Journal of microencapsulation最新文献

Aim: To determine the optimum condition for preparing chitooligosaccharide-catechin conjugate (COS-CAT) liposomes using different stabilising agents.

Methods: COS-CAT liposomes (0.1-1%, w/v) were prepared using soy phosphatidylcholine (SPC) (50-200 mM) and glycerol or cholesterol (25-100 mg). Encapsulation efficiency (EE), loading capacity (LC), physicochemical characteristics, FTIR spectra, thermal stability, and structure of COS-CAT liposomes were assessed.

Results: COS-CAT loaded liposome stabilised by cholesterol (COS-CAT-CHO) showed higher stability as shown by the highest EE (76.81%) and LC (4.57%) and the lowest zeta potential (ZP) (-76.51 mV), polydispersity index (PDI) (0.2674) and releasing efficiency (RE) (53.54%) (p < 0.05). COS-CAT-CHO showed the highest retention and relative remaining bioactivities of COS-CAT under various conditions (p < 0.05). FTIR spectra revealed the interaction between the choline group of SPC and -OH groups of COS-CAT. Phase transition temperature of COS-CAT-CHO was shifted to 184 °C, which was higher than others (p < 0.05).

Conclusion: SPC and cholesterol-based liposome could be used as a promising vesicle for maintaining bioactivities of COS-CAT.

This study aimed to prepare piperine (PIP) loaded liposomes in hyaluronic acid (HA) hydrogel to provide a hybrid superstructure for postoperative adhesion prevention. Liposomes were prepared using thin-film hydration method. The optimised formulation was characterised by size, SEM, TEM, FTIR, encapsulation efficiency (EE)% (w/w), and release pattern. Liposome-in-hydrogel formulation was investigated by rheology, SEM, and release studies. The efficacy was evaluated in a rat peritoneal abrasion model. EE% (w/w) increased with increasing lipid concentration from 10 to 30; however, a higher percentage of Chol reduced EE% (w/w). The optimised liposome (EE: 68.10 ± 1.71% (w/w), average diameter: 513 ± 8 nm, PDI: 0.15 ± 0.04) was used for hydrogel embedding. No sign of adhesion in 5/8 rats and no collagen deposition confirmed the in vivo effectiveness of the optimised formulation. Overall, providing a sustained delivery of PIP, the developed liposome-in-hydrogel formulation can be a promising carrier to prevent postoperative adhesion.

Azithromycin is an antibiotic proposed as a treatment for the coronavirus disease 2019 (COVID-19) due to its immunomodulatory activity. The aim of this study is to develop dry powder formulations of azithromycin-loaded poly(lactic-co-glycolic acid) (PLGA) nanocomposite microparticles for pulmonary delivery to improve the low bioavailability of azithromycin. Double emulsion method was used to produce nanoparticles, which were then spray dried to form nanocomposite microparticles. Encapsulation efficiency and drug loading were analysed, and formulations were characterised by particle size, zeta potential, morphology, crystallinity and in-vitro aerosol dispersion performance. The addition of chitosan changed the neutrally-charged azithromycin only formulation to positively-charged nanoparticles. However, the addition of chitosan also increased the particle size of the formulations. It was observed in the NGI^® data that there was an improvement in dispersibility of the chitosan-related formulations. It was demonstrated in this study that all dry powder formulations were able to deliver azithromycin to the deep lung regions, which suggested the potential of using azithromycin via pulmonary drug delivery as an effective method to treat COVID-19.

The purpose of this study was to evaluate the drug delivery and therapeutic potential of berberine (Br) loaded nanoformulation in rheumatoid arthritis (RA)-induced animal model. The Br-loaded NLCs (nanostructured lipid carriers) were prepared employing melt-emulsification process, and optimised through Box-Behnken design. The prepared NLCs were assessed for in-vitro and in-vivo evaluations. The optimised NLCs exhibited a mean diameter of 180.2 ± 0.31 nm with 88.32 ± 2.43% entrapment efficiency. An enhanced anti-arthritic activity with reduced arthritic scores to 0.66 ± 0.51, reduction in ankle diameter to 5.80 ± 0.27 mm, decline in paw withdrawal timing, and improvements in walking behaviour were observed in the Br-NLCs treated group. The radiographic images revealed a reduction in bone and cartilage deformation. The Br-NLCs showed promising results in the management of RA disease, can be developed as an efficient delivery system at commercial levels, and may be explored for clinical application after suitable experiments in the future.

The aims of this study were to develop co-delivery systems of paclitaxel (PTX) and etoposide prodrug (4'-O-benzyloxycarbonyl-etoposide, ETP-cbz) based on non-cross-linked human serum albumin (HSA) and poly(lactide-co-glycolide) nanoparticles and to evaluate the synergistic potential of these drugs in vitro. The nanoformulations were prepared by the high-pressure homogenisation technique and characterised using DLS, TEM, SEM, AFM, HPLC, CZE, in-vitro release, and cytotoxicity in human and murine glioma cells. All nanoparticles had 90-150 nm in size and negative ζ-potentials. The Neuro2A cells were the most sensitive to both HSA- and PLGA-based co-delivery systems (IC₅₀ 0.024 µM and 0.053 µM, respectively). The drugs' synergistic effect (combination index < 0.9) was observed in the GL261 cells for both types of co-delivery formulations and in the Neuro2A cells for the HSA-based system. These nanodelivery systems may be useful to improve combination chemotherapy for brain tumour treatment. To our knowledge, this is the first report describing the non-cross-linked HSA-based co-delivery nanosuspension which was prepared using nab™ technology.

Controlled release formulations of Ruta essential oil obtained by ionic gelation were developed. The presence of rue essential oil in the alginate and chitosan capsules was evidenced by Fourier transform infrared spectroscopy and differential scanning calorimetry. Release studies revealed that in acidic conditions (pH 4.2), the CHS-REO particles reached a Sw of 240% (w/w) in 30 days and 101% (w/w) for ALG-REO particles, generating a RR of 23.7% for CHS-REO and 20.4% for ALG-REO. On the other hand, at pH 6.8 it favored the Sw for ALG-REO 840% (w/w) and therefore the RR (45.6%) and disfavored the Sw of CHS-REO generating low RR (16.9%). Encapsulated rue essential oil showed equal or superior nematicidal activity against the nematode Melodogyne ssp., compared to free oil and a synthetic nematicide such as Carbofuran, without having a phytotoxic effect on the plant. This study revealed that REO encapsulated in biopolymeric matrices can be used as new nematicide formulations.

This study aimed to produce and characterise microparticles produced from barley residue proteins (BRP) enriched with β-carotene. The microparticles were obtained by freeze-drying five emulsion formulations with 0.5% w/w whey protein concentrate and different concentrations of maltodextrin and BRP (0, 1.5, 3.0, 4.5 and 6.0% w/w), with the dispersed phase consisting of corn oil enriched with β-carotene. The mixtures were mechanically mixed and sonicated, the formed emulsions were freeze-drying. The microparticles obtained were tested for encapsulation efficiency, humidity, hygroscopicity, apparent density, scanning electron microscopy (SEM), accelerated stability and bioaccessibility. Microparticles produced with the emulsion containing 6% w/w BRP had lower moisture content (3.47 ± 0.05%), higher encapsulation efficiency (69.11 ± 3.36%), bioaccessibility value of 84.1% and greater β-carotene protection against thermal degradation. SEM analysis showed that microparticles had sizes ranging from 74.4 to 244.8 µm. These results show that BRP are viable for the microencapsulation of bioactive compounds by freeze-drying.

Purpose: The study was aimed to encapsulate Hedyotis corymbosa extract (HCE) into phytosomes to improve its therapeutic efficacy in neuropathic pain by enhancing the bioavailability of chief chemical constituent Hedycoryside -A (HCA).

Methods: For preparing phytosomes complexes (F1, F2, and F3), HCE and phospholipids were reacted in disparate ratio. F2 was chosen to assess its therapeutic efficacy in neuropathic pain induced by partial sciatic nerve ligation. Nociceptive threshold and oral bioavailability were also estimated for F2.

Results: Particle size, zeta potential and entrapment efficiency for F2 were analysed as 298.1 ± 1.1 nm, -3.92 ± 0.41 mV and 72.12 ± 0.72% respectively. F2 gave enhanced relative bioavailability (158.92%) of HCA along with a greater neuroprotective potential showing a significant antioxidant effect and augmentation (p < 0.05) in nociceptive threshold with the diminution in damage to nerves.

Conclusion: F2 is an optimistic formulation for enhancing the HCE delivery for the effective treatment of neuropathic pain.

Current artificial ligaments based on polyethylene terephthalate (PET) are associated with some disadvantages due to their hydrophobicity and low biocompatibility. In this study, we aimed to modify the surface of PET using polyethylene glycol (PEG)-terminated polystyrene (PS)-linoleic nanoparticles (PLinaS-g-PEG-NPs). We accomplished that BMP-2 in two different concentrations encapsulated in nanoparticles with an efficiency of 99.71 ± 1.5 and 99.95 ± 2.8%. While the dynamic contact angle of plain PET surface reduced from 116° to 115° after a measurement periods of 10 s, that of PLinaS-g-PEG-NPs modified PET from 80° to 17.5° within 0.35 s. According to in vitro BMP2 release study, BMP-2 was released 13.12 ± 1.76% and 45.47 ± 1.78% from 0.05 and 0.1BMP2-PLinaS-g-PEG-NPs modified PET at the end of 20 days, respectively. Findings from this study revealed that BMP2-PLinaS-g-PEG-NPs has a great potential to improve the artificial PET ligaments, and could be effectively applied for ACL reconstruction.

Encapsulation is the way to wrap or coat one substance as a core inside another tiny substance known as a shell at micro and nano scale for protecting the active ingredients from the exterior environment. A lot of active substances, such as flavours, enzymes, drugs, pesticides, vitamins, in addition to catalysts being effectively encapsulated within capsules consisting of different natural as well as synthetic polymers comprising poly(methacrylate), poly(ethylene glycol), cellulose, poly(lactide), poly(styrene), gelatine, poly(lactide-co-glycolide)s, and acacia. The developed capsules release the enclosed substance conveniently and in time through numerous mechanisms, reliant on the ultimate use of final products. Such technology is important for several fields counting food, pharmaceutical, cosmetics, agriculture, and textile industries. The present review focuses on the most important and high-efficiency methods for manufacturing micro/nanocapsules and their several applications in our life.