS) and zeta potential (ZP) of the Esc-NLC, while a transmission electron microscope (TEM) was employed to observe its morphology. Also, HPLC was used to measure its drug loading (DL), encapsulation efficiency (EE) and the in-vitro release of the preparation, as well as investigate the pharmacokinetic parameters. In addition, its anti-colitis effect was evaluated via histopathological examination of HE-stained sections and detection of the concentrations of tumour necrosis factor-alpha (TNF-α), interleukin (IL)-1 beta (β), and IL-6 in serum with ELISA kits.

Results: The PS of Esc-NLC was 102.29 ± 0.63 nm with relative standard deviation (RSD) of 1.08% (with poly-dispersity index-PDI of 0.197 ± 0.023), while the ZP was -15.67 ± 1.39 mV with RSD of 1.24%. Solubility of esculetin was improved coupled with prolonged release time. Its pharmacokinetic parameters were compared with that of free esculetin, wherein the maximum concentration of the drug in plasma was increased by 5.5 times. Of note, bioavailability of the drug was increased by 1.7 times, while the half-life was prolonged by 2.4 times. In the anti-colitis efficacy experiment, the mice in Esc and Esc-NLC groups exhibited significantly reduced levels of TNF-α, IL-1β, and IL-6 in their sera comparable to the DSS group. Colon histopathological examination revealed that mice with ulcerative colitis in both Esc and Esc-NLC groups displayed improved inflammation, amid the Esc-NLC groups having the best prophylactic treatment effect.

Conclusion: Esc-NLC could ameliorate DSS-induced ulcerative colitis by improving bioavailability, prolonging drug release time and regulating cytokine release. This observation confirmed the potential of Esc-NLC to reduce inflammation in ulcerative colitis, albeit the need for follow-up research to verify the application of this strategy to clinical treatment of ulcerative colitis.

Aim: The aim of this manuscript was to fabricate agomelatine (AGM) loaded elastosomes to improve its corneal permeation and ocular bioavailability. AGM is a biopharmaceutical classification system (BCS) class II with low water solubility and high membrane permeability. It has a potent agonistic action on melatonin receptors, so it is used for glaucoma treatment.

Methods: Elastosomes were made using modified ethanol injection technique according to a 2² × 4¹ full factorial design. The chosen factors were: edge activators (EAs) type, surfactant percent (SAA %w/w), and cholesterol:surfactant ratio (CH:SAA ratio). The studied responses were encapsulation efficiency percent (EE%), mean diameter, polydispersity index (PDI), zeta potential (ZP), percentage of drug released after two hours (Q_2h%), and 24 hours (Q_24h%).

Results: The optimum formula with the desirability of 0.752 was composed of Brij98 as EA type, 15%w/w SAA%, and 1:1 CH:SAA ratio. It revealed EE% of 73.22%w/v and mean diameter, PDI, ZP, Q_2h%, and Q_24h% values of 484.25 nm, 0.31, -30.75 mV, 32.7%w/v, and 75.6%w/v, respectively. It demonstrated acceptable stability for three months and superior elasticity than its conventional liposome. The histopathological study ensured the tolerability of its ophthalmic application. Also, it was proven to be safe from the results of the pH and refractive index tests. The in vivo pharmacodynamic parameters of the optimum formula revealed dominance in a maximum % decrease in intraocular pressure (IOP), the area under the IOP response curve, and mean residence time with the value of 82.73%w/v, 820.69%h, and 13.98 h compared to that of the AGM solution (35.92%w/v, 181.30%h, and 7.52 h).

Conclusions: Elastosomes can be a promising option to improve AGM ocular bioavailability.

Aim: This work aimed to encapsulate Hypericum perforatum extract (HPE) into nanophytosomes (NPs) and assess the therapeutic efficacy of this nanocarrier in neuropathic pain induced by partial sciatic nerve ligation (PSNL).

Methods: Hydroalcoholic extract of Hypericum perforatum was prepared and encapsulated into NPs by thin layer hydration method. Particle size, zeta potential, TEM, differential scanning calorimetry (DSC), entrapment efficiency (%EE), and loading capacity (LC) of NPs were reported. The biochemical and histopathological examinations were measured in the sciatic nerve.

Results: Particle size, zeta potential, %EE, and LC were 104.7 ± 1.529 nm, -8.93 ± 1.71 mV, 87.23 ± 1.3%, and 53.12 ± 1.7%, respectively. TEM revealed well-formed and distinct vesicles. NPHPE (NPs of HPE) was significantly more effective than HPE in reducing PSNL-inducing pain. Antioxidant levels and sciatic nerve histology were reversed to normal with NPHPE.

Conclusions: This study demonstrates that encapsulating HPE with phytosomes is an effective therapeutic approach for neuropathic pain.

This study aimed to improve control over the curing behaviour of cold-mixed epoxy asphalt by using a microencapsulated curing agent (2-PZ@PC). Prepared through solvent evaporation, the 2-PZ@PC microcapsules had 2-phenylimidazole as the core material and polycarbonate as the shell material. The research examined the impact of core-shell mass ratio on microcapsule morphology and composition. Various equations, including the kinetics equation, Kissinger equation, Flynn-Wall-Ozawa, and Crane equations, were employed to assess the sustained release effect of 2-PZ@PC microcapsules on epoxy resin curing behaviour. Fluorescence microscopy and viscosity experiments were used to observe the release state of microcapsules and confirm the retardation phenomenon during construction. Optimal 2-PZ@PC microcapsules displayed a smooth spherical morphology and a maximum encapsulation rate of 32 wt% at a 1:1 core-shell ratio. The microencapsulated curing agent effectively regulated cold-mixed epoxy asphalt's curing behaviour, enhancing retention time control and application reliability.