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Current Pharmaceutical Design Jun 2024Diabetes mellitus is a global disease identified by hyperglycemia due to defects in insulin secretion, insulin action, or both.
BACKGROUND
Diabetes mellitus is a global disease identified by hyperglycemia due to defects in insulin secretion, insulin action, or both.
OBJECTIVE
The main objective of this research was to evaluate the ability of gelatinized Poly(ethylene glycol) (PEG) microparticles to be used as carriers for oral insulin delivery via double emulsion preparation.
METHODS
Five different batches of the formulation consisting of gelatin:PEG were prepared as follows: 0:1 (W1), 1:0 (W2), 1:1 (W3), 1:3 (W4), and 3:1 (W5). The prepared microparticles (from insulin-loaded batches) had particle sizes ranging from 19.5 ± 0.32-23.9 ± 0.22 μm and encapsulation and loading capacities ranging from 78.8 ± 0.24-88.9 ± 0.95 and 22.2 ± 0.96-29.7 ± 0.86%, respectively. The minimum and maximum in vitro release rates were 8.0 and 66.0%, respectively, for batches W1 and W2 at 8 h.
RESULTS
Insulin-loaded MPs induced a significant decrease in glucose levels, with a reduction from 100 to 33.35% in batch W5 at 9 h compared to that of subcutaneous insulin (100 to 22.63%). A liver function study showed that the formulation caused no obvious toxicity to the experimental rats.
CONCLUSION
Gelatinized PEG-based microparticles as insulin delivery systems may open a new window into the development of oral insulin for diabetic treatment.
PubMed: 38847248
DOI: 10.2174/0113816128309449240527053640 -
Heliyon Jun 2024In drug delivery, it is common to use porous particles as carrier media, instead of dense particles, due to their high specific surface area and available entrapment...
In drug delivery, it is common to use porous particles as carrier media, instead of dense particles, due to their high specific surface area and available entrapment volume, which allows a higher amount of drug to be encapsulated and then released. Chitosan microparticles are extensively used in drug delivery, but porous chitosan microparticles are scarcely reported. In this work, the preparation of porous chitosan microparticles using membrane emulsification is addressed, a technology that involves mild operating conditions and less energy consumption than traditional methods (such as ultrasound), and with higher control of the particle size. The dense structure is obtained by a water-in-oil emulsion. The porous structure is obtained by a gas-in-water-in-oil G/W/O double emulsion, where argon bubbles get entrapped in an aqueous chitosan solution that is further emulsified in a paraffin/petroleum ether mixture. Porous chitosan particles were obtained with sizes of 7.7 ± 1.6 μm, which was comparable with dense chitosan particles (6.2 ± 2.3 μm). The pore structure was optimized by varying the argon flow rate, being optimized at 0.24 L h. The impact of drug loading by adsorption or encapsulation, and of the drug release behaviour when using porous and dense particles were assessed, using the protein bovine serum albumin (BSA) as a model drug. The results showed that by encapsulating BSA the loading efficiency was above 95 % for both types of particles, with the release being slightly slower for the dense particles. As for the adsorbed BSA, the loading efficiency was significantly higher for porous particles - 70 % - against the 40 % for dense particles. Porous chitosan particles were successfully obtained using the membrane emulsification technology and showed that these carriers are advantageous regarding drug loading and release.
PubMed: 38845862
DOI: 10.1016/j.heliyon.2024.e31823 -
International Journal of Biological... Jun 2024As a translucent functional gel with biodegradability, non-toxicity and acid resistance, gellan gum has been widely used in probiotic packaging, drug delivery, wound... (Review)
Review
As a translucent functional gel with biodegradability, non-toxicity and acid resistance, gellan gum has been widely used in probiotic packaging, drug delivery, wound dressing, metal ion adsorption and other fields in recent years. Because of its remarkable gelation characteristics, gellan gum is suitable as the shell material of microcapsules to encapsulate functional substances, by which the functional components can improve stability and achieve delayed release. In recent years, many academically or commercially reliable products have rapidly emerged, but there is still a lack of relevant reports on in-depth research and systematic summaries regarding the process of microcapsule formation and its corresponding mechanisms. To address this challenge, this review focuses on the formation process and applications of gellan gum-based microcapsules, and details the commonly used preparation methods in microcapsule production. Additionally, it explores the impact of factors such as ion types, ion strength, temperature, pH, and others present in the solution on the performance of the microcapsules. On this basis, it summarizes and analyzes the prospects of gellan gum-based microcapsule products. The comprehensive insights from this review are expected to provide inspiration and design ideas for researchers.
Topics: Polysaccharides, Bacterial; Capsules; Emulsions; Hydrogen-Ion Concentration; Temperature
PubMed: 38843607
DOI: 10.1016/j.ijbiomac.2024.132697 -
PloS One 2024A Pickering emulsion was synergistically stabilised with zein nanoparticles (ZNPs) and starch nanocrystals (SNCs) to prepare it for menthol loading. After response...
Synergistic stabilization of a menthol Pickering emulsion by zein nanoparticles and starch nanocrystals: Preparation, structural characterization, and functional properties.
A Pickering emulsion was synergistically stabilised with zein nanoparticles (ZNPs) and starch nanocrystals (SNCs) to prepare it for menthol loading. After response surface optimisation of the emulsion preparation conditions, a Pickering emulsion prepared with a ZNPs:SNCs ratio of 1:1, a particle concentration of 2 wt% and a water:oil ratio of 1:1 provided the highest menthol encapsulation rate of the emulsions tested (83%) with good storage stability within 30 days. We examined the bilayer interface structure of the emulsion by optical microscopy, scanning electron microscopy, and confocal laser scanning microscopy. The results of simulated digestion experiments showed that the release rate of free fatty acid was 75.06 ± 1.23%, which ensured bioavailability. At the same time, the emulsions facilitated the slow release of menthol. Bacteriostatic studies revealed that the Pickering emulsion had a protective effect on menthol, with the most significant inhibitory effects on Escherichia coli and Staphylococcus aureus under the same conditions. Overall, this study proposes a novel approach for the application and development of l-menthol by combining it with Pickering emulsion.
Topics: Menthol; Emulsions; Nanoparticles; Zein; Starch; Staphylococcus aureus; Escherichia coli; Anti-Bacterial Agents; Particle Size
PubMed: 38843222
DOI: 10.1371/journal.pone.0303964 -
The Journal of Emergency Medicine Jun 2024
Topics: Humans; Tramadol; Fat Emulsions, Intravenous; Analgesics, Opioid; Blood Pressure; Male; Female
PubMed: 38839133
DOI: 10.1016/j.jemermed.2024.02.012 -
Journal of Colloid and Interface Science May 2024Understanding the digestion of lipid-based pharmaceutical formulations and food systems is necessary for optimising drug and nutrient delivery and has been extensively...
HYPOTHESIS
Understanding the digestion of lipid-based pharmaceutical formulations and food systems is necessary for optimising drug and nutrient delivery and has been extensively studied in bulk emulsion systems using the pH-stat method [1]. However, this approach is not suitable for investigation of individual lipid droplets, in particular the interface where the lipase acts. Microfluidic approaches to study digestion at lipid-water interfaces using droplet trapping have been proposed, however the aqueous phase in that case washes over the interface presenting uncertainty over the stoichiometry of interactions [2]. The internal interface of a Janus-like droplet, containing distinct aqueous and lipid compartments, mimics the interface of a lipid droplet in aqueous solution with controlled stoichiometry [3]. Hence, it was hypothesised that the internal interface of Janus droplets can offer a precise way to study the enzymatic digestion of lipids formulations.
EXPERIMENTS
Using microfluidic methods, Janus-like droplets were formed by coalescing emulsion droplets containing lipid formulation and pancreatic lipase. Polarised light microscopy (PLM) and in-situ small-angle X-ray scattering (SAXS) were used to investigate the droplets.
FINDINGS
PLM revealed the growth of an aligned inverse hexagonal phase (H), and with SAXS showed that this phase transformation and alignment resulted from enzymatic digestion. A subsequent partial transformation from H to inverse bicontinuous cubic phase occurred when simulated intestinal fluid was used instead of Tris buffer. Suggesting that phospholipids and bile salts could diffuse across the internal interface to locally affect their surroundings.
PubMed: 38838633
DOI: 10.1016/j.jcis.2024.05.087 -
Artificial Cells, Nanomedicine, and... Dec 2024Cell encapsulation into spherical microparticles is a promising bioengineering tool in many fields, including 3D cancer modelling and pre-clinical drug discovery. Cancer... (Review)
Review
Cell encapsulation into spherical microparticles is a promising bioengineering tool in many fields, including 3D cancer modelling and pre-clinical drug discovery. Cancer microencapsulation models can more accurately reflect the complex solid tumour microenvironment than 2D cell culture and therefore would improve drug discovery efforts. However, these microcapsules, typically in the range of 1 - 5000 µm in diameter, must be carefully designed and amenable to high-throughput production. This review therefore aims to outline important considerations in the design of cancer cell microencapsulation models for drug discovery applications and examine current techniques to produce these. Extrusion (dripping) droplet generation and emulsion-based techniques are highlighted and their suitability to high-throughput drug screening in terms of tumour physiology and ease of scale up is evaluated.
Topics: Humans; Neoplasms; Drug Discovery; Cell Encapsulation; Models, Biological; Capsules; Animals; Drug Compounding; Tumor Microenvironment
PubMed: 38829715
DOI: 10.1080/21691401.2024.2359996 -
International Journal of Nanomedicine 2024Due to its prevalence, recurrence, and the emergence of drug-resistance, vaginitis significantly impacts the well-being of women. Although cinnamon essential oil (CEO)...
BACKGROUND
Due to its prevalence, recurrence, and the emergence of drug-resistance, vaginitis significantly impacts the well-being of women. Although cinnamon essential oil (CEO) possesses antifungal activity, its hydrophobic properties limit its clinical application.
PURPOSE
To overcome this challenge, a nanoemulsification technology was employed to prepare cinnamon essential oil-nanoemulsion (CEO@NE), and its therapeutic efficacy and action mechanism for vaginitis was investigated in vivo and in vitro.
MATERIALS AND METHODS
CEO@NE, composed of 4% CEO, 78% distilled water, and 18% Tween 80, was prepared by ultrasonic nanoemulsification. The physical properties, anti- activity, cytotoxicity, immunomodulatory potential and storage stability of CEO@NE were explored. Subsequently, the effect of intravaginal CEO@NE treatment on vaginitis was investigated in mice. To comprehend the possible mechanism of CEO@NE, an analysis was conducted to ascertain the production of intracellular reactive oxygen species (ROS) in .
RESULTS
CEO@NE, with the droplet size less than 100 nm and robust storage stability for up to 8 weeks, exhibited comparable anti- activity with CEO. CEO@NE at the concentration lower than 400 μg/mL had no cytotoxic and immunomodulatory effects on murine splenocytes. Intravaginal treatment of CEO@NE (400 μg/mL, 20 μL/day/mouse for 5 consecutive days) curbed colonization, ameliorated histopathological changes, and suppressed inflammatory cytokine production in mice intravaginally challenged with . Notably, this treatment preserved the density of vaginal lactic acid bacteria (LAB) crucial for vaginal health. Co-culturing with CEO@NE revealed concentration-dependent augmentation of intracellular ROS generation and ensuing cell death. In addition, co-culturing LPS-stimulated murine splenocytes with CEO@NE yielded a decrease in the generation of cytokines.
CONCLUSION
This discovery provides insight into the conceivable antifungal and anti-inflammatory mechanisms of CEO@NE to tackle vaginitis. CEO@NE offers a promising avenue to address the limitations of current treatments, providing novel strategy for treating vaginitis.
Topics: Female; Animals; Oils, Volatile; Candidiasis, Vulvovaginal; Candida albicans; Antifungal Agents; Mice; Administration, Intravaginal; Cinnamomum zeylanicum; Emulsions; Reactive Oxygen Species; Humans; Nanoparticles; Mice, Inbred BALB C
PubMed: 38828194
DOI: 10.2147/IJN.S458593 -
Journal of Nanobiotechnology Jun 2024Targeted alpha therapy (TAT) relies on chemical affinity or active targeting using radioimmunoconjugates as strategies to deliver α-emitting radionuclides to cancerous...
Targeted alpha therapy (TAT) relies on chemical affinity or active targeting using radioimmunoconjugates as strategies to deliver α-emitting radionuclides to cancerous tissue. These strategies can be affected by transmetalation of the parent radionuclide by competing ions in vivo and the bond-breaking recoil energy of decay daughters. The retention of α-emitting radionuclides and the dose delivered to cancer cells are influenced by these processes. Encapsulating α-emitting radionuclides within nanoparticles can help overcome many of these challenges. Poly(lactic-co-glycolic acid) (PLGA) nanoparticles are a biodegradable and biocompatible delivery platform that has been used for drug delivery. In this study, PLGA nanoparticles are utilized for encapsulation and retention of actinium-225 ([Ac]Ac). Encapsulation of [Ac]Ac within PLGA nanoparticles (Z = 155.3 nm) was achieved by adapting a double-emulsion solvent evaporation method. The encapsulation efficiency was affected by both the solvent conditions and the chelation of [Ac]Ac. Chelation of [Ac]Ac to a lipophilic 2,9-bis-lactam-1,10-phenanthroline ligand ([Ac]AcBLPhen) significantly decreased its release (< 2%) and that of its decay daughters (< 50%) from PLGA nanoparticles. PLGA nanoparticles encapsulating [Ac]AcBLPhen significantly increased the delivery of [Ac]Ac to murine (E0771) and human (MCF-7 and MDA-MB-231) breast cancer cells with a concomitant increase in cell death over free [Ac]Ac in solution. These results demonstrate that PLGA nanoparticles have potential as radionuclide delivery platforms for TAT to advance precision radiotherapy for cancer. In addition, this technology offers an alternative use for ligands with poor aqueous solubility, low stability, or low affinity, allowing them to be repurposed for TAT by encapsulation within PLGA nanoparticles.
Topics: Nanoparticles; Polylactic Acid-Polyglycolic Acid Copolymer; Actinium; Humans; Cell Line, Tumor; Animals; Alpha Particles; Mice; Female; Biocompatible Materials; Breast Neoplasms; Radioimmunotherapy
PubMed: 38825717
DOI: 10.1186/s12951-024-02520-6 -
International Journal of Biological... Jun 2024A stable Madhuca indica oil-in-water nanoemulsion (99-210 nm, zeta potential: > - 30 mV) was produced employing Tween 20 (surfactant) and Transcutol P...
A stable Madhuca indica oil-in-water nanoemulsion (99-210 nm, zeta potential: > - 30 mV) was produced employing Tween 20 (surfactant) and Transcutol P (co-surfactant) (3:1). The nanoemulsion (oil: S = 3:7, 5:5, and 7:3) were subsequently incorporated into oxcarbazepine-loaded carboxymethylxanthan gum (DS = 1.23) dispersion. The hydrogel microspheres were formed using the ionic gelation process. Higher oil concentration had a considerable impact on particle size, drug entrapment efficiency, and buoyancy. The maximum 92 % drug entrapment efficiency was achieved with the microspheres having oil: S ratio 5:5. FESEM study revealed that the microspheres were spherical in shape and had an orange peel-like surface roughness. FTIR analysis revealed a hydrogen bonding interaction between drug and polymer. Thermal and x-ray examinations revealed the transformation of crystalline oxcarbazepine into an amorphous form. The microspheres had a buoyancy period of 7.5 h with corresponding release of around 83 % drug in 8 h in simulated stomach fluid, governed by supercase-II transport mechanism. In vivo neurobehavioral studies on PTZ-induced rats demonstrated that the microspheres outperformed drug suspension in terms of rotarod retention, number of crossings, and rearing activity in open field. Thus, Madhuca indica oil-in-water nanoemulsion-entrapped carboxymethyl xanthan gum microspheres appeared to be useful for monitoring oxcarbazepine release and managing epileptic seizures.
Topics: Microspheres; Animals; Rats; Mannans; Hydrogels; Particle Size; Epilepsy; Male; Drug Carriers; Emulsions; Seizures; Drug Liberation; Plant Oils; Anticonvulsants; Galactose
PubMed: 38825290
DOI: 10.1016/j.ijbiomac.2024.132739