Increase In Encapsulation Efficiency Research Articles

Determination of antioxidant capacity of glutathione encapsulated in alginate microcapsules using spectrophotometric and electrochemical methods

This paper includes the preparation and physicochemical characterization of sodium alginate microcapsules intended for the oral administration of glutathione (GSH), a vital endogenous antioxidant in combating oxidative stress. Using various methods such as optical microscopy, FTIR spectrometry, and cyclic voltammetry, the morphology, chemical structure, release mechanism, and antioxidant capacity of the released glutathione in simulated digestive fluids (gastric medium with pH=2 and intestinal medium with pH=7.4, without enzymes) were analyzed. The results showed the stability of the alginate microcapsules in digestive fluids and highlighted an increase in encapsulation efficiency with higher concentrations of encapsulated glutathione. Additionally, it was shown that sodium alginate-based microcapsules exhibit different swelling capacities depending on the pH and glutathione concentration, showing remarkable potential for controlled delivery of the active compound. The in vitro release study demonstrated more efficient release of glutathione in simulated intestinal fluid (SIF) than in simulated gastric fluid (SGF). The calculation of the electrochemical index using cyclic voltammetry demonstrated superior antioxidant activity of encapsulated glutathione compared to free glutathione. Correlating the DPPH inhibition percentage with the electrochemical index showed high Pearson coefficients both in SGF and in SIF, indicating a good correlation between DPPH or ABTS free radical species inhibition and electrochemical measurements. Therefore, sodium alginate and glutathione microcapsules show potential for developing efficient delivery systems for glutathione or other pharmaceutical compounds.

QbD decorated ellagic acid loaded polymeric nanoparticles: Factors influencing desolvation method and preliminary evaluations

Polymeric nanoparticles are one of the emerging drug delivery systems in the field of oncology. Ellagic acid is a polyphenolic compound with vast effects like anti-cancer, anti-viral, and anti-oxidant. The ellagic acid nanoparticles was prepared by desolvation method. Formulating ellagic acid NPs using BSA enhances the stability and solubility of ellagic acid. Quality by design (QbD) based approach was adopted to improve the final quality and effectiveness of the formulation. The Critical quality attribute (CQAs) was defined and risk assessment was performed with the help of the Ishikawa fishbone diagram. Solubility analysis was done for the drug with methanol, ethanol, water, and acetone. Preliminary studies were performed to study the effect of type of desolvating agent, the concentration of polymer the pH of the polymer solution, amount of desolvating agent on the particle size and entrapment efficiency of the nanoparticles. A greater quantity of desolvating agent results in a narrower particle size because of thorough desolvation, and the increased encapsulation efficiency is linked to reduced protein-protein interactions. Desolvation process can cause the protein to gradually change structure, form clumps, and eventually form nanoparticles, so might be its shows increase in entrapment efficiency. A desolvating agent volume of 4 ml resulted in a particle size of 1724 ± 1.27 nm. When the amount of desolvating agent was increased to 6 ml and 8 ml, the particle size decreased to 160 ± 0.66 nm and 218 ± 0.47 nm, respectively. Fourier Transform Infrared Spectroscopy (FTIR) data showed no incompatibilities were observed between drug and polymer. In-vitro dissolution showed the nanoparticles may follow the control release pattern over 24 hours. All the formulated batches of zeta potential were found to be in the range −30 mV to +30 mV which indicated good colloidal stability of the NPs and the PDI value ranging from 0.18 to 2.8. The higher drug encapsulation of the drug was more than 50 % which gives higher drug release at a site of action and in-vitro drug release of more than 80 % may improve the dosage frequency. The in vitro drug release data was also studied by various kinetic models. The in vitro drug release analysis shows sustained release of drug from nanoparticles and follow Korsmeyer-Peppas model. All these findings were in good agreement which may open a new gateway for future research in the field of oral oncology.

Fabrication and characterization of long-lasting antifungal film containing cinnamaldehyde-loaded complex coacervation microcapsules based on gelatin and gum Arabic

A novel long-acting antifungal active film was successfully created, as an alternative to conventional chemical food preservatives. The antifungal films incorporated with cinnamaldehyde (CA) microcapsules achieved long-lasting antifungal activity, mitigated yellowing caused by the direct addition of CA, and showed improved flexibility properties. CA multinuclear microcapsules were produced using gelatin with a Bloom value of 200 and gum Arabic, resulting in increased encapsulation efficiency (99.86 %), good dispersibility and enhanced antifungal ability (inhibition zone diameter of 32 mm). These microcapsules can be incorporated into films as a sustained-release antifungal agent. Compared to unencapsulated CA, the addition of 1 % CA microcapsules reduced the ultraviolet transmittance (<36.40 %) of the film while maintaining visible-light transmittance (36.40 %–65.20 %), and improving its elongation at break (23.49 %). The water vapor permeability of the film was not affected by the inclusion of CA microcapsules below 0.25 %. Moreover, microcapsules can enhance the thermal properties of the film. Antifungal films incorporated with 0.5 %–2 % microcapsules may offer better long-acting inhibition against A. brasiliensis. This study presents a new promising pathway for food storage.

Inclusion Complexation of Remdesivir with Cyclodextrins: A Comprehensive Review on Combating Coronavirus Resistance—Current State and Future Perspectives

Cyclodextrin (CD) derivatives have gained significant attention in biomedical applications due to their remarkable biocompatibility, unique inclusion capabilities, and potential for functionalization. This review focuses on recent advancements in CD-based assemblies, specifically their role in improving drug delivery, emphasizing remdesivir (RMD). The review introduces CD materials and their versatile applications in self-assembly and supramolecular assembly. CD materials offer immense potential for designing drug delivery systems with enhanced activity. Their inherent inclusion capabilities enable the encapsulation of diverse therapeutic agents, including RMD, resulting in improved solubility, stability, and bioavailability. The recent advances in CD-based assemblies, focusing on their integration with RMD have been concentrated here. Various strategies for constructing these assemblies are discussed, including physical encapsulation, covalent conjugation, and surface functionalization techniques. Furthermore, exploring future directions in these fields has also been provided. Ongoing research efforts are directed toward developing novel CD derivatives with enhanced properties, such as increased encapsulation efficiency and improved release kinetics. Moreover, the integration of CD-based assemblies with advanced technologies such as nanomedicine and gene therapy holds tremendous promise for personalized medicine and precision therapeutics

Antimicrobial activity of nanoemulsion containing &lt;i&gt;Moringa oleifera&lt;/i&gt; seed protein

Plant-based antimicrobial substances have been recognized as antimicrobial agents. These peptides demonstrate antimicrobial properties against a wide range of pathogens. This study reports the efficacy of &lt;i&gt;Moringa oleifera &lt;/i&gt;nanoemulsion as an antimicrobial. &lt;i&gt;M. oleifera &lt;/i&gt;seed was defatted and the protein was extracted from the grounded seed, characterized, and formulated into nanoemulsions by spontaneous nanoemulsification. This method is economically and environmentally safe as the components of nanoemulsion are biodegradable. The formulation was evaluated for particle size, viscosity, pH, antimicrobial activity, and kill time assay. The nanoemulsion was nanosized (43.440 nm - 74.430 nm) with increased encapsulation efficiency in a dose-dependent manner and a suitable pH (5.91 ± 0.01 to 6.14 ± 0.01), excellent dynamic viscosity (32 ± 7 to 39 ± 0). The antimicrobial and minimum inhibitory concentration study displayed a wide range of effectiveness on &lt;i&gt;Pseudomonas aeruginosa&lt;/i&gt; and &lt;i&gt;Staphylococcus aureus&lt;/i&gt;, the time-kill assay showed moderate biocidal activity. Therefore, &lt;i&gt;M. oleifera &lt;/i&gt;seed protein nanoemulsion has the potential to act as antimicrobial.

Design of multiple-function matrix encapsulated with Marjoram extract to support cellular functions, stimulate collagen synthesis and decrease infection in wound

This study aimed to assess the role of the combination of design techniques of the engineered substrates, and the effect of encapsulating Marjoram (Origanum Majorana L.) into the matrix network was studied. To this end, PVA-PEG matrices were designed through 3 techniques of freeze–thaw (FT), the combination of both methods of freeze-drying and freeze-thawing(FT-FD), and ternary technique(freeze-drying,freeze-thawing,cross-linking(FT-FD/CL)), by combining equal volume ratios of both polymers. The results indicated the ternary technique can provide better physicochemical properties(porosity: 96%, lower degradation rate, higher modulus) compared to FT and FT-FD methods. Afterward, encapsulation of Marjoram-extracted bio-actives in the matrix network designed with the ternary technique demonstrated that the increase in the extract concentration up to 3% can increase encapsulation efficiency. The encapsulation also caused a more cohesive network by better bonding between functional groups in herbal biomolecules and polymer chains of the matrix. Mass transport mechanisms and release kinetics of matrix-encapsulated bio-actives indicated a deviation from Fickian diffusion and the release by diffusion and swelling process. Biologically, matrix-loaded herbal carbohydrate(Epi-alpha-Cadinol) improved fibroblast adhesion and distribution on the substrate surface, and led to the better synthesis of collagen fibers, especially in 3% herbal extract, and antibacterial activities owing to the controlled release of sesquiterpenoids and N-Acetyl-l-proline.

Complexation characteristics between acetylated starch and soy protein isolates and intestinal digestion behavior of the polymers encapsulated active compound

The interaction between acetylated starch (AS) and soy protein isolates (SPI) was investigated under different pH conditions, and their corresponding physicochemical properties of the complexes were investigated. This study found that, at pH9.0, the β-turn structure of the protein in the complexes changed into Random coil with the highest ratio, and the thermal stability of the complexes was found to be reduced, which was contributed to the destruction of the crystalline region to a large extent. Meanwhile, the confocal laser scanning microscopy (CLSM) results showed that the complexes demonstrated a dispersed phase at pH5.0, and the SPI structure unfolded maximum at pH9.0. Following the determination of the changes in the rheological property under the existence of NaCl and urea, it was proposed that electrostatic interaction was the major interaction force for all the three complexes. However, hydrophobic and hydrogen bonding forces also seemed to play a more important role for AS/SPI-pH9 complexes than either AS/SPI-pH2 or AS/SPI-pH5 complexes. Complexation significantly increased encapsulation efficiency and loading capacity of curcumin compared to their corresponding individual polymer, followed by a reduced release kinetics at intestinal fluid but not at simulate gastric fluid stage via an in vitro digestion.

Nanoliposomal Encapsulation of Capparis spinosa Extract and Its Application in Jelly Formulation.

This research aimed to encapsulate the Capparis spinosa fruit extract to increase its stability for incorporation into food products such as jelly or jelly powder. After extraction, the nanoliposomes containing the extract were prepared in ratios of 60-0, 50-10, 40-20, and 30-30 lecithin-to-cholesterol. The effects of lecithin-to-cholesterol concentrations on the related parameters were then evaluated. The results showed that the average particle size was in the range of 95.05 to 164.25 nm, and with an increasing cholesterol concentration, the particle size of the nanoliposomes increased. The addition of cholesterol increased the zeta potential from -60.40 to -68.55 millivolt. Furthermore, cholesterol led to an increase in encapsulation efficiency, and even improved the stability of phenolic compounds loaded in nanoliposomes during storage time. Fourier transform infrared (FTIR) spectroscopy confirmed the successful loading of the extract. Field emission scanning electron microscopy (FE-SEM) analysis revealed nano-sized spherical and almost-elliptical liposomes. For jelly powders, the water solubility index ranged from 39.5 to 43.7% (p > 0.05), and the hygroscopicity values ranged between 1.22 and 9.36 g/100 g (p < 0.05). In conclusion, nanoencapsulated Capparis spinosa extract displayed improved stability and can be used in jelly preparation without any challenge or unfavorable perception.

Synthesis and Characterization of Self-Assembled Highly Stearate-Grafted Hydroxyethyl Starch Conjugates

Polysaccharide-based nanoformulations with tailored hydrophobic properties have become a frontier in nanomedicine applications. Herein, highly hydrophobicized hydroxyethyl starch (HES) conjugates were synthesized by grafting stearic acid (SA) with HES via a carbodiimide-mediated reaction. A detailed NMR characterization of HES and the conjugates was studied to obtain structural information. The grafting ratio of the stearate-HES (St-HES) conjugates was determined from 1H NMR spectra as 29.4% (St-HES29.4) and 60.3% (St-HES60.3). Thermal analyses and X-ray diffractograms suggested an entire transition from amorphous HES to a semicrystalline (St-HES60.3) character upon increasing the degree of grafting. Both conjugates, St-HES29.4 and St-HES60.3, were able to form self-assembled particles with a diameter of 130.7 nm and 152.5 nm, respectively. SEM images showed that the self-aggregates were mostly spherical in shape. These conjugates can be employed to entrap highly hydrophobic drugs with an increased encapsulation efficiency and loading capacity.

Tumour-specific hybrid nanoparticles in therapy of breast cancer

In this study, salicylic acid (SA) dopped into poly(3-hydroxybutyrate) (PHB) and prepared nanoparticles (NPs) to increase encapsulation efficiency, anti-cancer activity of caffeic acid (Caff), and folic acid (FA) for breast cancer treatment. NPs were prepared by solvent evaporation method and characterised by FTIR, DSC, SEM, and entrapment-loading efficiencies. The mean diameter, polydispersity index (PDI), and zeta potential (ZP) were evaluated by dynamic light scattering (DLS). In vitro release and stability studies were done via eppendorf method. The cytotoxicity, cell dead and internalisation of NPs were shown by MTT, fluorescein and confocal microscopy. The diameter and ZP of NPs were 172 ± 7 nm and −29 ± 0.38 mV. The entrapment efficiencies of 5 and 10 Caff NPs were 79 ± 0.23% and 70 ± 0.42%. NPs showed good stability within 30 d and sustained release over 25 d. FA-5Caff NPs showed 37 ± 0.3% viability on MCF-7. FA-Caff NPs were identified as promising carrier system for breast cancer therapy.

Bilosomes and Biloparticles for the Delivery of Lipophilic Drugs: A Preliminary Study.

In this study, bile acid-based vesicles and nanoparticles (i.e., bilosomes and biloparticles) are studied to improve the water solubility of lipophilic drugs. Ursodeoxycholic acid, sodium cholate, sodium taurocholate and budesonide were used as bile acids and model drugs, respectively. Bilosomes and biloparticles were prepared following standard protocols with minor changes, after a preformulation study. The obtained systems showed good encapsulation efficiency and dimensional stability. Particularly, for biloparticles, the increase in encapsulation efficiency followed the order ursodeoxycholic acid < sodium cholate < sodium taurocholate. The in vitro release of budesonide from both bilosytems was performed by means of dialysis using either a nylon membrane or a portion of Wistar rat small intestine and two receiving solutions (i.e., simulated gastric and intestinal fluids). Both in gastric and intestinal fluid, budesonide was released from bilosystems more slowly than the reference solution, while biloparticles showed a significant improvement in the passage of budesonide into aqueous solution. Immunofluorescence experiments indicated that ursodeoxycholic acid bilosomes containing budesonide are effective in reducing the inflammatory response induced by glucose oxidase stimuli and counteract ox-inflammatory damage within intestinal cells.

Chitosan nanoparticles-based in vivo delivery of miR-155 modulates the Viral haemorrhagic septicaemia virus-induced antiviral immune responses in zebrafish (Danio rerio)

Viral haemorrhagic septicaemia virus (VHSV) is one of the highly pathogenic virus, which causes viral haemorrhagic septicaemia disease in both marine and freshwater fish. Micro RNA-155 (miRNA-155) is a multifunctional small non-coding RNA and it involves regulation of immune responses during viral infection. In this study, dre-miR-155 mimics were encapsulated into chitosan nanoparticles (CNPs). Resulted encapsulated product (miR-155-CNPs) was investigated for its immunomodulation role in zebrafish during experimentally challenged VHSV infection. Successful encapsulation of dre-miR-155 mimics into CNPs was confirmed through average nanoparticle (NPs) size (341.45 ± 10.00 nm), increased encapsulation efficiency percentage (98.80%), bound dre-miR-155 with chitosan, sustained release in vitro (up to 40%), and the integrity of RNA. Overexpressed miR-155 was observed in gills, muscle, and kidney tissues (5.42, 19.62, and 140.72-folds, respectively) after intraperitoneal delivery of miR-155-CNPs into zebrafish upon VHSV infection (miR-155-CNPs + VHSV). The miR-155-CNPs + VHSV infected fish had the highest cumulative survival (85%), which was associated with low viral copy numbers. The miR-155-overexpressing fish showed significantly decreased expression of ifnγ, irf2bpl, irf9, socs1a, il10, and caspase3, compared to that of the miR-155 inhibitor + VHSV infected fish group. In contrast, il1β, tnfα, il6, cd8a, and p53 expressions were upregulated in miR-155-overexpressed zebrafish compared to that of the control. The overall findings indicate the successful delivery of dre-miR-155 through miR-155-CNPs that enabled restriction of VHSV infection in zebrafish presumably by modulating immune gene expression.

Enhanced tumor targeting with near-infrared light-activated indocyanine green encapsulated in covalent organic framework for combined photodynamic therapy (PDT) and photothermal therapy (PTT)

Covalent organic framework (COF), a new emerging class of crystalline porous polymeric networks with reversible covalent bonds are a better smart material in Nano medicine in this regard. 1,3,5-Triformylbenzene (TFB) and 2,5-Bis(methylsulfonyl)-1,4-diaminobenzene (BMSDAB) are used to develop a uniform shaped covalent organic framework at room temperature (RT-USCOF). In order to achieve the PTT and PDT effect in RT-USCOF, near infrared photosensitizer, photothermal and fluorescence agent, indocyanine green (ICG) was encapsulated. Moreover, enhanced loading content of ICG in I RT-USCOF to produce II RT-USCOF followed by stabilize with hyaluronic acid designed in order to reduce drug leakage and increase carrier stability. The II RT-USCOF-HA exhibits an increased encapsulation efficiency of 57.75% and a drug loading capacity of 53.59%. The developed system shows an 80% ICG release upon exposure to NIR 808-laser in acidic pH relative to the one without light irradiation proved the effective structural changes under light cause drug release. The newly developed II RT-USCOF-HA shows excellent biocompatibility against NIH 3T3 cell lines and CT2A cell lines under dark. Whereas, upon irradiation with NIR 808 nm laser, the system kills more than 70% of the cells and cellular uptake studies also proved the same. Finally, flow cytometry analysis confirmed, the II-RT-USCOF-HA treated with CT2A cell lines shows an early apoptosis cell population of 1.95%, a late apoptosis rate of 1.24% and a necrotic cell death of 4.77%, which are significantly greater than the free ICG treated groups. The singlet oxygen production followed by thermal ablation of tumor cells by the developed system further demonstrates its efficacy as a PDT/PTT probe.

Native and pregelatinized potato and rice starches and maltodextrin as encapsulating agents for linseed oil ethyl esters – Comparison of emulsion and powder properties

This study compared selected physical and chemical properties of emulsions and encapsulated powders containing linseed oil ethyl esters prepared with native and pregelatinized rice and potato starches, and potato maltodextrin. Emulsions with native starches and maltodextrin met the criteria of a Newtonian fluid, while with pregelatinized starches showed characteristics of a non-Newtonian fluid. The pregelatinized starches improved the emulsions’ stability, yet emulsion degradation by creaming was comparable to that of emulsion containing maltodextrin. Only pregelatinized potato starch was characterized by increased encapsulation efficiency. Capsules made with both rice starches and native potato starch were more oxidatively stable than that made with maltodextrin. Additionally, both powders with potato starch and pregelatinized rice starch showed a lower release of volatiles related to oxidation. Summarizing, pregelatinized potato starch displayed potential to replace maltodextrin based on relatively high encapsulation efficiency and high potential to diminish volatiles connected with oxidation processes, like hexanal.

A non-thermal modification method to promote the interaction of zein-alginate oligosaccharides composites for better encapsulation and stability—Cold plasma

This current research explored the application of cold plasma (CP) treatment to modify zein-alginate oligosaccharide (zein-AOS) composites in an ethanol-water solution. Anti-solvent method was used to prepare zein-AOS nanoparticles (NPs), and the objective was to investigate the mechanism by which CP promotes interaction between protein and saccharides. Characterization results indicated that CP treatment improved hydrogen bonding and electrostatic interaction between zein and AOS. The CP zein-AOS NPs underwent dispersion and rearrangement, resulting in smaller aggregates with better dispersibility. Among the various induction conditions tested, the zein-AOS85 NPs (induced at 85 W for 2 min) exhibited superior performance as delivery wall materials, with smaller particle size (234.67 nm), larger specific surface area (9.443 m2/g), and higher surface charge (−35.43 mV). In addition, zein-AOS85 showed high stability when used as delivery wall material, providing more binding sites and self-assembly dynamics for nutrients. Curcumin was used as the nutrient model in this study, and CP was found to enhance hydrogen bonding, electrostatic interaction, and hydrophobic interaction between zein, AOS, and nutrients, resulting in increased encapsulation efficiency (EE) from 63.80 % to 85.17 %. The delivery system also exhibited good pH, ionic strength, storage, and dispersion stability.

Development of Liposomal and Liquid Crystalline Lipidic Nanoparticles with Non-Ionic Surfactants for Quercetin Incorporation.

The aim of the present study is the development, physicochemical characterization, and in vitro cytotoxicity evaluation of both empty and quercetin-loaded HSPC (hydrogenated soy phosphatidylcholine) liposomes, GMO (glyceryl monooleate) liquid crystalline nanoparticles, and PHYT (phytantriol) liquid crystalline nanoparticles. Specifically, HSPC phospholipids were mixed with different non-ionic surfactant molecules (Tween 80 and/or Span 80) for liposomal formulations, whereas both GMO and PHYT lipids were mixed with Span 80 and Tween 80 as alternative stabilizers, as well as with Poloxamer P407 in different ratios for liquid crystalline formulations. Subsequently, their physicochemical properties, such as size, size distribution, and ζ-potential were assessed by the dynamic and electrophoretic light scattering (DLS/ELS) techniques in both aqueous and biological medium with serum proteins. The in vitro biological evaluation of the empty nanosystems was performed by using the MTT cell viability and proliferation assay. Finally, the entrapment efficiency of quercetin was calculated and the differences between the two different categories of lipidic nanoparticles were highlighted. According to the results, the incorporation of the non-ionic surfactants yields a successful stabilization and physicochemical stability of both liposomal and liquid crystalline nanoparticles. Moreover, in combination with an appropriate biosafety in vitro profile, increased encapsulation efficiency of quercetin was achieved. Overall, the addition of surfactants improved the nanosystem's stealth properties. In conclusion, the results indicate that the physicochemical properties were strictly affected by the formulation parameters, such as the type of surfactant.

Fabrication and characterization of zein-sodium alginate complex nanoparticles as an effective naringenin delivery system: Physicochemical stability, solubility, antioxidant activity

Naringenin (NAR) is a native polyphenolic compound that has a variety of physiological benefits. However, the application of NAR in functional food fields is limited due to its high hydrophobicity and insufficient oral bioavailability. The objective of this study is to prepare naringenin-encapsulated zein-sodium alginate nanoparticles (NAR-Z/SA NPs) to improve the antioxidant effects of NAR by increasing the water solubility. The spherical NAR-Z/SA NPs possessed increased encapsulation efficiency (83.92 ± 0.32%) and loading capacity (18.24 ± 0.73%). The X-ray diffraction and differential scanning calorimetry results confirmed that NAR was in an amorphous state after being encapsulated. Fourier transform infrared spectroscopy revealed that hydrogen bonding, electrostatic interaction, and hydrophobic interaction drove the formation of the NAR-Z/SA NPs. Meanwhile, NAR-Z/SA NPs exhibited desirable pH (3.0–8.0), ionic (0–50 mM) and heating treatment (80°C) stability. Furthermore, NAR-Z/SA NPs had improved solubility and antioxidant activity compared with free NAR. In addition, the NAR-Z/SA NPs showed sustained release of NAR under simulated gastrointestinal conditions. These findings provide an effective choice for the broad application of NAR in food industries.

Development of probiotic-loaded calcium alginate-maltodextrin microparticles based on electrohydrodynamic technique

Maintaining the viability of probiotic bacteria in food products for intestinal delivery remains a challenge. Consequently, the objective of this study was to encapsulate Lactobacillus rhamnosus (NCDC 18) in calcium alginate–maltodextrin hydrogel systems by combining electrospraying and freeze-drying techniques. The microparticles were produced using varying concentrations of sodium alginate (SA) (2, 3, and 4%) in conjunction with maltodextrin (MD) (0, 2, and 4%). A definitive screening design (DSD) was used to design experiments and explain the effect of independent variables (concentrations of SA, calcium chloride, and MD and electrospraying voltage) on the response variables: loss of viability, encapsulation efficiency, drying yield, Carr's index, and Hausner ratio. The obtained microparticles were characterized by employing Scanning Electron Microscopy (SEM), Fourier Transform Infrared Spectroscopy (FTIR), and Differential Scanning Calorimetry (DSC). The addition of MD significantly increased encapsulation efficiency up to 75.19% and decreased viability loss up to 2.539 log CFU/mL in microparticles. The morphological analysis revealed the particle surface structure and variation in porosity in response to varying variables. The FTIR spectra confirmed that the addition of SA, MD, and probiotics caused synergistic changes in the functional bonding. The XRD analysis could further elucidate the interactions of SA with MD in the microcapsules. Our study could confirm that MD acted as a cryoprotectant and decreased the concavities and pores on the surface of the microparticles, thereby enhancing their probiotic-related properties.

Antibiotics modified by hydrophobic ion-pairing – A solution world's problems with resistant bacteria?

Resistance to antibiotics is one of the greatest dangers to the humanity, according to the World Health Organization. To reduce the amount of used antibiotics, various targeted drug delivery is considered, e.g., biopolymeric micro- or nanoparticles, electrospun nanofibers, or self-emulsifying drug delivery systems. In the case of hydrophilic antibiotics, there is an issue of relatively low encapsulation efficiencies and too rapid release, due to chemical character impairment (hydrophobic carrier – hydrophilic antibiotic). It results in not only lower clinical success rate, but also in creating a huge antibiotic waste when the manufacturing process is converted to the industrial conditions. A possible solution to overcome these problems is changing the chemical character of the antibiotics by a simple reaction of ion pairing with either cationic or ionic surfactants that may decrease water solubility of antibiotics without any loss, or with even better, bactericidal properties. This approach increases encapsulation efficiency up to nearly 100%. As the result, lower doses of antibiotics can be used in drug delivery systems that provide a more sustainable release. However, there is a risk of a higher toxicity due to the presence of surfactants and the origin of improved antibacterial properties have not yet been fully explained. Herein, we present the review of the current achievements in the field of antibiotics hydrophobized by hydrophobic ion pairing (HIP) for various drug delivery systems with the special regard to the antibacterial properties and biocompatibility.

Synthesis and Characterization of PCL-Idebenone Nanoparticles for Potential Nose-to-Brain Delivery.

The present work is focused on the preparation of an optimal model of poly-ε-caprolactone nanoparticles as potential carriers for nasal administration of idebenone. A solvent/evaporation technique was used for nanoparticle preparation. Poly-ε-caprolactone with different molecular weights (14,000 and 80,000 g/mol) was used. Polysorbate 20 and Poloxamer 407, alone and in combination, were used as emulsifiers at different concentrations to obtain a stable formulation. The nanoparticles were characterized using dynamic light scattering, SEM, TEM, and FTIR. The resulting structures were spherical in shape and their size distribution depended on the type of emulsifier. The average particle size ranged from 188 to 628 nm. The effect of molecular weight and type of emulsifier was established. Optimal models of appropriate size for nasal administration were selected for inclusion of idebenone. Three models of idebenone-loaded nanoparticles were developed and the effect of molecular weight on the encapsulation efficiency was investigated. Increased encapsulation efficiency was found when poly-ε-caprolactone with lower molecular weight was used. The molecular weight also affected the drug release from the nanostructures. Dissolution study data were fitted into various kinetic models and the Korsmeyer-Peppas model was found to be indicative of the release mechanism of idebenone.